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Angiogenesis JAK

JAK

Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. They were initially named "just another kinase" 1 and 2 (since they were just two of many discoveries in a PCR-based screen of kinases), but were ultimately published as "Janus kinase". The name is taken from the two-faced Roman god of beginnings, endings and duality, Janus, because the JAKs possess two near-identical phosphate-transferring domains. One domain exhibits the kinase activity, while the other negatively regulates the kinase activity of the first.
Cat No. product name
T1829 RuxolitinibHOT Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC50: 3.3/2.8 nM) and is relatively less selective for JAK3 (IC50: 322 nM).
T1849 Momelotinib Momelotinib is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with...
T1929 Filgotinib GLPG0634(filgotinib) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.
T1985 WHI-P154 WHI-P154 is a potent JAK3 inhibitor.
T1995 FedratinibHOT Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
T2012 Oclacitinib Oclacitinib(PF03394197) is a potent and selective JAKs inhibitor with IC50 of 10-99 nM; not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nM).
T2035 WHI-P258 WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of ne...
T2045 WHI-P131 Janex-1 is a cell-permeable, reversible, effective, ATP-competitive, and selective inhibitor of JAK3 (IC50: 78 μM); little inhibitory against JAK1/2, or Zap/Sy...
T2156 WP1066 WP1066 is a inhibitor of JAK2 (IC50: 2.30 μM) and STAT3 (IC50: 2.43 μM) in HEL cells; shows activity to JAK2, STAT3/5, and ERK1/2, not JAK1 and JAK3. WP1066 h...
T7499 TAK-779 TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
T2360 Baricitinib Phosphate Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
T2398 Tofacitinib CitrateHOT Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
T2460 JAK 3 inhibitor IV JAK 3 inhibitor IV is a JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transgluta...
T2485 Baricitinib Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activit...
T2487 Cerdulatinib Cerdulatinib is an novel oral dual Syk/JAK inhibitor.
T2600 AG490 AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn,...
T2636 Decernotinib Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
T2638 Gandotinib LY2784544(Gandotinib) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3...
T2709 TAK901 TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others...
T2853 Curcumol Curcumol, a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
T3042 JAK2 Inhibitor V NSC 42834(JAK2 Inhibitor V, Z3) is a novel specific inhibitor of Jak2, inhibiting Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner.
T3043 Ruxolitinib (INCB-18424) phosphate Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivi...
T3065 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
T3068 AT9283 AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
T3069 AZD1480 AZD1480 is a novel ATP-competitive JAK2 inhibitor (IC50: 0.26 nM), selectivity act against Tyk2 and JAK3, and to a smaller extent against JAK1. AZD1480 has been...
T3072 XL019 XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
T3076 GLPG0634 analogue GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
T3080 Pyridone 6 Pyridone 6(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying sign...
T3201 WDR5-0103 WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
T3398 Icaritin Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apopt...
T3620 Solcitinib Solcitinib (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus...
T3673 Mollugin Mollugin may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for...
T3998 Itacitinib Itacitinib is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
T4209 TAK-659 hydrochloride TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent...
T4210 SAR20347 SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
T4227 SB1317 hydrochloride (1204918-72-8(free base)) SB1317 is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
T6020 Pacritinib Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
T6104 Cerdulatinib hydrochloride Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and ...
T6124 Mubritinib Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
T6156 S-Ruxolitinib Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
T6266 PP2 PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
T5049 NVP-BSK805 NVP-BSK805 is an ATP-competitive JAK2 inhibitor.
T6309 AZ 960 AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
T6321 Tofacitinib Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
T6790 BMS911543 BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
T6838 FLLL32 FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).
T6914 Oclacitinib maleate Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, whic...
T6916 OICR9429 OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukem...
T6122 CEP33779 CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
T7503 Upadacitinib Upadacitinib (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43...
T4476 AS1517499 AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM
T4657 WHI-P97 WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipox...
T5091 FM381 FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK...
T5140 WDR5-0103 hydrochloride[890190-22-4(free base)] WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
T6145 ZM 39923 HCl ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminas...
T5382 PF-06651600 PF-06651600 is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
T5492 JAK3-IN-6 JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM
TQ0037 Abrocitinib Abrocitinib (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).
TQ0061 CHZ868 CHZ868 is a type II JAK2 inhibitor (IC50: 0.17 μM in EPOR JAK2 WT Ba/F3 cell).
TQ0010 PF-06700841 PF-06700841 is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). It also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).
TQ0196 Cucurbitacin I Cucurbitacin I, a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
T3024 Avitinib Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with poten...
T6920 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).
TN1059 Ganoderic acid B Ganoderic acid B is a chemical marker in quality control of G. lucidum and related products. Ganoderic acid B-containing herbs has potential influence towards t...
TN2002 Obovatol Obovatol has antioxidant, neuroprotective, antiinflammatory, antithrombotic and antitumour effects, it is a potent NF-κB inhibitors for Alzheimer's disease tre...
T12091L MM-589 TFA MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
T12091 MM-589 MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
T12427 PF-06700841 (P-Tosylate) PF-06700841 P-Tosylate is a potent dual inhibitor of Janus kinase 1 (JAK1) and TYK2 (IC50s of 17 nM and 23 nM, respectively).
T12549 JAK-IN-11 JAK-IN-11 is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.
T10424 AZ-3 AZ-3 is a potent and selective JAK1 inhibitor (IC50: 34 nM).
T10431 AZD4205 AZD4205 is a selective JAK1 inhibitor (IC50: 73 nM) and weakly inhibits JAK2/JAK3 (IC50: >14.7, >30 μM).
T14687 BMS-986165 BMS-986165 inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of...
T15037 Momelotinib Mesylate Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
T15038 Momelotinib sulfate Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
T15096 Delgocitinib Delgocitinib is a novel and specific inhibitor of JAK (IC50s: 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2).
T15606 JAK1-IN-4 JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in...
T10009 JAK3-IN-7 JAK3-IN-7 is an effective and selective JAK3 inhibitor (IC50 <0.01 μM) extracted from patent WO2011013785A1.
T11690 ITK inhibitor 2 ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor , with an IC50 of 2 nM.
T11708 JAK2-IN-4 JAK2-IN-4 is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.
T11709 JAK3 covalent inhibitor-1 JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs.
T11710 JAK-IN-5 JAK-IN-5 is an inhibitor of JAK.
T11711 Jaspamycin Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity. Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to ...
T11713 JBJ-02-112-05 JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
T11714 JBJ-04-125-02 JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities. JBJ-04-125-02 is a potent, mut...
T11721L JDTic dihydrochloride JDTic is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
T11721 JDTic JDTic has a very long duration of action, with effects in animals seen for up to several weeks after administration of a single dose, although its binding to th...
T8546 BD750 BD750 is an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation(IC50 of 1.5 μM and 1.1 μM ...
T16995 TAS05567 TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3,...
T2S1040 Jolkinolide B Jolkinolide B has potent anti-inflammatory, and antitumor activities, it is able to enhance apoptosis of human leukemic HL-60 and THP-1 cells, at least in part,...
T2S1975 Ponicidin Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infecti...
T4672 Brevilin A Brevilin A is a sesquiterpene lactone isolated from Centipeda minima, inhibits janus kinase activity and blocks STAT3 signaling in cancer cells with anti-tumor ...
T5S0993 Kurarinone Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong...
T5S1467 Cucurbitacin E Cucurbitacin E is a natural product isolated from the climbing stem of Cucumic melo L. It significantly suppresses the activity of the cyclin B1/CDC2 complex.Cu...
TJS1779 Protosappanin A Protosappanin A has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB infl...
TN2511 1,6-O,O-Diacetylbritannilactone 1,6-O,O-Diacetylbritannilactone(OODBL) has anti-inflammatory activity, it has a potential therapeutic efficacy on inflammatory diseases especially allergic airw...
TN2775 2-Methoxystypandrone 2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the infl...
TN3364 Agrimonolide Agrimonolide is a potential α1 adrenergic receptor antagonist, it exerts anti-inflammatory activity, at least in part, via suppressing LPS-induced activation o...
TN3541 Broussonin E Broussonin E could suppress inflammation by modulating macrophages activation state via inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathw...
TMA1743 Ergosterol peroxide Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Fo...
TN4774 Physalin A Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate can...
T2341 KW2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-...
T17019 TCS 21311 TCS 21311 is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respective...
T14331 Gusacitinib Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
T8742 JAK2 inhibitor G5-7 JAK2 inhibitor G5-7 is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by bin...
T8719 SC99 SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregati...
T4657L WHI-P97 HCl 211555-05-4(free base) WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 ...
T4657L WHI-P97 HCl 211555-05-4(free base) WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 ...
Ruxolitinib HOT
T1829CAS 941678-49-5
Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC50: 3.3/2.8 nM) and is relatively less selective for JAK3 (IC50: 322 nM).
Momelotinib
T1849CAS 1056634-68-4
Momelotinib is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with...
Filgotinib
T1929CAS 1206161-97-8
GLPG0634(filgotinib) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.
WHI-P154
T1985CAS 211555-04-3
WHI-P154 is a potent JAK3 inhibitor.
Fedratinib HOT
T1995CAS 936091-26-8
Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
Oclacitinib
T2012CAS 1208319-26-9
Oclacitinib(PF03394197) is a potent and selective JAKs inhibitor with IC50 of 10-99 nM; not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nM).
WHI-P258
T2035CAS 21561-09-1
WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of ne...
WHI-P131
T2045CAS 202475-60-3
Janex-1 is a cell-permeable, reversible, effective, ATP-competitive, and selective inhibitor of JAK3 (IC50: 78 μM); little inhibitory against JAK1/2, or Zap/Sy...
WP1066
T2156CAS 857064-38-1
WP1066 is a inhibitor of JAK2 (IC50: 2.30 μM) and STAT3 (IC50: 2.43 μM) in HEL cells; shows activity to JAK2, STAT3/5, and ERK1/2, not JAK1 and JAK3. WP1066 h...
TAK-779
T7499CAS 229005-80-5
TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
Baricitinib Phosphate
T2360CAS 1187595-84-1
Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
Tofacitinib Citrate HOT
T2398CAS 540737-29-9
Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
JAK 3 inhibitor IV
T2460CAS 58753-54-1
JAK 3 inhibitor IV is a JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transgluta...
Baricitinib
T2485CAS 1187594-09-7
Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activit...
Cerdulatinib
T2487CAS 1198300-79-6
Cerdulatinib is an novel oral dual Syk/JAK inhibitor.
AG490
T2600CAS 133550-30-8
AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn,...
Decernotinib
T2636CAS 944842-54-0
Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
Gandotinib
T2638CAS 1229236-86-5
LY2784544(Gandotinib) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3...
TAK901
T2709CAS 934541-31-8
TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others...
Curcumol
T2853CAS 4871-97-0
Curcumol, a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
JAK2 Inhibitor V
T3042CAS 195371-52-9
NSC 42834(JAK2 Inhibitor V, Z3) is a novel specific inhibitor of Jak2, inhibiting Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner.
Ruxolitinib (INCB-18424) phosphate
T3043CAS 1092939-17-7
Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivi...
TG101209
T3065CAS 936091-14-4
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
AT9283
T3068CAS 896466-04-9
AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
AZD1480
T3069CAS 935666-88-9
AZD1480 is a novel ATP-competitive JAK2 inhibitor (IC50: 0.26 nM), selectivity act against Tyk2 and JAK3, and to a smaller extent against JAK1. AZD1480 has been...
XL019
T3072CAS 945755-56-6
XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
GLPG0634 analogue
T3076CAS 1206101-20-3
GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
Pyridone 6
T3080CAS 457081-03-7
Pyridone 6(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying sign...
WDR5-0103
T3201CAS 890190-22-4
WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
Icaritin
T3398CAS 118525-40-9
Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apopt...
Solcitinib
T3620CAS 1206163-45-2
Solcitinib (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus...
Mollugin
T3673CAS 55481-88-4
Mollugin may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for...
Itacitinib
T3998CAS 1334298-90-6
Itacitinib is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
TAK-659 hydrochloride
T4209CAS 1952251-28-3
TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent...
SAR20347
T4210CAS 1450881-55-6
SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
SB1317 hydrochloride (1204918-72-8(free base))
T4227CAS T4227
SB1317 is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
Pacritinib
T6020CAS 937272-79-2
Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
Cerdulatinib hydrochloride
T6104CAS 1369761-01-2
Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and ...
Mubritinib
T6124CAS 366017-09-6
Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
S-Ruxolitinib
T6156CAS 941685-37-6
Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
PP2
T6266CAS 172889-27-9
PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
NVP-BSK805
T5049CAS 1092499-93-8
NVP-BSK805 is an ATP-competitive JAK2 inhibitor.
AZ 960
T6309CAS 905586-69-8
AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
Tofacitinib
T6321CAS 477600-75-2
Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
BMS911543
T6790CAS 1271022-90-2
BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
FLLL32
T6838CAS 1226895-15-3
FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).
Oclacitinib maleate
T6914CAS 1640292-55-2
Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, whic...
OICR9429
T6916CAS 1801787-56-3
OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukem...
CEP33779
T6122CAS 1257704-57-6
CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
Upadacitinib
T7503CAS 1310726-60-3
Upadacitinib (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43...
AS1517499
T4476CAS 919486-40-1
AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM
WHI-P97
T4657CAS 211555-05-4
WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipox...
FM381
T5091CAS 2226521-65-7
FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK...
WDR5-0103 hydrochloride[890190-22-4(free base)]
T5140CAS T5140
WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
ZM 39923 HCl
T6145CAS 1021868-92-7
ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminas...
PF-06651600
T5382CAS 1792180-81-4
PF-06651600 is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
JAK3-IN-6
T5492CAS 1443235-95-7
JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM
Abrocitinib
TQ0037CAS 1622902-68-4
Abrocitinib (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).
CHZ868
TQ0061CAS 1895895-38-1
CHZ868 is a type II JAK2 inhibitor (IC50: 0.17 μM in EPOR JAK2 WT Ba/F3 cell).
PF-06700841
TQ0010CAS 1883299-62-4
PF-06700841 is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). It also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).
Cucurbitacin I
TQ0196CAS 2222-07-3
Cucurbitacin I, a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
Avitinib
T3024CAS 1557267-42-1
Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with poten...
ON123300
T6920CAS 1357470-29-1
ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).
Ganoderic acid B
TN1059CAS 81907-61-1
Ganoderic acid B is a chemical marker in quality control of G. lucidum and related products. Ganoderic acid B-containing herbs has potential influence towards t...
Obovatol
TN2002CAS 83864-78-2
Obovatol has antioxidant, neuroprotective, antiinflammatory, antithrombotic and antitumour effects, it is a potent NF-κB inhibitors for Alzheimer's disease tre...
MM-589 TFA
T12091LCAS 2097887-21-1
MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
MM-589
T12091CAS 2097887-20-0
MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
PF-06700841 (P-Tosylate)
T12427CAS 2140301-96-6
PF-06700841 P-Tosylate is a potent dual inhibitor of Janus kinase 1 (JAK1) and TYK2 (IC50s of 17 nM and 23 nM, respectively).
JAK-IN-11
T12549CAS 916742-11-5
JAK-IN-11 is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.
AZ-3
T10424CAS 2228908-91-4
AZ-3 is a potent and selective JAK1 inhibitor (IC50: 34 nM).
AZD4205
T10431CAS 2091134-68-6
AZD4205 is a selective JAK1 inhibitor (IC50: 73 nM) and weakly inhibits JAK2/JAK3 (IC50: >14.7, >30 μM).
BMS-986165
T14687CAS 1609392-27-9
BMS-986165 inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of...
Momelotinib Mesylate
T15037CAS 1056636-07-7
Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
Momelotinib sulfate
T15038CAS 1056636-06-6
Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
Delgocitinib
T15096CAS 1263774-59-9
Delgocitinib is a novel and specific inhibitor of JAK (IC50s: 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2).
JAK1-IN-4
T15606CAS 2091134-35-7
JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in...
JAK3-IN-7
T10009CAS 1263774-57-7
JAK3-IN-7 is an effective and selective JAK3 inhibitor (IC50 <0.01 μM) extracted from patent WO2011013785A1.
ITK inhibitor 2
T11690CAS 1309784-09-5
ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor , with an IC50 of 2 nM.
JAK2-IN-4
T11708CAS 1438284-00-4
JAK2-IN-4 is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.
JAK3 covalent inhibitor-1
T11709CAS 2300106-50-5
JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs.
JAK-IN-5
T11710CAS 2096999-92-5
JAK-IN-5 is an inhibitor of JAK.
Jaspamycin
T11711CAS 22242-96-2
Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity. Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to ...
JBJ-02-112-05
T11713CAS T11713
JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
JBJ-04-125-02
T11714CAS 2060610-53-7
JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities. JBJ-04-125-02 is a potent, mut...
JDTic dihydrochloride
T11721LCAS 785835-79-2
JDTic is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
JDTic
T11721CAS 361444-66-8
JDTic has a very long duration of action, with effects in animals seen for up to several weeks after administration of a single dose, although its binding to th...
BD750
T8546CAS 892686-59-8
BD750 is an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation(IC50 of 1.5 μM and 1.1 μM ...
TAS05567
T16995CAS 1429038-15-2
TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3,...
Jolkinolide B
T2S1040CAS 37905-08-1
Jolkinolide B has potent anti-inflammatory, and antitumor activities, it is able to enhance apoptosis of human leukemic HL-60 and THP-1 cells, at least in part,...
Ponicidin
T2S1975CAS 52617-37-5
Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infecti...
Brevilin A
T4672CAS 16503-32-5
Brevilin A is a sesquiterpene lactone isolated from Centipeda minima, inhibits janus kinase activity and blocks STAT3 signaling in cancer cells with anti-tumor ...
Kurarinone
T5S0993CAS 34981-26-5
Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong...
Cucurbitacin E
T5S1467CAS 18444-66-1
Cucurbitacin E is a natural product isolated from the climbing stem of Cucumic melo L. It significantly suppresses the activity of the cyclin B1/CDC2 complex.Cu...
Protosappanin A
TJS1779CAS 102036-28-2
Protosappanin A has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB infl...
1,6-O,O-Diacetylbritannilactone
TN2511CAS 1286694-67-4
1,6-O,O-Diacetylbritannilactone(OODBL) has anti-inflammatory activity, it has a potential therapeutic efficacy on inflammatory diseases especially allergic airw...
2-Methoxystypandrone
TN2775CAS 85122-21-0
2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the infl...
Agrimonolide
TN3364CAS 21499-24-1
Agrimonolide is a potential α1 adrenergic receptor antagonist, it exerts anti-inflammatory activity, at least in part, via suppressing LPS-induced activation o...
Broussonin E
TN3541CAS 90902-21-9
Broussonin E could suppress inflammation by modulating macrophages activation state via inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathw...
Ergosterol peroxide
TMA1743CAS 2061-64-5
Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Fo...
Physalin A
TN4774CAS 23027-91-0
Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate can...
KW2449
T2341CAS 1000669-72-6
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-...
TCS 21311
T17019CAS 1260181-14-3
TCS 21311 is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respective...
Gusacitinib
T14331CAS 1425381-60-7
Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
JAK2 inhibitor G5-7
T8742CAS 939681-36-4
JAK2 inhibitor G5-7 is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by bin...
SC99
T8719CAS 882290-02-0
SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregati...
WHI-P97 HCl 211555-05-4(free base)
T4657LCAS T4657L
WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 ...
WHI-P97 HCl 211555-05-4(free base)
T4657LCAS T4657L
WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 ...