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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 (R)-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/S...
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).
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 AG-490 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 SAR-20347 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 BMS-911543 BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1nM, ~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 <p>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, w...
T6916 OICR-9429 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...
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 4...
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...
(R)-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/S...
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).
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.
AG-490
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...
SAR-20347
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.
BMS-911543
T6790CAS 1271022-90-2
BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1nM, ~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
<p>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, w...
OICR-9429
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...
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 4...
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...