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JAK

The JAK-STAT signalling pathway is a chain of interactions between proteins in a cell, and is involved in processes such as immunity, cell division, cell death and tumour formation. There are 4 JAK proteins: JAK1, JAK2, JAK3 and TYK2. JAKs contains a FERM domain (approximately 400 residues), an SH2-related domain (approximately 100 residues), a kinase domain (approximately 250 residues) and a pseudokinase domain (approximately 300 residues). The kinase domain is vital for JAK activity, since it allows JAKs to phosphorylate (add phosphate groups to) proteins.
Cat No. product name
T2341 KW-2449 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-1R...
T6515 Go6976 Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and ...
T9251 Fedratinib hydrochloride hydrate Fedratinib hydrochloride hydrate is a potent, selective, ATP-competitive and orally active JAK2 inhibitor.
T1829 Ruxolitinib 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).
T38624 Fosifidancitinib Fosifidancitinib is a potent inhibitor of JAK 1 and JAK 3.
T2709 TAK-901 TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others....
T3201 WDR5-0103 WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
T6S1966 Curculigoside 1. Curculigoside can prevent bone loss , improve osteogenesis and inhibit osteoclastogenesis of hAFSCs, suggesting its potential use to regulate hAFSC osteogenic...
T6309 AZ960 AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
T6838 FLLL32 FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).
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 th...
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 new...
T3065 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
T2360 Baricitinib phosphate Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
T2398 Tofacitinib Citrate Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
T2853 Curcumol Curcumol, a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
T6321 Tofacitinib Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
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....
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 has ...
T6217 LFM-A13 LFM-A13(IC50=2.5 μM), a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and...
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 ...
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).
T2S1975 Ponicidin Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infectio...
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 inflammat...
T8719 SC99 SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation...
T3398 Icaritin Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apopto...
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 leukemi...
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, L...
T9195 SHR0302 SHR0302 is a JAK inhibitor that binds JAK1 with stronger affinity than others (Selectivity for JAK1 is more than 10 times for JAK2, 77 times for JAK3, 420 times ...
T14331 Gusacitinib Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
T5S0167 Atractylenolide I 1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reductio...
T21503 (E/Z)-Zotiraciclib (E/Z)-Zotiraciclib inhibits CDK2, JAK2, and FLT3 effectively with IC50s of 13, 73, and 56 nM, respectively.
T1985 WHI-P154 WHI-P154 is a potent JAK3 inhibitor.
T8742 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 binding ...
T2378 RGB-286638 free base RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3...
T1995 Fedratinib Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
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).
T14687 Deucravacitinib 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 ...
T22338 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide GDC046, a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.
T2485 Baricitinib Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activiti...
T6145 ZM39923 hydrochloride 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 transglutaminase...
T3043 Ruxolitinib 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 selectivit...
T9826 GDC-0214 GDC-0214 is an inhaled small-molecule JAK1 inhibitor and reduces fractional exhaled nitric oxide (Feno).
T3072 XL019 XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
T7123 AMG-47a AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the lev...
T22319 DTP3 DTP3 is a selective MKK7/GADD45β inhibitor, which inhibits cancer-selective NF-κB survival pathway.
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 a...
T4S1499 Ginsenoside Rk1 Ginsenoside Rk1 is a component created by processing the ginseng plant at high temperatures. Ginsenoside Rk1 has an anti-inflammatory effect, suppresses the acti...
T35341 NVP-BSK805 dihydrochloride NVP-BSK805 2HCl是一种有效的,选择性的,ATP竞争性的JAK2抑制剂,IC50为0.5 nM,比作用于JAK1, JAK3和TYK2选择性高20倍以上。
T22142 RO8191 RO8191 (CDM-3008), an imidazonaphthyridine compound, is an agonist of interferon (IFN) receptor.
KW-2449
T2341
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-1...
Go6976
T6515
Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 an...
Fedratinib hydrochloride hydrate
T9251
Fedratinib hydrochloride hydrate is a potent, selective, ATP-competitive and orally active JAK2 inhibitor.
Ruxolitinib
T1829
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).
Fosifidancitinib
T38624
Fosifidancitinib is a potent inhibitor of JAK 1 and JAK 3.
TAK-901
T2709
TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others....
WDR5-0103
T3201
WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
Curculigoside
T6S1966
1. Curculigoside can prevent bone loss , improve osteogenesis and inhibit osteoclastogenesis of hAFSCs, suggesting its potential use to regulate hAFSC osteogenic...
AZ960
T6309
AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
FLLL32
T6838
FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).
Ganoderic acid B
TN1059
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 th...
WHI-P258
T2035
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 new...
TG101209
T3065
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
Baricitinib phosphate
T2360
Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
Tofacitinib Citrate
T2398
Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
Curcumol
T2853
Curcumol, a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
Tofacitinib
T6321
Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
Gandotinib
T2638
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....
WP1066
T2156
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 ha...
LFM-A13
T6217
LFM-A13(IC50=2.5 μM), a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR...
Momelotinib
T1849
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 ...
AT9283
T3068
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).
Ponicidin
T2S1975
Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infectio...
Protosappanin A
TJS1779
Protosappanin A has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB infla...
SC99
T8719
SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation...
Icaritin
T3398
Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apopto...
OICR-9429
T6916
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 leukemi...
AG490
T2600
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, ...
SHR0302
T9195
SHR0302 is a JAK inhibitor that binds JAK1 with stronger affinity than others (Selectivity for JAK1 is more than 10 times for JAK2, 77 times for JAK3, 420 times ...
Gusacitinib
T14331
Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
Atractylenolide I
T5S0167
1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reducti...
(E/Z)-Zotiraciclib
T21503
(E/Z)-Zotiraciclib inhibits CDK2, JAK2, and FLT3 effectively with IC50s of 13, 73, and 56 nM, respectively.
WHI-P154
T1985
WHI-P154 is a potent JAK3 inhibitor.
G5-7
T8742
JAK2 inhibitor G5-7 is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by bindin...
RGB-286638 free base
T2378
RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3...
Fedratinib
T1995
Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
ON123300
T6920
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).
Deucravacitinib
T14687
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 ...
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
T22338
GDC046, a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.
Baricitinib
T2485
Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activiti...
ZM39923 hydrochloride
T6145
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 transglutaminase...
Ruxolitinib phosphate
T3043
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 selectivit...
GDC-0214
T9826
GDC-0214 is an inhaled small-molecule JAK1 inhibitor and reduces fractional exhaled nitric oxide (Feno).
XL019
T3072
XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
AMG-47a
T7123
AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the lev...
DTP3
T22319
DTP3 is a selective MKK7/GADD45β inhibitor, which inhibits cancer-selective NF-κB survival pathway.
Brevilin A
T4672
Brevilin A is a sesquiterpene lactone isolated from Centipeda minima, inhibits janus kinase activity and blocks STAT3 signaling in cancer cells with anti-tumor a...
Ginsenoside Rk1
T4S1499
Ginsenoside Rk1 is a component created by processing the ginseng plant at high temperatures. Ginsenoside Rk1 has an anti-inflammatory effect, suppresses the acti...
NVP-BSK805 dihydrochloride
T35341
NVP-BSK805 2HCl是一种有效的,选择性的,ATP竞争性的JAK2抑制剂,IC50为0.5 nM,比作用于JAK1, JAK3和TYK2选择性高20倍以上。
RO8191
T22142
RO8191 (CDM-3008), an imidazonaphthyridine compound, is an agonist of interferon (IFN) receptor.
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