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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
TQ0010 Brepocitinib 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).
T1995 Fedratinib Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
TQ0037 Abrocitinib Abrocitinib (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).
T14331 Gusacitinib Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
T3201 WDR5-0103 WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
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, which...
T15038 Momelotinib sulfate Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
T3076 GLPG0634 analog GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
T2S1040 Jolkinolide B Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can...
T12266L Ilginatinib maleate Ilginatinib maleate is a highly active and orally bioavailable inhibitor of JAK2.
T5382 Ritlecitinib PF-06651600 is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
T6309 AZ960 AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
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 signi...
T6156 Ruxolitinib (S enantiomer) Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
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 in ...
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 mi...
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...
T2S1975 Ponicidin Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infectio...
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 ...
T2485 Baricitinib Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activiti...
T6124 Mubritinib Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
T15037 Momelotinib Mesylate Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
T3042 NSC 42834 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.
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 th...
T3065 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
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...
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 ...
TQ0196 Cucurbitacin I Cucurbitacin I, a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
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 ...
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 NC...
T6020 Pacritinib Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
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 pathwa...
T12091 MM-589 MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
T12266 Ilginatinib Ilginatinib is a highly active and orally bioavailable inhibitor of JAK2.
T35341 NVP-BSK805 dihydrochloride
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.
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 ...
TN2002 Obovatol Obovatol has antioxidant, neuroprotective, antiinflammatory, antithrombotic and antitumour effects, it is a potent NF-κB inhibitors for Alzheimer's disease treat...
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...
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...
T9826 GDC-0214 GDC-0214 is an inhaled small-molecule JAK1 inhibitor and reduces fractional exhaled nitric oxide (Feno).
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 ...
T9251 Fedratinib hydrochloride hydrate Fedratinib hydrochloride hydrate is a potent, selective, ATP-competitive and orally active JAK2 inhibitor.
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 ...
T4210 SAR-20347 SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
T3398 Icaritin Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apopto...
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).
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 S...
T8719 SC99 SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation...
T11710 JAK-IN-5 JAK-IN-5 is an inhibitor of JAK.
Brepocitinib
TQ0010
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).
Fedratinib
T1995
Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
Abrocitinib
TQ0037
Abrocitinib (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).
Gusacitinib
T14331
Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
WDR5-0103
T3201
WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
Oclacitinib maleate
T6914
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, which...
Momelotinib sulfate
T15038
Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
GLPG0634 analog
T3076
GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
Jolkinolide B
T2S1040
Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can...
Ilginatinib maleate
T12266L
Ilginatinib maleate is a highly active and orally bioavailable inhibitor of JAK2.
Ritlecitinib
T5382
PF-06651600 is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
AZ960
T6309
AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
Pyridone 6
T3080
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 signi...
Ruxolitinib (S enantiomer)
T6156
Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
BD750
T8546
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 i...
WHI-P97 HCl 211555-05-4(free base)
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 m...
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...
Ponicidin
T2S1975
Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infectio...
Upadacitinib
T7503
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 ...
Baricitinib
T2485
Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activiti...
Mubritinib
T6124
Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
Momelotinib Mesylate
T15037
Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
NSC 42834
T3042
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.
Jaspamycin
T11711
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 t...
TG101209
T3065
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
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...
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 ...
Cucurbitacin I
TQ0196
Cucurbitacin I, a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
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...
JAK1-IN-4
T15606
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 ...
Pacritinib
T6020
Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
Broussonin E
TN3541
Broussonin E could suppress inflammation by modulating macrophages activation state via inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathwa...
MM-589
T12091
MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
Ilginatinib
T12266
Ilginatinib is a highly active and orally bioavailable inhibitor of JAK2.
NVP-BSK805 dihydrochloride
T35341
JBJ-02-112-05
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.
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 bind...
Obovatol
TN2002
Obovatol has antioxidant, neuroprotective, antiinflammatory, antithrombotic and antitumour effects, it is a potent NF-κB inhibitors for Alzheimer's disease trea...
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...
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 l...
GDC-0214
T9826
GDC-0214 is an inhaled small-molecule JAK1 inhibitor and reduces fractional exhaled nitric oxide (Feno).
TAK-659 hydrochloride
T4209
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 ...
Fedratinib hydrochloride hydrate
T9251
Fedratinib hydrochloride hydrate is a potent, selective, ATP-competitive and orally active JAK2 inhibitor.
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 ...
SAR-20347
T4210
SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
Icaritin
T3398
Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apopto...
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).
Cerdulatinib hydrochloride
T6104
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 S...
SC99
T8719
SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregatio...
JAK-IN-5
T11710
JAK-IN-5 is an inhibitor of JAK.
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