JAK
Janus kinases (JAKs), belonging to a distinct family of tyrosine kinases, are non-receptor tyrosine kinases that transduce signals of cytokine receptors via diverse signal transduction pathways. Mammalian JAK family consists of four structurally similar members, JAK1, JAK2, JAK3 and Tyrosine kinase 2 (TYK2), which are characterized by containing seven JAK homology (JH) domains. The presence of JH1 and JH2 domains is the most intriguing feature of JAK proteins. JH1 domain is the main catalytic domain; while JH2 is usually considered as a catalytically inactive pseudokinase domain. However, results of recent studies have shown that JH2 acts as a dual-specificity protein kinase to phosphorylate two regulatory sites (Ser523 and Tyr570) in JAK2.
Products for JAK
- Cat.No. Product Name Information
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GC72769
(1R)-AZD-1480
(1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP competitive JAK1 and JAK2 inhibitor.
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GC34971
(3R,4S)-Tofacitinib
(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib.
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GC34972
(3S,4R)-Tofacitinib
(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib.
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GC34973
(3S,4S)-Tofacitinib
(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib.
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GC63864
(E/Z)-Zotiraciclib hydrochloride
(E/Z)-TG02 hydrochloride; (E/Z)-SB1317 hydrochloride
(E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor. -
GC32023
Abrocitinib (PF-04965842)
PF-04965842
Abrocitinib (PF-04965842) (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. -
GC32028
BMS-066
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.
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GC25168
Brepocitinib (PF-06700841)
PF-841
Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3. -
GC35554
Brevilin A
6-O-Angeloylprenolin, Brevelin A
A sesquiterpene lactone with anticancer activity -
GC68819
Butyzamide
Butyzamide is an orally effective Mpl activator, where Mpl is a receptor for thrombopoietin (TPO) involved in platelet production. Butyzamide increases the phosphorylation levels of JAK2, STAT3, STAT5 and MAPK. In mouse xenograft experiments, Butyzamide increases human platelet levels.
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GC11209
Cerdulatinib (PRT062070)
PRT062070, PRT2070
Cerdulatinib (PRT062070) (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively. -
GC11652
CHZ868
Type II JAK2 inhibitor
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GC31660
Delgocitinib (JTE-052)
Delgocitinib (JTE-052) (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
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GC71575
Deuruxolitinib
Deuruxolitinib, a deuterated Ruxolitinib , modulates the activity of JAK1/JAK2.
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GC16875
FLLL32
JAK2 Inhibitor X
STAT3 inhibitor -
GC19408
FM381
FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor
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GC70307
Fosifidancitinib
Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3.
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GC68378
GDC-4379
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GC12579
GLPG0634
GLPG0634
GLPG0634 (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. -
GC17222
GLPG0634 analogue
GLPG0634 analogue (Compoun 176) is a broad spectrum JAK inhibitor with IC50 values of <100 nM against JAK1, JAK2 and JAK3.
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GC69190
GS-829845
GS-829845 is the main active metabolite of Filgotinib. It is a JAK1 inhibitor, but its potency is about 10 times lower than that of the parent compound and it has a longer half-life.
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GC33041
Gusacitinib (ASN-002)
ASN-002
Gusacitinib (ASN-002) (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib (ASN-002) has anti-cancer activity in both solid and hematological tumor types. -
GC73627
HDAC/JAK/BRD4-IN-1
HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor.
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GC64108
Ifidancitinib
ATI-50002; ATI-502
Ifidancitinib (ATI-50002) is a potent and selective inhibitor of JAK kinases 1/3. -
GC32809
Ilginatinib (NS-018)
NS-018
Ilginatinib (NS-018) (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). -
GC33037
Ilginatinib hydrochloride (NS-018 hydrochloride)
NS-018 hydrochloride
Ilginatinib hydrochloride (NS-018 hydrochloride) (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). -
GC33018
Ilginatinib maleate (NS-018 (maleate))
NS-018 maleate
Ilginatinib maleate (NS-018 (maleate)) (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). -
GC19204
Itacitinib
INCB 039110
Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis. -
GC36351
Itacitinib adipate
INCB039110 adipate
Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis. -
GC72815
Itacnosertib (hydrocholide)
TP-0184 (hydrocholide
Itacnosertib drocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5. -
GC70213
JAK 3i
JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM).
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GC31866
JAK inhibitor 1
JAK inhibitor 1 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
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GC31999
JAK-IN-1
JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively.
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GC36366
JAK-IN-10
JAK-IN-10 is a JAK inhibitor.
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GC73148
JAK-IN-21
JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively.
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GC68000
JAK-IN-23
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GC71213
JAK-IN-24
JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively.
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GC69306
JAK-IN-25
JAK-IN-25 (compound 19) is an effective JAK inhibitor with IC50 values of 6 nM, 21 nM, 8 nM, and 1051 nM for TYK2, JAK1, JAK2, and JAK3 respectively. It inhibits human whole blood IL-12 (HEB IL-12) with an IC50 value of 28 nM. JAK-IN-25 has potential for use in cancer research.
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GC73475
JAK-IN-26
JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics.
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GC65453
JAK-IN-3
JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
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GC64959
JAK/HDAC-IN-1
JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively.
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GC73456
JAK1-IN-11
JAK1-IN-11 (compound 11) is a potent inhibitor of JAK,with IC50s of 0.02 nM (JAK1),and 0.44 nM (JAK2),respectively.
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GC71475
JAK1-IN-13
JAK1-IN-13 (compound 36b) is an orally active, potent and highly selective inhibitor of JAK1 with an IC50 of 0.044 nM.
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GC33036
JAK1-IN-3
Golidocitinib; AZD4205
JAK1-IN-3 (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM). -
GC33258
JAK1-IN-4
JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).
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GC36363
JAK1-IN-7
JAK1-IN-7
JAK1-IN-7 (JAK1-IN-7) is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect. -
GC36364
JAK2-IN-4
JAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.
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GC65405
JAK2-IN-6
JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.
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GC69305
JAK2/FLT3-IN-1
JAK2/FLT3-IN-1 is an orally effective dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3 respectively. It has anti-cancer activity.
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GC36365
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.
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GC33046
JAK3-IN-1
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
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GC73600
JAK3-IN-14
JAK3-IN-14 (compound 1) is a potent JAK3 inhibitor, with IC50 values of 38 and 600 nM for JAK3 and JAK2, respectively.
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GC31902
JAK3-IN-6
JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
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GC33382
JAK3-IN-7
JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM.
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GC71392
Lepzacitinib
Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3.
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GC14857
LFM-A13
BTK-specific tyrosine kinase inhibitor
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GC64372
Lorpucitinib
JNJ-64251330
Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease. -
GC36646
Momelotinib Mesylate
CYT387 Mesylate
Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. -
GC66329
NDI-034858
NDI-034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM.
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GC71049
Nimucitinib
Nimucitinib is a Janus kinase (JAK) inhibitor.
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GC36783
NVP-BSK805 dihydrochloride
A potent, selective JAK2 inhibitor
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GC31677
Oclacitinib maleate (PF-03394197 maleate)
Oclacitinib maleate (PF-03394197 maleate) (PF-03394197 maleate) is a novel JAK inhibitor.
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GC41329
Pacritinib
FMS-like tyrosine kinase 3 (FLT3) and Janus kinase 2 (JAK2) are tyrosine kinases that mediate cytokine signaling and are frequently mutated in cancers, particularly acute myeloid leukemia.
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GC10341
Peficitinb (ASP015K, JNJ-54781532)
ASP015K, JNJ-54781532
Peficitinb (ASP015K, JNJ-54781532) (ASP015K) is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. -
GC14938
PF-03394197(Oclacitinib)
PF-03394197
Novel Janus kinase inhibitor -
GC36882
PF-06263276
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively.
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GC19288
PF-06651600
PF-06651600
PF-06651600 (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM. -
GC19405
PF-06700841 P-Tosylate
PF-06700841 P-Tosylate
Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. -
GC64701
Povorcitinib
INCB54707
Povorcitinib is a potent and selective inhibitor of JAK1. -
GC64700
Povorcitinib phosphate
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GC30601
Propanamide
Propanamide is a potent and selective JAK inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment.
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GC71201
PROTAC TYK2 degradation agent1
PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader.
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GC34742
Protosappanin A
Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3.
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GC69780
Pumecitinib
Pumecitinib is a JAK inhibitor with anti-inflammatory activity.
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GC37522
RGB-286638
A multi-kinase inhibitor
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GC37523
RGB-286638 free base
A multi-kinase inhibitor
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GC70211
Ritlecitinib tosylate
Ritlecitinib tosylate is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM.
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GC25869
RO495
CS-2667
RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). -
GC37575
Ruxolitinib sulfate
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
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GC19320
SAR-20347
SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
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GC73139
SJ1008030 formic
SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2.
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GC73369
SJ988497
SJ988497 is a PROTAC JAK2 degrader.
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GC19334
Solcitinib
GLPG0778, GSK2586184
Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis. -
GC25992
TG-89
TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.
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GC31668
TYK2-IN-2
TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively.
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GC32052
Tyk2-IN-3
Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM.
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GC31659
Tyk2-IN-4 (BMS-986165)
BMS-986165
Tyk2-IN-4 (BMS-986165) (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. -
GC65387
Tyk2-IN-5
Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα.
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GC37846
Tyk2-IN-7
Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.
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GC37847
Tyk2-IN-8
Tyk2-IN-8 (Compound 3) is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2.
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GC19368
Upadacitinib
ABT-494
Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders. -
GC67867
VVD-118313
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GC40761
VX-509
VX-509 is a selective inhibitor of Janus kinase 3 (JAK3) with a Ki value of 2.5 nM in enzyme assays and an IC50 value of 50-170 nM in cellular assays dependent on JAK3 activity with no measurable activity against other JAK isotypes.
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GC37971
ZM39923
ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.