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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GC62130
(2R,5S)-Ritlecitinib
(2R,5S)-PF-06651600
(2R,5S)-Ritlecitinib ((2R,5S)-PF-06651600) is a potent and selective JAK3 inhibitor (IC50=144.8 nM) extracted from patent US20150158864A1, example 68. -
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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GC61807
(E/Z)-AG490
(E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
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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. -
GC17055
1,2,3,4,5,6-Hexabromocyclohexane
Potently and directly inhibits JAK2 tyrosine kinase autophosphorylation, specifically inhibiting ligand-dependent JAK2 activation.
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GC62233
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
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GC46503
2-(1,8-Naphthyridin-2-yl)phenol
2-NP
2-(1,8-Naphthyridin-2-yl)phenol is a selective enhancer of STAT1 transcription. 2-(1,8-Naphthyridin-2-yl)phenol can enhance the ability of IFN-γ to inhibit the proliferation of human breast cancer and fibrosarcoma cells. -
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. -
GC50003
AG 490
EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor
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GC10638
AT9283
A broad spectrum kinase inhibitor
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GC50066
Atiprimod dihydrochloride
JAK2 inhibitor
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GN10627
Atractylenolide I
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GC13433
AZ 960
A JAK2 inhibitor
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GC12504
AZD1480
A potent JAK2 inhibitor
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GC11572
Bardoxolone methyl
Bardoxolone methyl, NSC 713200, RTA 402, TP155
A synthetic triterpenoid with potent anticancer and antidiabetic activity -
GC14844
Baricitinib (LY3009104, INCB028050)
INCB 028050, LY3009104
A JAK1 and JAK2 inhibitor -
GC13830
Baricitinib phosphate
A JAK1 and JAK2 inhibitor
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GC91506
Bayer 18
Bayer 18 is a tyrosine kinase 2 (TYK2) inhibitor (IC50 = 18.7 nM).
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GC32028
BMS-066
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.
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GC12454
BMS-911543
A potent, selective JAK2 inhibitor
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GC62491
BMS-986202
BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM.
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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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GC12083
CEP-33779
A potent, orally available inhibitor of JAK2
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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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GC62908
Coumermycin A1
Coumermycin A1 is a JAK2 signal activator.
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GN10442
Curculigoside
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GC17050
CYT387
Momelotinib
A potent inhibitor of JAK1 and JAK2 -
GC16468
CYT387 sulfate salt
A potent inhibitor of JAK1 and JAK2
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GC10770
Decernotinib(VX-509)
Decernotinib, VRT-831509
Decernotinib(VX-509) is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively. -
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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GC43406
Delphinidin (chloride)
Ephdine
Delphinidin (chloride) is an anthocyanidin, a natural plant pigment which serves as the precursor of certain anthocyanins that provide the blue-red colors of flowers, fruits, and red wine.
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GC71575
Deuruxolitinib
Deuruxolitinib, a deuterated Ruxolitinib , modulates the activity of JAK1/JAK2.
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GC46148
Filgotinib-d4
GLPG0634-d4
An internal standard for the quantification of filgotinib -
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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GC62246
G5-7
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
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GC68378
GDC-4379
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GN10584
Ginsenoside Rk1
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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. -
GC47450
IL-4 Inhibitor
IL-4 Inhibitor (compound 52) is an IL-4 inhibitor, with an EC50 of 1.81 μM.
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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). -
GC63309
Ilunocitinib
Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1).
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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. -
GC63416
Itacnosertib
TP-0184
Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871. -
GC72815
Itacnosertib (hydrocholide)
TP-0184 (hydrocholide
Itacnosertib drocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5. -
GC62313
Izencitinib
TD-1473; JNJ-8398
Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. -
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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GC91148
JAK Inhibitor 31
A JAK2 inhibitor
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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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GC63448
JAK-IN-14
JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM.
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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. -
GC63029
JAK1-IN-8
JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1.
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GC13826
JAK2 Inhibitor V, Z3
Z3; NSC 42834;1-Butanone, 2-methyl-1-phenyl-4-(2-pyridinyl)-2-[2-(2-pyridinyl)ethyl]-
A selective inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK -
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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GC62500
JAK2-IN-7
JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
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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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GC62665
JAK2/FLT3-IN-1 TFA
JAK2/FLT3-IN-1 (TFA) is a potent and orally active 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. JAK2/FLT3-IN-1 (TFA) 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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GC14671
JANEX-1
Janex 1
A selective JAK3 inhibitor -
GC91059
LCC-12 (formate)
A copper (II) chelator and derivative of metformin
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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. -
GC13848
LY2784544
Gandotinib
Potent inhibitor of JAK2 -
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. -
GC40791
MS-1020
MS-1020 is a cell-permeable inhibitor of janus kinase 3 (JAK3), strongly inhibiting constitutive autophosphorylation of JAK3 in L540 cells when used at 30-50 μM.
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GC66329
NDI-034858
NDI-034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM.