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JAK

JAK

货号 产品名 CAS号 信息
CSN12244 ZM39923 HCl 1021868-92-7 ZM39923 HCl is a potent and selective JAK3 inhibitor with pIC50 value of 7.1, as well as inhibits EGFR, JAK1 and CDK4 with pIC50 values of 5.6, 4.4, and < 5.0.
CSN13641 XL019 945755-56-6 XL019 is a selective and potent JAK2 inhibitor with IC50 value of 2.2 nM, with less potency to JAK1, JAK3, FLT3 and PDGFRβ with IC50 values of 134.3 nM, 214.2 nM, 139.7 nM and 125.4 nM, respectively.
CSN13436 (S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide 857064-38-1 WP1066 is a dual inhibitor for both JAK2 and STAT3 with IC50 value of 2.30 μM and 2.43 μM, respectively.
CSN18107 WHI-P97 211555-05-4 WHI-P97 is a rationally designed potent inhibitor of JAK-3.
CSN16224 WHI-P154 211555-04-3 WHI-P154 is a specific inhibitor of JAK3 with IC50 value of 1.8 μM, almost shows no activity against JAK1 or JAK2.
CSN18721 Upadacitinib 1310726-60-3 Upadacitinib is a selective JAK1 inhibitor with an IC50 of 43 nM.
CSN16364 3-((3R,4R)-4-Methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile   477600-75-2 Tofacitinib is a FDA-approved JAK inhbitor used to treat moderate to severe rheumatoid arthritis, with IC50 values of 1 nM, 20 nM and 112 nM for JAK3, JAK2 and JAK1, respectively.
CSN12901 3-((3R,4R)-4-Methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile 2-hydroxypropane-1,2,3-tricarboxylate 540737-29-9 Tofacitinib Citrate is a FDA-approved JAK inhbitor used to treat moderate to severe rheumatoid arthritis, with IC50 values of 1 nM, 20 nM and 112 nM for JAK3, JAK2 and JAK1, respectively.
CSN12694 TG101209 936091-14-4 TG 101209 is a potent and selective JAK2 inhibitor with IC50 of 6 nM, also inhibits Flt3 and RET with IC50 values of 25 nM and 17 nM, respectively.
CSN15697 Solcitinib 1206163-45-2 Solcitinib is a highly selective JAK1 inhibitor with IC50 value of 9.8 nM, with much less potency against JAK1 and JAK2 with IC50 values >100nM.
CSN18612 Ruxolitinib (S enantiomer) 941685-37-6 S-Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, > 130-fold selectivity for JAK1/2 versus JAK3.
CSN17456 Ruxolitinib sulfate 1092939-16-6 Ruxolitinib sulfate is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, > 130-fold selectivity for JAK1/2 versus JAK3.
CSN13499 (R)-3-(4-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate 1092939-17-7 Ruxolitinib phosphate is a potent and selective JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, > 130-fold selectivity for JAK1/2 versus JAK3.
CSN12394 (R)-3-(4-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile   941678-49-5 Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, > 130-fold selectivity for JAK1/2 versus JAK3.
CSN16800 Pyridone 6 457081-03-7 Pyridone 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 significantly weaker affinities(130 nM to 10 mM) for other protein tyrosine kinases.
CSN16871 Peficitinib 944118-01-8 Peficitinb is an oral Janus kinase (JAK) inhibitor. Peficitinib inhibits JAK1, JAK2, JAK3 and Tyk2 enzyme activities with IC50s of 3.9, 5.0, 0.71 and 4.8 nM, respectively, and has moderate selectivity for JAK3 inhibition.
CSN13490 Pacritinib 937272-79-2 Pacritinib is a macrocyclic multiple inhibitor of JAK2 (V617F), JAK2, FLT3 (D835Y) and FLT3 with IC50 values of 19 nM, 23 nM, 6 nM and 22 nM, respectively.
CSN19239 trans-N-methyl-1-(4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide maleate 1640292-55-2 Oclacitinib Fumarate is a potent JAK inhibitor with IC50 value ranging in 10-99 nM for JAK family members, most potent against JAK1 with IC50 value of 10 nM.
CSN17137 NVP-BSK805 1092499-93-8 NVP-BSK805 is a selective JAK2 and JAK2(V617F) mutant inhibitor with IC50 value of 0.48 nM, with >20-fold selectivity over TYK2, JAK3 and JAK1 (IC50 values of 10.8, 18.7 and 31.6 nM, respectively).
CSN18966 NVP-BSK805 2HCl 1942919-79-0 NVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM and > 20-fold selectivity towards JAK1, JAK3 and TYK2.
CSN16932 NSC 42834 195371-52-9 NSC 42834, a specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
CSN18967 Ilginatinib maleate 1354799-87-3 NS-018 maleate is an ATP-competitive small-molecule inhibitor of JAK2 with IC50 of 470?nM in Ba/F3-JAK2V617F cells .
CSN17611 Ilginatinib 1239358-86-1 NS-018 is a highly selective JAK2 inhibitor.
CSN17610 Ilginatinib HCl 1239358-85-0 NS-018 HCl is a highly selective JAK2 inhibitor.
CSN13502 Gandotinib 1229236-86-5 LY2784544 is a potent, selective and ATP-competitive inhibitor of JAK2 with IC50 value of 3 nM for both JAK2 and JAK2V617F, as well as inhibits FLT3 with IC50 value of 4 nM, less potent to JAK1 and JAK3 with IC50 values of 19.8 nM and 48 nM, respectively, with additional minor inhibition of STAT3.
CSN11286 Lestaurtinib 111358-88-4 Lestaurtinib is a tyrosine kinase inhibitor structurally related to staurosporine. This semisynthetic derivative of the indolocarbazole K252a was investigated by Cephalon as a treatment for various types of cancer.
CSN16118 JANEX-1 202475-60-3 JANEX-1 is a cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (IC50 = 78 μM) and has no effect on JAK1, JAK2, or Zap/Syk or SRC tyrosine kinases.
CSN18043 JAK3-IN-1 1805787-93-2 JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM).
CSN17204 Itacitinib 1334298-90-6 Itacitinib is an oral selective JAK1 tyrosine kinase inhibitor, which is potential for the treatment of rheumatoid arthritis, myelofibrosis, rheumatoid arthritis and plaque psoriasis.
CSN13689 GLPG0634 analog 1206101-20-3 GLPG0634 analog is a pan JAK inhibitor with IC50s of 50-200 nM for JAK1/JAK2/JAK3.
CSN18801 FLLL32 1226895-15-3 FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of < 5 μM.
CSN15694 N-(5-(4-((1,1-Dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide 1206161-97-8 Filgotinib is a selective JAK1/2 inhibitor with IC50 values of 10/28nM, with less potency against JAK3 and TYK2 with IC50 values of 810 nM and 116 nM, respectively.
CSN13843 Decernotinib 944842-54-0 Decernotinib is a selective JAK3 inhibitor with Ki value of 2.5nM, with >4-fold selectivity over JAK1, JAK2, and TYK2 with Ki values of 11nM, 13nM and 13nM, respectively.
CSN17436 Momelotinib sulfate 1056636-06-6 CYT387 sulfate is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.
CSN17437 Momelotinib Mesylate 1056636-07-7 CYT387 mesylate is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.
CSN13153 Momelotinib 1056634-68-4 CYT387 is a selective and potent ATP-competitive JAK1/2 inhibitor with IC50 values of 11nM and 18nM, respectively, with less potency against JAK3 with IC50 value of 155 nM.
CSN13905 Cerdulatinib 1198300-79-6 Cerdulatinib is a multiple tyrosine kinase inhibitor with IC50 values of 12 nM/6 nM/8 nM and 0.5 nM, for JAK1/JAK2/JAK3 and TYK2, also shows potency against MST1, ARK5, MLK1, Fms. Syk, etc. with IC50 values ranging in 4-51 nM.
CSN19204 Cerdulatinib HCl 1369761-01-2 Cerdulatinib HCl is a dual JAK/SYK inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. It also inhibits other kinases with IC50 less than 200 nM.
CSN15836 CEP-33779 1257704-57-6 CEP-33779 is a highly selective JAK2 inhibitor with IC50 value of 1.8 nM, with much less potency against JAK1 and TYK2 with >40- and >800-fold IC50 values.
CSN16254 BMS-911543 1271022-90-2 BMS-911543 is a selective ATP-competitive JAK2 inhibitor with IC50 value of 1.1 nM, with much less potency against JAK1, JAK3 and TYK2 with IC50 values of 360nM, 75 nM and 66nM.
CSN17535 Baricitinib phosphate 1187595-84-1 Baricitinib Phosphate can selectively inhibit JAK1/2 inhibitor with IC50 values of 5.9 nM and 5.7 nM.
CSN13692 2-(3-(4-(3H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile 1187594-09-7 Baricitinib can selectively inhibit JAK1/2 inhibitor with IC50 values of 5.9 nM and 5.7 nM.
CSN13663 AZD-1480 935666-88-9 AZD1480 is a selective ATP-competitive JAK1/2 inhibitor with IC50 value of 1.3 and <0.4 nM, respectively, as well as shows inhibitory effect on JAK3 and Tyk2.
CSN17120 AZ960 905586-69-8 AZ 960 is a potent ATP-competitive JAK inhibitor with IC50 values of <3 nM and 9nM for JAK2 and JAK3, respectively.
CSN17038 (3S,4S)-Tofacitinib 1092578-47-6 (3S,4S)-Tofacitinib is an isomer of tofacitinib, an inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
CSN17455 (3S,4R)-Tofacitinib 1092578-48-7 (3S,4R)-Tofacitinib is an isomer of tofacitinib, which is an inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
CSN17037 (3R,4S)-Tofacitinib 1092578-46-5 (3R,4S)-Tofacitinib is an isomer of tofacitinib, an inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
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