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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. |