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JAK

JAK

货号 产品名 CAS号 信息
CSN26377 WHI-P258 21561-09-1 WHI-P258 is a quinazoline compound that binds to the active site of JAK3 with an estimated Ki of 72 µM, but does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM[1][2].
CSN12405 Fedratinib 936091-26-8 TG 101348 is an inhibitor of JAK2 with an IC₅₀ of 6 nM and also inhibits related kinases FLT3, RET, and JAK3 with less potent activity, having IC₅₀ values of 25, 17 and 169 nM, respectively.
CSN23146 TCJL37 1258294-34-6 TCJL-37 is a potent TYK2 inhibitor.
CSN20642 SD-1029 118372-34-2 SD1029 is a cell-permeable xanthenedione compound that acts as a JAK2-selective inhibitor.
CSN27609 SC99 882290-02-0 SC99 is a selective inhibitor of JAK2-STAT3 activation.
CSN24499 SAR-20347 1450881-55-6 SAR-20347 is a TYK2 and JAK inhibitor with IC50 values of 0.6, 23, 26 and 41nM for TYK2, JAK1, JAK2 and JAK3, respectively.
CSN23211 ZM 449829 4452-06-6 Potent, selective JAK3 inhibitor
CSN19685 ((3R,4R)-4-Methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)(pyrrolidin-1-yl)methanone 1262832-74-5 PF-956980 is a FGF1 receptor antagonist, a PDGF receptor modulator, an Flt3 tyrosine kinase modulator, and a VEGF antagonist used as immunosuppressive agent.
CSN26122 Ropsacitinib (PF-06826647) 2127109-84-4 PF-06826647 is a selective TYK2 inhibitor It is being tested in moderate-to-severe psoriasis in a Phase II clinical trial.
CSN23226 Brepocitinib P-Tosylate 2140301-96-6 PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. PF-06700841 P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively[1].
CSN26398 Ritlecitinib 1792180-81-4 PF-06651600 is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM.
CSN19687 PF-06263276 1421502-62-6 PF-06263276 is a potent and selective pan-JAK inhibitor which is suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
CSN22134 Oclacitinib 1208319-26-9 Oclacitinib 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.
CSN23010 NSC 33994 82058-16-0 NSC 33994 is a selective inhibitor of JAK2 with IC50 of 60 nM.
CSN23158 TCS 21311 1260181-14-3 NIBR3049, also known as TCS-21311, is a potent and selective JAK3 inhibitor IC50 values of 8 nM..
CSN23767 JAK3-IN-6 1443235-95-7 JAK3-IN-6 is an irreversible, potent and highly selective JAK3 inhibitor with IC50 value of 0.15 nM, 4300-fold selective for JAK3 over JAK1 in enzyme assays.
CSN24175 JAK/HDAC-IN-1 2284621-75-4 JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor with improved antiproliferative and proapoptotic activities over SAHA and ruxolitinib in several hematological cell lines.
CSN22435 JAK-IN-1 1334673-53-8 JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
CSN20267 JAK Inhibitor C35 1400687-19-5 JAK inhibitor C6 is a potent dual JAK1/3 inhibitor providing exceptional biochemical potency against JAK1 and JAK3 while maintaining good selectivity against JAK2 and Tyk2.
CSN22434 JAK-IN-5 2096999-92-5 JAK inhibitor 1 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
CSN33128 Izencitinib 2051918-33-1 Izencitinib is an orally active, non-selective and gut-restricted JAK inhibitor.
CSN22145 Itacitinib adipate 1334302-63-4 Itacitinib adipate is a selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
CSN26688 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide 1258292-64-6 GDC046 was an effective and selective oral biouse inhibitor of TYK2, with Ki values of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM against TYK2, JAK1, JAK2 and JAK3, respectively.
CSN23319 FM-381 2226521-65-7 FM381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper position +7 in JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
CSN26689 FM-479 2226521-64-6 FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases[1]. FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
CSN27527 Fedratinib hydrochloride hydrate 1374744-69-0 Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
CSN32905 Deuruxolitinib 1513883-39-0 Deuruxolitinib is a JAK1/2 inhibitor.
CSN21229 Delgocitinib 1263774-59-9 Delgocitinib is a novel and specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
CSN19758 Debio 0617B 1332329-27-7 Debio 0617B is a mutiple kinase inhitor and can inhibit the growth of STAT3-Driven solid tumors through combined inhibition of JAK, SRC, and class III/V receptor tyrosine kinases..
CSN19970 Curculigoside 85643-19-2 Curculigoside, a natural product isolated and purified from the rhizomes of Curculigo orchioides Gaertn., can prevent bone loss, improve osteogenesis and inhibit osteoclastogenesis of hAFSCs, suggesting its potential use to regulate hAFSC osteogenic differentiation for treating bone disorders.Curculigoside can also promote calcium deposition and increase the levels of ALP and Runx2 in osteoblasts under oxidative stress via anti-oxidative character, and possesses potent antioxidant properties against oxidative stress insults.
CSN16269 CTX-0294885 1439934-41-4 CTX-0294885 is a bisanilino pyrimidine and exhibits inhibitory activity against a broad range of kinases in vitro, further developed into a Sepharose-supported kinase capture reagent. CTX-0294885 is a broad spectrum kinase inhibitor that inhibited FAK, FLT3, JAK2, JAK3, Src, Aurora kinase A, and VEGF receptor 3 (IC50s = 4, 1, 3, 28, 2, 18, and 3 nM, respectively) in an initial screen.
CSN25619 Deucravacitinib 1609392-27-9 BMS-986165 is a highly selective and allosteric TYK2 inhibitor. It is a high affinity JH2 ligand with Ki values of 0.02 nM and 1nM for binding to Tyk2 pseudokinase domain and JAK1 pseudokinase (JH2) domain, respectively. It blocked receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.
CSN20396 JAK1-IN-4 2091134-35-7 AZD4205 is a potent ATP-competitive inhibitor that inhibits JAK1 with a Ki of 2.8 nM and exhibits excellent selectivity compared with other JAK family kinases and across the kinome.
CSN22196 Golidocitinib 2091134-68-6 AZD-4205 is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively).
CSN22692 Atiprimod 2HCl 130065-61-1 Atiprimod 2HCl is an inhibitor JAK2 with IC50 of 397 nM.
CSN13724 AG490 133550-30-8 AG-490 is a broad-spectrum inhibitor that has several targets including EGFR (IC50 = 2 μM), ErbB2 (IC50 = 13.5 μM), STAT3 and JAK2.
CSN24191 Abrocitinib 1622902-68-4 Abrocitinib is a potent and selective JAK1 inhibitor with IC50s of 29 and 803nM for JAK1 and JAK2, respectively.
CSN27798 G5-7 939681-36-4
CSN27819 RO495 1258296-60-4
CSN32457 Ivarmacitinib 1445987-21-2
CSN32470 Gusacitinib 1425381-60-7
CSN43357 Tyk2-IN-3 1779493-12-7
CSN42980 JAK-IN-11 916742-11-5
CSN51409 BMS-986202 1771691-34-9
CSN67834 Ilunocitinib 1187594-14-4
CSN79368 JAK-IN-18 2247925-32-0
CSN104034 7-(3,5-Difluoro-4-(morpholinomethyl)phenyl)-N-(6-((3S,5R)-3,5-dimethylpiperazin-1-yl)pyridin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine 1180158-99-9
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