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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.
AT9283 is a multi-targeted inhibitor with IC50s of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl (T315I), JAK2 and JAK3, Aurora A and Aurora B, respectively.
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.
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.
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.
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.
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.
WHI-P154 is a specific inhibitor of JAK3 with IC50 value of 1.8 μM, almost shows no activity against JAK1 or JAK2.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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Tags: JAK3 | JAK | JAK3 相关产品 | JAK3 基因表达
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