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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.
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.
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.
Baricitinib can selectively inhibit JAK1/2 inhibitor with IC50 values of 5.9 nM and 5.7 nM.
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.
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.
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.
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Tags: JAK1 | JAK | JAK1 相关产品 | JAK1 基因表达
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