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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.
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.
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.
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.
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.
WP1066 is a dual inhibitor for both JAK2 and STAT3 with IC50 value of 2.30 μM and 2.43 μM, 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.
Baricitinib can selectively inhibit JAK1/2 inhibitor with IC50 values of 5.9 nM and 5.7 nM.
AZ 960 is a potent ATP-competitive JAK inhibitor with IC50 values of <3 nM and 9nM for JAK2 and JAK3, respectively.
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.
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.
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.
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Tags: JAK2 | JAK | JAK2 相关产品 | JAK2 基因表达
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