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SNS-032 is a potent inhibitor of cyclin-dependent kinases (CDKs)9, 2 and 7 (IC50 values are 4, 38 and 62 nM respectively).
Stattic, a nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1.
TAK-285 is a dual HER2 and EGFR (HER1) inhibitor with IC50 of 17 nM and 23 nM, > 10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.
TP-3654 is a selective Pim kinase inhibitor with Ki values of 5nM, 239nM and 42nM for Pim-1, Pim-2 and Pim-3, respectively, as well as with an average EC50 of 67nM for cellular PIM-1 inhibition in the PIM-1/BAD overexpression system and with moderate potency to FLT3.
UNC0224 is a selective inhibitor of G9a with IC50 of 15 nM.
UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively.
(+)-JQ-1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family.
ACY-1215 is a selective HDAC6 inhibitor with IC50 of 5 nM, being > 10-fold selective for HDAC6 than HDAC1/2/3 (IC50 = 58, 48, and 51 nM) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2.
ARRY-162 is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay.
Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
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