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BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc.
BP-1-102 is an orally available, small-molecule inhibitor of transcription factor STAT3.
CHIR-98014 (CT98014) is highly selective aminopyrimidine-derivatived inhibitor of GSK-3 with IC50 of 650nM and 580nM for GSK-3 and GSK-3(measured by kinase assays), respectively, and exhibits >1000-fold selectivity for GSK-3 over closely related kinases, such as cdc2.
CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively.
Chlorpromazine Hydrochloride is the hydrochloride salt form of chlorpromazine, a phenothiazine and traditional antipsychotic agent with anti-emetic activity.Chlorpromazine Hydrochloride exerts its antipsychotic effect by blocking postsynaptic dopamine receptors in cortical and limbic areas of the brain.
Crenolanib is a potent class III RTKs inhibitor with Kd values of 3.2nM, 2.1nM and 0.74nM for PDGFRα, PDGFRβ and FLT3.
Dabrafenib is a potent, selective and efficacious inhibitor of B-RafV600E with IC50 value of 0.7 nM, and less potent to B-Raf and C-Raf with IC50 values of 5.2 nM and 6.3 nM, respectively.
Desidustat, an antianaemic drug, is a HIF hydroxylase inhibitor.
EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity with Ki value of 2.5±0.5 nM.
Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Foretinib is less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and with little activity to FGFR1 and EGFR.
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