Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.
More Information Supplier PageSGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively.
More Information Supplier PageCNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of
More Information Supplier PageSKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.
More Information Supplier PageBeta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.
More Information Supplier PageBeta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.
More Information Supplier PageMM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic inhibitor of the WDR5/MLL1 protein-protein interaction, which bind to WDR5 with Ki < 1 nM and IC50 =2.4nM.
More Information Supplier PageIOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 is an inhibitor of ALKBH5.
More Information Supplier PageBromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.
More Information Supplier PageRGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
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