Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1.
More Information Supplier PageCUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
More Information Supplier PageOrteronel(TAK-700) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3.
More Information Supplier PageDanoprevir is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2.
More Information Supplier PageDanoprevir is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2.
More Information Supplier PageRitonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
More Information Supplier PageRitonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
More Information Supplier PageBIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase are observed at concentrations vastly exceeding the IC50 for telomerase. BIBR 1532 induces apoptosis in cancer cells.
More Information Supplier PageBIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase are observed at concentrations vastly exceeding the IC50 for telomerase. BIBR 1532 induces apoptosis in cancer cells.
More Information Supplier PagePD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.
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