GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).
Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a tubulin-binding microtubule polymerization inhibitor that targets the colchicine-binding site. By inducing tubulin depolymerization, Combretastatin A-1 phosphate tetrasodium inhibits the Wnt β-catenin pathway and leads to the deactivation of AKT. It possesses both anti-tumor and anti-vascular properties.
Combretol has leishmanicidal activity, it showed moderate activity (growth inhibition 87.3 and 73.0 %, respectively, at 50 μM) against a multidrug-resistant L. tropica line. Combretol also shows weakly active cytotoxic activity.
MC-Val-Cit-PAB-Retapamulin is a drug-linker conjugate for antibody-drug conjugates (ADC) that exhibits potent antitumor activity. This compound utilizes Retapamulin, a ribosome inhibitor, connected through the ADC linker MC-Val-Cit-PAB.
Potent inhibitor of CDK16 and CDK14 (IC50 values are 6 and 140 nM, respectively in kinase activity assay; IC50 = 563 nM for CDK14 in BRET assay). Also binds CDK2 (IC50 = 493 nM). Inhibition reversible upon compound wash-out. Control for FMF-04-159-2 (Cat. No. 7158).