SU9516, 10 mg

From STEMCELL Technologies, this selective small-molecule inhibitor targets the cyclin/CDK pathway by inhibiting cyclin-dependent kinases. It specifically inhibits CDK2, CDK1 and, to a lesser extent, CDK4, with reported IC₅₀ values of 22, 40, and 200 nM, respectively. The compound competitively binds in the ATP binding pocket of CDK2 and CDK1, and is highly selective, showing no inhibition of PKC, p38 MAPK, PDGFR or EGFR (IC₅₀ > 10 µM). It is supplied as a crystalline solid with a purity of ≥ 98%, a molecular weight of 241.3 g/mol and the chemical formula C₁₃H₁₁N₃O₂ (CAS 377090-84-1).

In published cancer research, the inhibitor has been shown to decrease proliferation in human colon carcinoma cell lines RKO and SW480 through inhibition of retinoblastoma protein (Rb) phosphorylation, leading to increased Rb/E2F complex formation, cell cycle arrest and subsequent apoptosis. It also induces mitochondrial injury, caspase activation and apoptosis through downregulated transcription of the antiapoptotic protein MCL-1 in U937, Jurkat and HL-60 leukaemia or lymphoma cell lines, and has been used to induce apoptosis, alone or in combination with paclitaxel, in the inflammatory breast cancer cell line SUM149PT.

For handling, the product is stable at -20 °C as supplied, should be protected from prolonged exposure to light, and remains stable for 12 months from the date of receipt. It is soluble in DMSO at ≤ 20 mM, has low solubility in aqueous media, and stock solutions in DMSO are recommended to be stored at -20 °C and aliquoted to avoid repeated freeze-thaw cycles. For cell culture use, the stock should be diluted into culture medium immediately before use, with the final DMSO concentration kept at or below 0.1% to avoid potential cell toxicity.