SU9516 是一种有效的 CDK2 抑制剂，IC₅₀ 值为 22 nM，同时对 CDK1 和 CDK4 也有抑制作用，IC₅₀ 值分别为 40 和 200 nM。

SU9516 is a potent CDK2 inhibitor, with an IC 50 of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC 50 s of 40, 200 nM, respectively.

Solid

CDK2 22 nM (IC50) CDK1 40 nM (IC50

SU9516 shows slight activities against PKC, p38, PDGFr and EGFR, with IC50 of >10, >10, 18, and >100 μM. SU9516 (5 μM) decreases cdk2-specific Phosphorylation of pRB and inhibits cell cycle progression in RKO cells. SU9516 (5 μM) also induces apoptosis in RKO and SW480 Cells. SU9516 (5 μM) results in enhanced pRb/E2F complex formation in HT-29 cells. SU9516 enhances presence of E2F species in multiprotein complexes. SU9516 (5 μM) rapidly induces cytochrome crelease, Bax mitochondrial translocation, and apoptosis in association with pronounced down-regulation of the antiapoptotic protein Mcl-1. SU9516 causes down-regulation of Mcl-1 mRNA levels in human leukemia cells. Furthermore, SU9516 treatment results in a marked increase in reactive oxygen species production. has not independently confirmed the

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Lane ME, et al. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 2001 Aug 15;61(16):6170-7.
[2]. Yu B, et al. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochem Pharmacol. 2002 Oct 1;64(7):1091-100.

In Vitro: DMSO : ≥ 100 mg/mL (414.51 mM)配制储备液