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SU9516

CAS No. : 377090-84-1

產(chǎn)品活性：SU9516 is a potent CDK2 inhibitor, with an IC₅₀ of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC₅₀s of 40, 200 nM, respectively.

研究領(lǐng)域：Cell Cycle/DNA Damage  |  Autophagy  |  Apoptosis

作用靶點：CDK  |  Autophagy  |  Apoptosis

In Vitro: 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.

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