SU 9516
Discontinued Product
Chemical Name: (Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-indol-2-one
Purity: ≥99%
Biological Activity
SU 9516 is a cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 0.02 - 0.03, 0.04 - 0.2, 0.2 - 1.7 and 0.9 μM for cdk2, cdk1, cdk4 and cdk9, respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G1 and G2-M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells.
Lane et al.
Cancer Res., 2001;61:6170 -
SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells.
Yu et al.
Biochem.Pharmacol., 2002;64:1091 -
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
J.Med.Chem., 2018;61:9105 -
The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional m
Gao et al.
Mol.Pharmacol., 2006;70:645
Product Datasheets
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Citations for SU 9516
The citations listed below are publications that use Tocris products. Selected citations for SU 9516 include:
2 Citations: Showing 1 - 2
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The AHR represses nucleotide excision repair and apoptosis and contributes to UV-induced skin carcinogenesis.
Authors: Pollet Et al.
Cell Death Differ 2018;25:1823
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The FGF-1-specific single-chain antibody scFv1C9 effectively inhibits breast cancer tumour growth and metastasis.
Authors: Shi Et al.
J Cell Mol Med 2014;18:2061
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