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SU 9516

Basic information Safety Supplier Related

SU 9516 Basic information

Product Name:
SU 9516
Synonyms:
  • 3-(1H-Imidazol-4-ylmethylene)-5-methoxy-1,3-dihydro-indol-2-one
  • CS-1784
  • 3-(1H-imidazol-5-ylmethylidene)-5-methoxy-1H-indol-2-one
  • SU 9516;SU-9516
  • (Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-indol-2-one
  • (Z)-3-((1H-iMidazol-4-yl)Methylene)-5-Methoxyindolin-2-one
  • (Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-indol-2-one SU9516
  • (3Z)-1,3-Dihydro-3-(1H-imidazol-5-ylmethylene)-5-methoxy-2H-indol-2-one
CAS:
377090-84-1
MF:
C13H11N3O2
MW:
241.25
Product Categories:
  • Enzyme Inhibitors by Enzyme
  • Intracellular Signaling
  • A to
  • Cyclin Dependant Kinase 2Serine/Threonine Kinase Biology
  • Cyclin-Dependent Kinase (CDK)Cell Signaling and Neuroscience
  • Inhibitors
  • Kinase/Phosphatase Biology
  • Protein Kinase Inhibitors
  • Serine/Threonine Kinase Inhibitors
Mol File:
377090-84-1.mol
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SU 9516 Chemical Properties

storage temp. 
Store at +4°C
solubility 
DMSO: ~17 mg/mL
form 
crystalline
color 
brown
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Safety Information

Safety Statements 
22-24/25
WGK Germany 
3
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SU 9516 Usage And Synthesis

Uses

SU 9516 is a 3-substituted indolinone CDK inhibitor with potent and selective inhibition towards cyclin-dependant kinases.

Definition

ChEBI: 3-(1H-imidazol-5-ylmethylidene)-5-methoxy-1H-indol-2-one is a member of indoles.

Biological Activity

Potent, selective cdk2 inhibitor (IC 50 values are 0.022, 0.04, >10, >10, 18 and >100 μ M for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G 1 and G 2 -M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro .

References

[1]. lane me, yu b, rice a, et al. a novel cdk2-selective inhibitor, su9516, induces apoptosis in colon carcinoma cells. cancer res, 2001, 61(16): 6170-6177.
[2]. yu b, lane me, wadler s. su9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight e2f complexes in human colon carcinoma cells. biochem pharmacol, 2002, 64(7): 1091-1100.
[3]. gao n, kramer l, rahmani m, et al. 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 mechanism. mol pharmacol, 2006, 70(2): 645-655.

SU 9516Supplier

Shanghai Boyle Chemical Co., Ltd.
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