SU 9516A cell permeable, potent, selective and ATP-competitive inhibitor

SU 9516 (CAS 377090-84-1)

SU 9516 | CAS 377090-84-1 is rated 5.0 out of 5 by 1.
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Synonym: 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
Application: A cell permeable, potent, selective and ATP-competitive inhibitor
CAS Number: 377090-84-1
Molecular Weight: 241.25
Molecular Formula: C13H11N3O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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SU 9516 is a cell permeable, potent, selective and ATP-competitive inhibitor of Cdk2/cyclin A (IC50=22nM), Cdk1/cyclin B (IC50=40nM) and Cdk4/cyclin D1 (IC50=200nM). SU9516 has no effect on the activity of PKC, p38, PDGFRβ and EGFR (IC50>10μM). The compound displays anti-proliferative and pro-apoptotic properties in tumor cells and inhibits proliferation of growth factor-stimulated colon carcinoma cells. SU 9516 does this by binding to Cdk2 and thus preventing the phosphorylation of pRb and its dissociation from E2F.


References

M.E. Lane, et al.; Cancer Res. 61, 6170 (2001). B. Yu, et al.; Biochem Pharmacol. 64, 1091 (2002). D.J. Moshinsky, et al.; BBRC 310, 1026 (2003). X. Li, et al.; Bioorg. Med. Chem. Lett. 13, 1939 (2003).

Physical State :
Solid
Solubility :
Soluble in DMSO (17 mg/ml), and ethanol (20 mM). Insoluble in water.
Storage :
Store at 4° C
Melting Point :
220.28° C (Predicted)
Boiling Point :
601.52° C at 760 mmHg (Predicted)
Density :
1.38 g/cm3 (Predicted)
Refractive Index :
n20D 1.70 (Predicted)
IC50 :
cdk2: IC50 = 22 nM; cdk1: IC50 = 40 nM; cdk4: IC50 = 0.2 µM; PKC: IC50 = >10 µM; p38: IC50 = >10 µM; PDGFR: IC50 = 18 µM; EGFR: IC50 = >100 µM
pK Values :
pKa: 12.2 (Predicted), pKb: 4.74 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5289419
MDL Number :
MFCD05865243
SMILES :
COC1=CC\2=C(C=C1)NC(=O)/C2=C\C3=CN=CN3

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Certificate of Analysis

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SU 9516  Product Citations

See how others have used SU 9516. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 25394488  Su, M. et al. 2015. Cell Death Differ. 22: 986-99.

PMID: # 24101496  Bogdanow, et al. 2013. Proc Natl Acad Sci U S A. 110: 17510-5.

PMID: # 20844576  Zydek, M. et al. 2010. PLoS Pathog. 6: -.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from An increase in p21 protein expression was An increase in p21 protein expression was observed by WB in HCT 116 cells after treatment with SU 9516. -SCBT QC
Date published: 2015-01-23
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