SU9516 SU9516 is a selectively potent ATP-competitive inhibitor of CDKs; displays anti-proliferative and proapoptotic properties in tumor cells.

SU9516  (CAS 666837-93-0)

SU9516 is rated 5.0 out of 5 by 2.
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| See 3 Citations
Synonym: (Z)-3-((1H-imidazol-5-yl)methylene)-5-methoxyindolin-2-one
Application: A selectively potent ATP-competitive inhibitor of CDKs
CAS Number: 666837-93-0
Molecular Weight: 241.25
Molecular Formula: C13H11N3O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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PRODUCT NAME CATALOG # UNIT PRICE QTY FAVORITES
SU9516 sc-204905 5 mg $149.00

SU9516 is a 3-substituted indolinone compound displaying anti-proliferative and proapoptotic properties in tumor cells. SU9516 displays activity as a selectively potent ATP-competitive inhibitor of CDKs. It also shows no significant effect (IC50 >10 μM) on the activities of PKC, p38, PDGFRβ, or EGFR. SU9516 has an Inhibitory effect on proliferation of growth-factor stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F. SU9516 is an inhibitor of Cdc2, Cdk2 and Cdk4.


References

1. Lane, M E., et al., 2001. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer research. 61(16): 6170-7. PMID: 11507069
2. Yu, Bo., et al., 2002. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochemical pharmacology. 64(7): 1091-100. PMID: 12234612

Physical State :
Solid
Solubility :
Soluble in DMSO (10 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/A: IC50 = 22 nM; Cdk1/B: IC50 = 40 nM; Cdk4/D1: IC50 = 200 nM; PKC: IC50 = >10 µM ; p38: IC50 = >10 µM ; PDGFR: IC50 = 18 µM ; EGFR : IC50 = >100 µM ; ATP-dependent molecular chaperone HSP82: EC5050 = 1250 nM (Candida albicans ); Trypanosoma brucei: EC5050 = 180 nM
pK Values :
pKa: 12.20, pKb: 4.74
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5289419
MDL Number :
MFCD05865243
SMILES :
COC1=CC2=C(C=C1)NC(=O)/C2=CC3=CN=CN3

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Certificate of Analysis

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Citations 1 to 3 of 3 total

PMID: # 25394488
Su, M. et al. 2015. MicroRNA-221 inhibits autophagy and promotes heart failure by modulating the p27/CDK2/mTOR axis. Cell death and differentiation. 22: 986-99.

PMID: # 24101496
Bogdanow, et al. 2013. Human cytomegalovirus tegument protein pp150 acts as a cyclin A2-CDK-dependent sensor of the host cell cycle and differentiation state. Proc Natl Acad Sci U S A. 110: 17510-5.

PMID: # 20844576
Zydek, M. et al. 2010. Cyclin-dependent kinase activity controls the onset of the HCMV lytic cycle. PLoS Pathog.. 6: -.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Yu et al Yu et al. (PubMed ID 12234612) found that kinase inhibitor, SU9516, induced colon carcinoma cell growth arrest via downregulation of cyclin D1 and inhibition of cdk2 activity. -SCBT Publication Review
Date published: 2015-04-12
Rated 5 out of 5 by from Great antibody theses reagents worked well Great antibody theses reagents worked well
Date published: 2015-10-27
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