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SU9516 CDK inhibitor

Cat.No.S7636

SU 9516 is a 3-substituted indolinone CDK inhibitor with IC50 of 22 nM, 40 nM, and 200 nM for CDK2, CDK1, and CDK4, respectively.
SU9516 CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 241.25

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Quality Control

Batch: S763601 DMSO]48 mg/mL]false]Ethanol]12 mg/mL]false]Water]Insoluble]false Purity: 99.85%
99.85

Chemical Information, Storage & Stability

Molecular Weight 241.25 Formula

C13H11N3O2

 Storage (From the date of receipt)
CAS No. 377090-84-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC2=C(C=C1)NC(=O)C2=CC3=CN=CN3

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (198.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
CDK2 [1]
22 nM
CDK1 [1]
40 nM
CDK4 [1]
200 nM
In vitro
SU9516 decreases cdk2-specific phosphorylation of the retinoblastoma protein pRB, increases caspase-3 activation, and alters cell cycle in RKO and SW480 cells. This compound also inhibits the cell proliferation, and induces cell apoptosis in both cell lines. [1] It kills leukemic cells through inhibition of RNA Pol II CTD phosphorylation, oxidative damage and transcriptional down-regulation of Mcl-1. [2] In human T-cell leukemia Jurkat cells, this chemical significantly enhances sensitivity to methotrexate. [3] In addition, it also suppresses Aurora-A centrosomal localization and consequent centrosome amplification. [4]
Kinase Assay
CDK kinase assay
Kinase assays are performed in 96-well polypropylene plates. Each reaction contained 2 μg of histone H1 at a final concentration of 10 μM [γ-33P]ATP (0.2 μCi/well; approximately twice the experimentally determined Km), 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100, and 10% glycerol in a 40 μL volume. The reaction is initiated with the addition of 20 μL enzyme (6 ng cdk2/well resulting in a final concentration of 1.6 nM), which is previously diluted 1:50–1:200 in the same buffer, and allowed to proceed for 1 h at room temperature. Reaction is stopped by the addition of 0.01 mL 10% phosphoric acid, and 25 μL of reaction mixture is transferred to P30 phosphocellulose filter mat paper. The filter mat is washed three times with 1.0% phosphoric acid, air dried, and then counted for radioactivity in a liquid scintillation counter. The cdk4 kinase assay for cyclin D1-cdk4 is carried out in a polypropylene 96-well microtiter plate format measuring the incorporation of radioactive phosphate into GST-Rb. Purified cyclin D1-cdk4 is incubated with 1 μg GST-Rb in 20 mM HEPES (pH 7.5) in the presence of 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100, and 10% glycerol. The final cdk4 concentration is 10 ng/well, or 1.6 nM. Kinase reaction is initiated by the addition of ATP at a final concentration of 10 μM ATP (twice the experimentally determined Km) and [γ-33P]ATP (1.0 μCi per well) in a 60-μL volume and allowed to proceed at room temperature for 1 h. Reaction is stopped by the addition of 0.01 ml 10% phosphoric acid, and 25 μL of reaction mixture is transferred to P30 phosphocellulose filter mat paper. The filter mat is treated as for Cdk1/Cdk2 assays.
References

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