Home Cell Cycle CDK inhibitor SU9516 For research use only.

SU9516

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 Chemical Structure

SU9516 Chemical Structure

CAS: 377090-84-1

Selleck's SU9516 has been cited by 3 Publications

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Purity & Quality Control

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

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Biological Activity

Description 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.
Targets
CDK2 [1] CDK1 [1] CDK4 [1]
22 nM 40 nM 200 nM
In vitro
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. SU9516 also inhibits the cell proliferation, and induces cell apoptosis in both cell lines. [1] SU9516 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, SU9516 significantly enhances sensitivity to methotrexate. [3] In addition, SU9516 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.
Cell Research Cell lines RKO cells and SW480 cells
Concentrations 24 hours
Incubation Time ~50 μM
Method RKO cells and SW480 cells are seeded in replicates in 96-well plates at 1 × 104 cells/well and allowed to attach overnight. SU9516 is added in concentrations from 0.05 μM to 50.00 μM for 24 h, the cells are then washed twice with PBS, and cells are replenished with complete media. The cells are fixed at 0, 4, and 7 days post-drug removal and assayed for protein levels using a modified SRB cytotoxicity assay. The cells are fixed in 10% trichloroacetic acid for 1 h, washed in distilled H2O, and stained in 0.4% SRB/acetic acid for 30 min. The cells are then washed in 0.1% acetic acid, solubilized in 10 mM Tris (pH 9), and analyzed on a Bio-Rad 360 microplate reader at 595 nm. All experiments are repeated at least three times.

Chemical lnformation & Solubility

Molecular Weight 241.25 Formula

C13H11N3O2
CAS No. 377090-84-1 SDF Download SU9516 SDF
Smiles COC1=CC2=C(C=C1)NC(=O)C2=CC3=CN=CN3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 48 mg/mL ( (198.96 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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