SU9516

SKU: orb1301017

Description

SU9516 is a potent and selective small molecule inhibitor of CDK2 (IC50 = 22 nM), with additional activity against CDK1 and CDK4. It is widely used in biochemical and cellular research to study cell cycle regulation, proliferation, and has been applied in both in vitro and in vivo cancer models.

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 377090-84-1
• MW: 241.25
• Purity: >99.99% (May vary between batches)
• Formula: C₁₃H₁₁N₃O₂
• SMILES: C(=C\1/C=2C(NC1=O)=CC=C(OC)C2)\C3=CN=CN3
• Target: CDK,PKC,p38 MAPK,Apoptosis,Autophagy
• Solubility: Ethanol:4.8 mg/mL (19.9 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (10.36 mM);H2O:<1 mg/mL (insoluble);DMSO:55 mg/mL (227.98 mM)

Bioactivity

• Target IC50:
  PDGFR:18000 nM|CDK2:22 nM|CDK4:200 nM|CDK1:40 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. SU9516 also inhibits the cell proliferation, and induces cell apoptosis in both cell lines. SU9516 kills leukemic cells through inhibition of RNA Pol II CTD phosphorylation, oxidative damage and transcriptional down-regulation of Mcl-1. In human T-cell leukemia Jurkat cells, SU9516 significantly enhances sensitivity to methotrexate. In addition, SU9516 also suppresses Aurora-A centrosomal localization and consequent centrosome amplification.
• Cell Research:
  Method: Cells are seeded at 2×103/well of white bottom 96-well plates, treated with INCB018424 from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37 ℃ in an atmosphere containing 5% CO2. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC50 curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK2, CDK4, CDK1, CDK, Cyclin dependent kinase, Autophagy, Apoptosis, inhibit, Inhibitor, SU 9516, SU9516, SU-9516, p38 MAPK, p38, p38MAPK, PKC

Compound Identifiers

PubChem CID

5289419