CDK8-IN-12

SKU: orb1745164

Description

CDK8-IN-12 is a potent, selective, and orally bioavailable CDK8 inhibitor (Ki: 14 nM) with additional activity against GSK-3α/β and PCK-θ. It demonstrates anti-proliferative effects in MV4-11 leukemia cells and is a valuable chemical probe for researching transcription-dependent cancers and inflammatory diseases in experimental models.

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2613307-67-6
• MW: 381.86
• Purity: 99.83% (May vary between batches)
• Formula: C₂₁H₂₀ClN₃O₂
• SMILES: O=C1C2(CCN(CC2)C=3C(=CN=CC3Cl)C4=CC=5C(O4)=CC=CC5)CCN1
• Target: GSK-3,PKC,CDK
• Solubility: DMSO:27.5 mg/mL (72.02 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.24 mM)

Bioactivity

• Target IC50:
  MV-4-11 cells:0.36 μM(GI50)|GSK-3β:4 nM(ki)|PCKθ:109 nM(ki)|GSK-3α:13 nM(ki)|CDK8:14 nM(Ki)
• In Vivo:
  CDK8-IN-12 (intravenous administration ; 5 mg/kg in rats ; 2 mg/kg in mice) had a T1/2 of 0.9 h and 0.34 h in rats and mice, respectively.
• In Vitro:
  CDK8-IN-12 (0.36, 0.72 μM ; 2 h) significantly reduced the phosphorylation of STAT1 serine 727.

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

CDK8, CDK8IN12, CDK8-IN-12, GSK3, GSK-3α, GSK-3β

Compound Identifiers

PubChem CID

162643699