Senexin A

SKU: orb1301597

Description

Senexin A is a potent and selective small molecule inhibitor of CDK8 (Kd = 0.83 µM) and CDK19 (Kd = 0.31 µM). It is a valuable research tool for studying the Mediator complex in oncology and inflammation, with utility in both in vitro biochemical assays and cellular pathway analysis.

Research Area

Cell Biology

Key Properties

• CAS Number: 1366002-50-7
• MW: 274.32
• Purity: 98.00%
• Formula: C₁₇H₁₄N₄
• SMILES: N#Cc1ccc2ncnc(NCCc3ccccc3)c2c1
• Target: CDK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (14.58 mM);DMSO:100 mg/mL (364.54 mM)

Bioactivity

• Target IC50:
  CDK19:0.31 μm|CDK8:0.83 μM
• In Vivo:
  Administering Senexin A daily for five days completely counteracts the tumor-promoting effects of chemotherapy, displaying no detectable toxicity or significant impacts on body weight, organ weights, or blood cell counts in C57BL/6 mice. The adverse effects of doxorubicin treatment are entirely negated when followed by Senexin A administration, significantly enhancing the responsiveness of A549/MEF tumors to doxorubicin.
• In Vitro:
  Senexin A inhibited CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively and CDK8 kinase activity with IC50 of 0.28 μM.CDK8 stimulates Wnt/β-catenin, and Senexin A inhibits β-catenin–dependent transcription in HCT116 colon carcinoma cells.
• Animal Research:
  Tumor-free C57BL/6-derived SCID mice were injected with a single dose of doxorubicin or carrier control. Five days later, mice received. injection of 2 × 10^6 human A549 lung carcinoma cells, and tumor take was measured over 4 wk.

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

Inhibitor, inhibit, CDK, CDK8, Cyclin dependent kinase, Senexin A

Compound Identifiers

PubChem CID

56927063