SEL120-34A HCl

SKU: orb1309850

Description

SEL120-34A HCl is a potent, ATP-competitive, and orally bioavailable small molecule inhibitor of CDK8 and CDK19. It demonstrates antitumor activity in research models and is a valuable tool for investigating the role of the Mediator kinase module in oncology, inflammation, and super-enhancer driven transcription both in vitro and in vivo.

Research Area

Cell Biology

Key Properties

• CAS Number: 1609452-30-3
• MW: 450.6
• Purity: 98.13% (May vary between batches)
• Formula: C₁₅H₁₉Br₂ClN₄
• SMILES: Cl.Cc1c(Br)c(Br)c2CCCn3c(nc1c23)N1CCNCC1
• Target: CDK
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:0.5 mg/mL (1.11 mM);DMSO:8.33 mg/mL (18.49 mM)

Bioactivity

• Target IC50:
  CDK8-CyclinC:4.4 nM (IC50)|CDK19-CyclinA:10.4 nM (IC50)|CDK9-CyclinT:1070 nM (IC50)
• In Vivo:
  The growth of tumor in mice bearing MV4-11 cancer cells inhibited by SEL120-34A (30, 60 mg/kg, p.o.), and also arrests the growth of KG-1-derived tumors at 30 mg/kg via oral administration.
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• In Vitro:
  SEL120-34A HCl is a selective, ATP-competitive inhibitor of CDK8(IC50 of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively). SEL120-34A HCl is active against a panel of AML cell lines (GI50<1 μM), such as SKNO-1, KG-1, HEL-60, MOLM-16, MV-4-11, OciAML-2, MOLM-6 and OciAML-3 cells, consistent with the effective inhibition range of STAT1 S727 and STAT5 S726.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK9/cycT, CDK8/CycC, CDK19/CycC, CDK, Cyclin dependent kinase, inhibit, Inhibitor, SEL12034A HCl, SEL-120-34A HCl, SEL120-34A HCl, SEL120 34A HCl

Compound Identifiers

PubChem CID

73776232