CBFβ Inhibitor

SKU: orb1306073

Description

This small molecule inhibitor is cell-permeable and specifically disrupts the interaction between CBFβ and Runx1. It serves as a valuable research tool for studying Runx complex function in hematopoiesis and leukemia, applicable in both cellular and biochemical assays.

Research Area

Cell Biology, Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 493028-20-9
• MW: 234.32
• Purity: 96.50% (May vary between batches)
• Formula: C₁₂H₁₄N₂OS
• SMILES: CCC1=C(N=C(N)S1)C1=CC=C(OC)C=C1
• Target: DNA/RNA Synthesis
• Solubility: Ethanol:25 mg/mL (106.69 mM);DMSO:55 mg/mL (234.72 mM)

Bioactivity

• In Vitro:
  The ELISA results have shown that CBFβ Inhibitor is very effective in inhibiting the CBFβ-Runx1 interaction (IC50: 3.2 μM). In the leukemia cell line ME-1 expressing CBFβ-SMMHC, CBFβ Inhibitor reduced cell proliferation dose-dependently. Treatment with CBFβ Inhibitor for 3 days showed an increase in apoptotic cells. Treatment with CBFβ Inhibitor for 14 days individually or with all-trans-retinoic acid (ATRA) resulted in cells with greater variation in size and shape, lower nuclear-to-cytoplasmic ratio, increased folding, and lobation of nuclei, and more clumped chromatin. All of these morphology changes are consistent with differentiation to more mature forms. CBFβ Inhibitor at 50 μM increased proliferation of Hep-G2 cells. CBFβ treatment with Inhibitor resulted in a statistically significant reduction in Runx1 bound to DNA .
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Storage & Handling

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

Alternative Names

RNA Synthesis, RNASynthesis, 5-Ethyl-4-(4-methoxy-phenyl)-thiazol-2-ylamine, CBF, CBFβ Inhibitor, CBFb Inhibitor, CBFbeta Inhibitor, DNA Synthesis, DNASynthesis

Compound Identifiers

PubChem CID

828523