BI8626

SKU: orb2655815

Description

BI8626 (BI-8626) is a specific, small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 0.9 uM, does not inhibit the activity of other HECT-domain ubiquitin ligases (HECW2, NEDD4,UBA1 and UbcH5b, IC50>50 uM); suppresses colony formation of Ls174T cells with IC50 of 0.7 uM; inhibits MYC-dependent transactivation in colorectal cancer cells, but not in stem and normal colon epithelial cells; stabilizes MYC-associated protein MIZ1.

Key Properties

• CAS Number: 1875036-75-1
• MW: 440.555
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₈N₈
• SMILES: NCC1=CC(CNC2=C(N=CN=C3N4CCN(CC5=CC=CC=C5)CC4)C3=NC=N2)=CC=C1
• Target: E3 Ubiquitin Ligase
• Solubility: In Vitro: DMSO : 83.33 mg/mL (189.15 mM)

Bioactivity

• In Vitro:
  Cell Cycle Analysis Cell line: Ls174T cells. Concentration: 0 μM, 5 μM, 10 μM, 15 μM, 20 μM. Incubation time: 0-4 days. Result: Retarded passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1. Western blot analysis. Cell line: U2OS cells. Concentration: 0 μM, 20 μM, 50 μM. Incubation time: 0 hour, 1 hour, 2 hours, 4 hours, 6 hours. Result: Retarded the degradation of MCL1 in response to UV irradiation in HeLa cells by inhibiting HUWE1 in U2OS cells.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BI-8626 | BI 8626

Quick Database Links

Gene Symbol

E3 Ubiquitin Ligase