BAP1-IN-1

SKU: orb2900555

Description

BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 353495-21-3
• MW: 292.33
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₆N₂O₂
• SMILES: O=[N+]([O-])C1=CC=C2NC(C3CC=CC3C2=C1)C4=CC=CC=C4
• Solubility: In Vitro: DMSO : 50 mg/mL (171.04 mM; Ultrasonic )

Bioactivity

• In Vivo:
  BAP1-IN-1 (Compound 8) (50 mg/kg/d; i.p.; 4 weeks) delays the progression of ASXL1-mutant leukemia and improves survival in mice. Animal model: NSGS mice, K562 (ASXL1-WT/Y591*) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588*) model. Dosage: 50 mg/kg/d. Administration: Intraperitoneal injection, drug treatments were started at day 28 after transplantation. Result: Significantly delayed progression of disease in both models.
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• In Vitro:
  BAP1-IN-1 (Compound 8) (1 μM; 30 min) specifically inhibits BAP1 not just in vitro but also within the cellular context. BAP1-IN-1 (0.1 μM; 24 h) significantly alters 240 genes in BAP1-WT cells, whereas only 33 transcripts are changed in BAP1-KO cells, demonstrating that the gene expression changes mainly depend on the presence of BAP1 protein. BAP1-IN-1 (0-10 μM; 72 h) selectively inhibits cells with ASXL1 GOF mutations. Western blot analysis. Cell line: CAL51 cells. Concentration: 1 μM. Incubation time: 30 min. Result: Remarkably inhibited BAP1 catalytic activity. Cell Viability Assay Cell line: THP1, MOML13, K562, THP1-ASXL1-WT and THP1-ASXL1-Y591fs cells. Concentration: 0, 0.1, 0.3, 1, 3 and 10 μM Incubation time: 72 h. Result: K562 cells (ASXL1-Y591*) were significantly more sensitive to the treatment. Cells with ASXL1fs mutations were ten times more sensitive to the treatment.
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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