BAP1-IN-1

• CAT Number: I042070
• CAS Number: 353495-21-3
• Molecular Formula: C18H16N2O2
• Molecular Weight: 292.33
• Purity: ≥95%
• Synonyms: 8-nitro-4-phenyl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
• InChI: InChI=1S/C18H16N2O2/c21-20(22)13-9-10-17-16(11-13)14-7-4-8-15(14)18(19-17)12-5-2-1-3-6-12/h1-7,9-11,14-15,18-19H,8H2
• InChIKey: FBKCRWSTGRHOGI-UHFFFAOYSA-N
• SMILES: C1C=CC2C1C(NC3=C2C=C(C=C3)[N+](=O)[O-])C4=CC=CC=C4

BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM[1].
BAP1-IN-1 (Compound 8) (1 μM; 30 min) specifically inhibits BAP1 not just in vitro but also within the cellular context[1].
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[1].
BAP1-IN-1 (0-10 μM; 72 h) selectively inhibits cells with ASXL1 GOF mutations[1].
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[1].

Reference

[1]. Wang L, et al. Epigenetic targeted therapy of stabilized BAP1 in ASXL1 gain-of-function mutated leukemia. Nat Cancer. 2021 May;2(5):515-526.
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