BAP1-IN-1

Research use only, not for human use.

BAP1-IN-1 is an inhibitor of the catalytic activity of BRCA1-associated protein 1 (BAP1), which is related to cancer and can be used to study cancer.

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

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.

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*) modelDosage: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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353495-21-3

292.33

C18H16N2O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (171.04 mM; Ultrasonic )

O=[N+]([O-])C1=CC=C2NC(C3CC=CC3C2=C1)C4=CC=CC=C4

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(-20℃)

With Ice Pack

≥ 2 years