BAP1-IN-1_product_DataBase

Bioactivity	BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM[1].
Target	IC50: 0.1-1 μM (BAP1)
Invitro	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]. Western Blot Analysis[1] Cell Line:
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[1]. Animal Model:
Name	BAP1-IN-1
CAS	353495-21-3
Formula	C18H16N2O2
Molar Mass	292.33
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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