iBAP-II | BAP1 inhibitor | Probechem Biochemicals

Chemical Structure : iBAP-II

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iBAP-II (BAP1 inhibitor II)

货号: PC-72296Not For Human Use, Lab Use Only.

iBAP-II (BAP1 inhibitor II) is a next-generation, specific small molecule inhibitor of BAP1 histone H2A deubiquitinase activity with IC50 of <0.1 ug/mL.

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生物&药学活性

iBAP-II (BAP1 inhibitor II) is a next-generation, specific small molecule inhibitor of BAP1 histone H2A deubiquitinase activity with IC50 of <0.1 ug/mL.
iBAP-II displays higher affinity for BAP1 than the closest UCH family member, UCHL5, and other deubiquitinases, such as USP5, USP7, USP8, TNFAIP3-catalytic domain, USP2-catalytic domain, Otubain-1, and Ataxin3.
Inhibition of BAP1 via iBAP-II reduces ASXL3 protein stability in small cell lung cancer cells, without significant changes to ASXL1 and ASXL2 protein levels.
iBAP-II suppresses ASCL1 expression in NCI-H1963 cells, along with the mRNA levels involving a handful of known ASCL1 transcriptional targeted genes, such as GRP, DMPK, RNF183, SCN3A, MYCL, and CACNA1A.
iBAP-II exhibited more potent cell viability inhibition activity on four different BAP1-WT SCLC cell lines than iBAP.
iBAP-II (50 mg/kg/d) significantly delayed the disease progression in SCLC xenograft model.

物理化学性质&存储条件

分子量	308.337
分子式	C18H16N2O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(8-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-4-yl)phenol

参考文献

1. Natsumi Tsuboyama, et al. Oncogene. 2022 Feb.

2. Lu Wang, et al. Nat Cancer. 2021 May;2(5):515-526.

iBAP-II (BAP1 inhibitor II)

生物&药学活性

物理化学性质&存储条件

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iBAP-II (BAP1 inhibitor II)

生物&药学活性

物理化学性质&存储条件

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