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Chemical Structure : iBAP-II
Catalog No.: 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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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.
| M.Wt | 308.337 | |
| Formula | C18H16N2O3 | |
| Appearance | Solid | |
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1. Natsumi Tsuboyama, et al. Oncogene. 2022 Feb.
2. Lu Wang, et al. Nat Cancer. 2021 May;2(5):515-526.
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