iBAP-II
Modify Date: 2024-01-03 19:45:05
iBAP-II structure
|
Common Name | iBAP-II | ||
|---|---|---|---|---|
| CAS Number | 1013813-81-4 | Molecular Weight | 308.337 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C18H16N2O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of iBAP-IIiBAP-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. |
| Name | iBAP-II |
|---|
| Description | 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. |
|---|---|
| References | 1. Natsumi Tsuboyama, et al. Oncogene. 2022 Feb. 2. Lu Wang, et al. Nat Cancer. 2021 May;2(5):515-526. |
| Molecular Formula | C18H16N2O3 |
|---|---|
| Molecular Weight | 308.337 |