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iBAP-II | BAP1 inhibitor

CAS:
1013813-81-4
Catalog Number:
10-4038
Activity:
BAP1 inhibitor
Chemical Names:
4-(8-Nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-yl)phenol
Molecular Weight:
308.33
Molecular Formula:
C18H16N2O3
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

iBAP-II (1013813-81-4) is an inhibitor of the H2AK119 deubiquitinase BAP1 (IC50 = 0.092 µg/ml).  It is selective for BAP1 over UCHL5, USP5,7,8, TNFAIP3-catalytic domain, USP2-catalytic domain, Otubain-1, and Ataxin3. iBAP-II disrupted the BAP1/ASXL3/BRD4 axis via induction of protein degradation of the ASXL3 scaffold protein in the small cell lung cancer lines NCI-H1963, NCI-H748, and NCI-H1882.  It also suppressed expression of the master transcription factor ASCL1 in NCI-H1963 small cell lung cancer cells. iBAP-II significantly delayed disease progression in a small cell lung cancer xenograft mouse model.

References/Citations:

  1. Tsuboyama et al. (2022), Therapeutic targeting of BAP1/ASXL3 sub-complex in ASCL1-dependent small cell lung cancer; Oncogene 41 2152
iBAP-II | BAP1 inhibitor is also available in the Cellular Metabolism Library.
CAS:
1013813-81-4
Catalog Number:
10-4038
Activity:
BAP1 inhibitor
Chemical Names:
4-(8-Nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-yl)phenol
Molecular Weight:
308.33
Molecular Formula:
C18H16N2O3
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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