SMARCA4 and SMARCA2 |
Glioblastoma |
PFI-3 targets the essential bromodomain and blocks SWI/SNF’s chromatin binding [167,168]. |
SMARCA2 and SMARCA4 |
SMARCA4-deficient lung-cancer; uveal melanoma |
A dual allosteric small-molecule inhibitor targets ATPase activity of SMARCA2 and SMARCA4 [169]. |
SMARCA2 and SMARCA4 |
AR/FOXA1-driven prostate cancer |
AU-15330 is a proteolysis-targeting chimera degrader of the SMARCA2 and SMARCA4 [170]. |
SMARCA2 and SMARCA4 |
SMARCA4-mutant lung cancer |
SMASh degron-mediated SMARCA2 depletion [171]. |
SMARCA2, SMARCA4, and PBRM1 |
Unknown |
GNE-064 is a chemical probe targeting the bromodomains SMARCA2, SMARCA4, and PBRM1 [172]. |
PBAF complex |
Unknown |
LM146 targets the PBAF complex component by blocking the specific bromodomains within the complex [173]. |
BRD7/9 |
Unknown |
Compounds LP99 is selective inhibitor of the BRD7 and BRD9 bromodomains [174]. |
BRD7/9 |
Unknown |
VZ185 is a selective and rapid degrader of BRD9 and of its close homolog BRD7 [175]. |
BRD7/9 |
Unknown |
GSK6776 as a soluble and selective BRD7/9 inhibitor [176]. |
BRD9 |
AML xenograft model |
BI-7273 and BI-956456 are potent and selective BRD9 bromodomain inhibitors [177]. |
BRD9 |
Unknown |
GNE-375 is a small-molecule inhibitor of the BRD9 bromodomain [178]. |
BRD9 |
Human AML |
I-BRD9 is BRD9 bromodomain inhibitor [179]. |
BRD9 |
Human AML |
Compound dBRD9 bridges the BRD9 bromodomain and the E3 ubiquitin ligase complex for degradation [180]. |
BPTF |
Breast cancer cells |
Compound BZ1 targets the BPTF bromodomain [181]. |
BPTF |
Lung cancer cells |
Compounds Cpd8 and Cpd10 are highly potent and selective inhibitors of the BPTF bromodomain [22]. |