33 products were found matching "K11723"!

LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with Kd values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry. It is selective for BRD7/9 over a panel of 48 BRDs at concentrations up to 10 µM determined using differential scanning...

Protein function: Acts both as coactivator and as corepressor. May play a role in chromatin remodeling. Activator of the Wnt signaling pathway in a DVL1-dependent manner by negatively regulating the GSK3B phosphotransferase activity. Induces dephosphorylation of GSK3B at 'Tyr-216'. Down-regulates TRIM24-mediated...

BRD9 contains a single bromodomain and has five isoforms that are produced by alternative splicing. It is thought to function in chromatin remodeling as part of the SWI/SNF complex. I-BRD9 is a BRD9 bromodomain inhibitor with a pIC50 value of 7.3 and a pKd value of 8.7. It displays 700-fold greater selectivity over...

BI-7273 is a potent BRD9 bromodomain inhibitor (Kd = 15.4 nM, IC50 = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC50 = 117 nM). It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1...

MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4). It is characterized as a proteolysis-targeting chimera (PROTAC) and contains JQ-1, which binds bromo- and extra-terminal (BET) proteins, linked to a ligand for the E3 ubiquitin ligase VHL. MZ1...

TP-472 is an inhibitor of bromodomain BRD9 (Kd = 33 nM, EC50 = 320 nM in a NanoBRET assay). It has >30-fold selectivity over all other bromodomain family members with the exception of the highly homologous BRD7 bromodomain (Kd = 340 nM in an isothermal titration calorimetry (ITC) assay). See the Structural Genomic...

BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM, IC50s = 75 nM and 3.4 µM, respectively) that demonstrates cellular activity by semi-quantitative FRAP assay with ~90% inhibition of BRD9 and BRD7 at 0.1 µM and 1 µM, respectively. It does not bind to other bromodomain-containing...

Protein function: Acts both as coactivator and as corepressor. May play a role in chromatin remodeling. Activator of the Wnt signaling pathway in a DVL1-dependent manner by negatively regulating the GSK3B phosphotransferase activity. Induces dephosphorylation of GSK3B at 'Tyr-216'. Down-regulates TRIM24-mediated...

This gene encodes a protein which is a member of the bromodomain-containing protein family. The product of this gene has been identified as a component of one form of the SWI/SNF chromatin remodeling complex, and as a protein which interacts with p53 and is required for p53-dependent oncogene-induced senescence...

The acetylation of histone lysine residues plays a crucial role in the epigenetic regulation of gene transcription. Acetylated lysine residues are recognized by a small protein domain known as a bromodomain. These domains function in linking protein complexes to acetylated nucleosomes, thereby controlling chromatin...

This gene encodes a protein which is a member of the bromodomain-containing protein family. The product of this gene has been identified as a component of one form of the SWI/SNF chromatin remodeling complex, and as a protein which interacts with p53 and is required for p53-dependent oncogene-induced senescence...