Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein’s interaction with ERα.

Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein’s interaction with ERα.

GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively.

Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein’s interaction with ERα.

GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively.

GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively.

VX-984 (M9831) is an orally active, potent, selective, and ATP-competitive inhibitor of DNA-PK. VX-984 effectively suppresses non-homologous end joining (NHEJ) and increases DNA double-strand breaks (DSBs). It enhances the cytotoxic effects of ionizing radiation (IR) in various cancer cell lines, including non-small cell lung cancer (NSCLC) cell lines, in vitro. Additionally, VX-984 reduces DNA-PKcs autophosphorylation.