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.
More Information Supplier PageMethyl-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.
More Information Supplier PageGNE-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.
More Information Supplier PageGNE-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.
More Information Supplier PageGNE-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.
More Information Supplier PageVX-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.
More Information Supplier PageVX-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.
More Information Supplier PageVX-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.
More Information Supplier PageRogaratinib(BAY-1163877) is a highly potent and selective small molecule inhibitor of pan‐FGFR kinase activity, which specifically inhibits FGFR1, 2, 3 and 4 with an IC50 values of 1.8 nM,
More Information Supplier PageTapotoclax (AMG-176) is a potent, selective, and orally bioavailable macrocyclic inhibitor of MCL1 with a Ki of 0.13 nM. It induces a potent apoptosis in models of hematologic malignancies.
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