Chemical Structure : BAY-184
CAS No.: 2520347-03-7
Catalog No.: PC-23297Not For Human Use, Lab Use Only.
BAY-184 is a potent, selective and in vivo-active KAT6A/B inhibitor with IC50 of 71/83 nM respectively.
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10 mg | $458 | In stock | |
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BAY-184 is a potent, selective and in vivo-active KAT6A/B inhibitor with IC50 of 71/83 nM respectively.
BAY-184 displays an overall good selectivity, with high selectivity against the close members of the MYST family, with only a residual low micromolar activity for KAT7 (11-fold), and with no activity against the more distantly related histone acetyltransferase p300 (IC50 > 10 μM).
BAY-184 also shows high selectivity against a full kinase panel at a concentration of 10 μM (366 kinases) at Eurofins.
BAY-184 (1 uM) elicited a swift decline in H3K23ac levels in ZR-75-1 cells, shows IC50 of 670 nM for H3K23 acetylation in HTRF assays, and IC50 of 168 nM in ER target gene reporter assay.
BAY-184 inhibits cell growth of ZR-75-1 breast cancer cells with IC50 of 130 nM, shows IC50 values of <1 uM against ER-positive breast cancer subtypes.
BAY-184 (50-150 mg/kg, po, twice daily (2 qd)) induced a dose-dependent inhibition of tumor growth in ZR-75-1 xenografts.
M.Wt | 420.48 | |
Formula | C23H20N2O4S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-([1,1'-Biphenyl]-2-sulfonyl)-6-(dimethylamino)-1-benzofuran-2-carboxamide |
1. Ter Laak A, et al. J Med Chem. 2024 Oct 25. doi: 10.1021/acs.jmedchem.4c01709.
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