RGNCY-0043 (YH249, p300/b-catenin antagonist)

OUT OF STOCK!!  E-mail us at info@reagency.co if you are interested in this product.

YH249 is the first specific p300/β-catenin antagonist that binds directly and specifically to p300, thereby disrupting the p300/β-catenin interaction.  YH249 maintains the pluripotency of mESC and hPSC in a Wnt dependent manner and blocks the differentiation of C2C12 adult mouse muscle setm/progenitor cells.  YH249 may be an invaluable chemogenomic tool to further aid in the dissection of the complexities and divergent outcomes associated with differential coactivator usage in the Wnt signalling cascade.  IC50 for Hek-293, STF1.1 (Wnt/β-catenin-driven luciferase) is 0.06 + 0.08  μM and Survivin-Hek-293 (1KB Human survivin promotor-driven luciferase) is >20 μM.

SMILES: CN1CC(N([C@@H](CC2=CC=C(O)C=C2)C(N(CC3=CC=CC(Cl)=C3N(C)C)C4)=O)[C@@]4([H])N1C(NCC5=CC=CC(OC)=C5OC)=O)=O 

 Systematic Name:  (6S,9aS)-8-(3-chloro-2-(dimethylamino)benzyl)-N-(2,3-dimethoxybenzyl)-6-(4-hydroxybenzyl)-2-methyl-4,7-dioxohexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamideMolecular Weight:  651.16

Formula: C33H39ClN6O6

MWT: 651.16

PMID: 26008738

Reference: Specific Direct Small Molecule p300/β-Catenin Antagonists Maintain Stem Cell Potency. Higuchi Y, Nguyen C, Yasuda SY, McMillan M, Hasegawa K, Kahn M.  Curr Mol Pharmacol. May 26 2015; (Epub ahead of print).

Data Sheet

Interested in this reagent? E-mail us at info@reagency.co and let us know.

Tags: p300, Wnt, RGNCY-0043, YH249, b-Catenin, Catenin, Hek, STF, Survivin