$ 235.20
Details
The racemic mixture of a cell-permeable (4-methoxyphenyl)chloroacrylaldehyde compound whose ( Z )-isomer (isomer content 12-15%) acts as a p300-selective histone acetytransferase (HAT) inhibitor (IC50 = 4.2μM using racemic mixture with 13% Z-isomer) and selectively disrupts β-catenin association with p300, but not CBP or LEF1/TCF4, exhibiting much reduced potency against KAT5, CBP, MYST4, MYST2 (IC50 ≥38μM) and little or no inhibitory efficacy toward GCN5 and PCAF HAT activity (IC50 >100μM). Shown to selectively prevents human and mouse β-catenin-, zebrafish β-catenin-1-, but not zebrafish β-catenin-2-, mediated transcription activity without affecting β-catenin activation or nuclear translocation. Induces apoptosis in Wnt signaling-dependent cancer cultures (IC50 15 to 22μM; 72 h) in vitro without affecting the viability of Wnt-independent H460 (up to 200μM and 72 h) and selectively abrogates Wnt signaling in ventral and lateral regions, but not within dorsal organizer, in 5.3 hpf epiboly stage zebrafish embryos in vivo . A great complement to the selective β-catenin-CBP interaction blocker ICG-001 (Cat. no. 504712). ( E )-isomer is available separately (Cat. no.509166) as negative control.
