Windorphen

A cell-permeable bis(4-methoxyphenyl)chloroacrylaldehyde whose (Z)-isomer (isomeric content 12-15%) acts as a p300-selective histone acetytransferase (HAT) inhibitor (IC₅₀ = 4.2 µM) and selectively disrupts β-catenin association with p300, but not CBP or LEF1/TCF4, exhibiting much reduced potency against KAT5, CBP, MYST4, MYST2 (IC₅₀ = 38.2, 51.3, 59.5, 62.2 µM, respectively) and little or no inhibitory efficacy toward GCN5 and PCAF HAT activity (IC₅₀ >100 µM). Shown to preferentially suppress human and mouse β-catenin-, zebrafish β-catenin-1-, but not zebrafish β-catenin-2-, mediated transcription activity in various reporter assays (20 µM) without affecting β-catenin activation or nuclear translocation. Induces apoptosis in Wnt signaling-dependent cancer cultures (IC₅₀ in µM = 15.0/SW480, 19.2/RKO, 21.8/DU135, and 19.0/PC3; 72 h) in vitro without affecting the viability of Wnt-independent human lung cander cell line H460 (up to 200 µM & 72 h) and selectively abrogates Wnt signaling in ventral & lateral regions, but not within dorsal organizer, in 5.3 hpf epiboly stage zebrafish embryos in vivo, indicating that the Zebrafish β-catenin-1 & -2 regulate separate Wnt signaling events during zebrafish embryo development by associating with distinct binding partners. A great complement to the selective β-catenin-CBP interaction blocker ICG-001 (Cat. no. 504712) Pure (E)-isomer is available separately as a negative control.

Cell permeable: yes

Reversible: yes

Packaged under inert gas

Use only fresh DMSO for reconstitution.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)