Key Specifications Table
|Empirical Formula||CAS #|
Pricing & Availability
An invalid quantity was specified. The product quantity has been adjusted.
|5.09164.0001||Glass bottle||25 mg||
|Overview||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 = 4.2 µM 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 ≥38 µM) and little or no inhibitory efficacy toward GCN5 and PCAF HAT activity (IC50 >100 µM). Shown to selectively prevents human & 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 22 µM; 72 h) in vitro without affecting the viability of Wnt-independent 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. 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.|
|Synonyms||HAT Inhibitor XII, Wnt Pathway Inhibitor XXII, (E) & (Z)-3-Chloro-2,3-bis(4-methoxyphenyl)acrylaldehyde, WD, Wnt inhibitor dorsalizing, Histone Acetyltransferase Inhibitor XII|
|References||Hao. J., et al. 2013 Cell Rep. 4, 898.|
|Structure formula Image|
|Primary Target||p300 HAT|
|Purity||≥98% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Hao. J., et al. 2013 Cell Rep. 4, 898.|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.