Merck, 382115-10MG, Histone Acetyl Transferase Inhibitor VII, CTK7A

General description
A cell-permeable and water soluble hydrazinobenzoylcurcumin (HBC) compound that acts as a selective, reversible and mixed mode inhibitor of p300/CBP and PCAF histone acetyltransferases (IC₅₀ ≤ 25 and 50 µM, respectively) with minimal activity towards other histone modifying enzymes like, G9a, CARM1, HDAC1, SIRT2 and TIP60 (IC₅₀ >100 µM). Blocks the autoacetylation of p300 and PCAF and histone acetylation, downregulates cyclin E expression and induces senescence-like growth arrest at 100 µM in KB cells. Further, suppresses tumor growth in xenograft oral tumor nude mouse model (100 mg/kg, i.p., b.i.d.) and reduces H3K14 and H3K9 acetylation levels. Reported to potently inhibit bFGF-induced bovine aortic endothelial cells (BAECs) invasion and tube formation with an IC₅₀ of 0.93 µM and binds to Ca²⁺/calmodulin with high-affinity (Kd = 8.11 µM) and antagonize its functions in HCT15 cells.
Packaging
Packaged under inert gas
Other Notes
Arif, M., et al. 2010. Chem. Biol.17, 903.
Shim, J.S., et al. 2004. Chem. Biol.11, 1455.
Shim, J.S., et al. 2002. Bioorg. Med. Chem. Biol.10, 2439.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)