382115

Histone Acetyl Transferase Inhibitor VII, CTK7A

The Histone Acetyl Transferase Inhibitor VII, CTK7A controls the biological activity of Histone Acetyl Transferase. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonyme(s) : Histone Acetyl Transferase Inhibitor VII, CTK7A, HAT Inhibitor VII, p300/CBP Inhibitor V, PCAF Inhibitor III, Sodium-4-(3,5-bis(4-hydroxy-3-methoxystyryl)-1H-pyrazol-1-yl)benzoate, HBC, Na, Sodium-4-(3,5-bis(4-hydroxy-3-methoxystyryl)-1H-pyrazol-1-yl)benzoate, HBC, Na, HAT Inhibitor VII, p300/CBP Inhibitor V, PCAF Inhibitor III
• Formule empirique (notation de Hill): C₂₈H₂₃N₂NaO₆
• Poids moléculaire : 506.48
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.32

Propriétés

• Niveau de qualité: 100
• Pureté: ≥99% (HPLC)
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: tan
• Solubilité: DMSO: 100 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• Chaîne SMILES: OC1=CC=C(C=C1OC)/C=C/C2=CC(/C=C/C3=CC=C(O)C(OC)=C3)=NN2C4=CC=C(C=C4)C(O[Na])=O

Description

Description générale

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 (K_d = 8.11 µM) and antagonize its functions in HCT15 cells.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable