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382115

Sigma-Aldrich

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.

Synonym(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

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About This Item

Empirical Formula (Hill Notation):
C28H23N2NaO6
Molecular Weight:
506.48
UNSPSC Code:
12352200
NACRES:
NA.32

Quality Level

100

Assay

≥99% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

tan

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

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

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

Warning

Toxicity: Standard Handling (A)

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

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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