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5.05298

p300/CBP Inhibitor VI, L002

Name: p300/CBP Inhibitor VI, L002
Brand: MM

Synonym(s):

p300/CBP Inhibitor VI, L002, 4-(4-Methoxyphenylsulfonyloxyimino)-2,6-dimethyl-2,5-cyclohexadien-1-one, GCN5 Inhibitor III, Histone Acetyltransferase Inhibitor IX, PCAF Inhibitor IV

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About This Item

Empirical Formula (Hill Notation):

C₁₅H₁₅NO₅S

CAS Number:

321695-57-2

Molecular Weight:

321.35

MDL number:

MFCD00720402

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥99% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Properties

assay

≥99% (HPLC)

Quality Level

100

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

brown

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

SMILES string

[S](=O)(=O)(ON=C2C=C(C(=O)C(=C2)C)C)c1ccc(cc1)OC

InChI

1S/C15H15NO5S/c1-10-8-12(9-11(2)15(10)17)16-21-22(18,19)14-6-4-13(20-3)5-7-14/h4-9H,1-3H3

InChI key

VEWFTYOFWIXCIO-UHFFFAOYSA-N

Description

General description

A cell-permeable phenylsulfonyloxyiminocyclohexadienone compound that acts as a potent, selective, and reversible inhibitor of p300 histone acetyl transferase (IC₅₀ = 1.98 µM). Shown to occupy Ac-CoA binding pocket of p300, and less potent to CBP, PCAF, GCN5 and GNAT. Suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. Does neither inhibit the activities of histone deacetylases 1, 6, and 11 nor 8-diverse histone methyltransferases tested (DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2). Reported to suppress tumor growth in mice bearing tumor xenografts of MDAMB-468 cell line (at 500 µg/100 µl, i.p. twice a week).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
p300 HAT

Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Use only fresh DMSO for reconstitution.

Other Notes

Yang, H., et al. 2013. Mol. Cancer Ther.12, 610.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c