[CAS NO. 328968-36-1]  C646

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PRODUCTS SPECIFICATIONS [328968-36-1]

Store
Catalog
SLK-S7152
Brand
Selleck
CAS
328968-36-1

DESCRIPTION [328968-36-1]

Overview

MDLMFCD01784780
Molecular Weight445.42
Molecular FormulaC24H19N3O6
SMILESN(=O)(=O)C1=C(C=C(C)C(C)=C1)C=2OC(C=C3C(=O)N(N=C3C)C4=CC=C(C(O)=O)C=C4)=CC2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.2451 mL11.2254 mL22.4507 mL
5 mM0.4490 mL2.2451 mL4.4901 mL
10 mM0.2245 mL1.1225 mL2.2451 mL
50 mM---

Description

C646 is an inhibitor for , and inhibits with a of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, and .

Features

Extensively used as a pharmacologic probe in cancer cells. Potential use for prostate and lung cancers.

Targets

p300/CBP [1]
(Cell-free assay)
400 nM(Ki)

In vitro

C646 is an inhibitor for histone acetyltransferase, inhibits p300 with a K of 400 nM and is selective versus other acetyltransferases. C646 produces 86% inhibition of p300 in vitro at 10 μM. C646 is a classical reversible p300 inhibitor. C646 treatment (25μM) reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. C646 (20μM) induces apoptosis in androgen-sensitive and castration-resistant prostate cancer cell lines by interfering with AR and NF-kB pathways. C646 blocks dynamic acetylation of H3K4me3 globally in mouse and fly cells, and locally across the promoter and start-site of inducible genes in the mouse, thereby disrupting RNA polymerase II association and the activation of these genes.

In vivo

C646 infused into the ILPFC immediately after weak extinction training enhances the consolidation of fear extinction memory. C646 attenuates mechanical allodynia and thermal hyperalgesia, accompanied by a suppressed COX-2 expression, in the spinal cord.


Synonyms

Benzoic acid, 4-[4-[[5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]-
4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]benzoic acid
C 646