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Merck

SML0002

C646

≥98% (HPLC), p300/CBP histone acetyltransferase inhibitor, powder

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C24H19N3O6
CAS Number:
Molecular Weight:
445.42
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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Product Name

C646, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

red to brown

solubility

DMSO: >25 mg/mL

storage temp.

2-8°C

SMILES string

Cc1cc(-c2ccc(\C=C3\C(C)=NN(c4ccc(cc4)C(O)=O)C3=O)o2)c(cc1C)[N+]([O-])=O

InChI

1S/C24H19N3O6/c1-13-10-20(21(27(31)32)11-14(13)2)22-9-8-18(33-22)12-19-15(3)25-26(23(19)28)17-6-4-16(5-7-17)24(29)30/h4-12H,1-3H3,(H,29,30)/b19-12-

InChI key

HEKJYZZSCQBJGB-UNOMPAQXSA-N

Application

C646 was used to study the role of p300 in chronic neuropathic pain in rats with chronic constriction injury.

Biochem/physiol Actions

C646 is a competitive histone acetyltransferase (HAT) p300/CBP inhibitor with a Ki of 400 nM and is selective versus other acetyltransferases.
C646 is a potent, cell permeable and selective inhibitor of p300 and CBP (p300/CBP) histone acetyltransferases. Inhibition of p300/CBP by C646 affects the activity of a variety of transcriptional factors such as NF-κB, p53 and MyoD that are associated with physiology, disease processes, hippocampal synaptic plasticity, spatial memory and contextual fear.
C646 is a potent, competitive, and selective histone acetyltransferase (HAT) p300/CBP inhibitor.

Features and Benefits

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.


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Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Articles

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

Related Content

당사는 유전자 조절 연구 분야에서 표적 식별 및 검증을 위해 전사 인자 조절인자, 염색질 변형 효소 억제제, 작용제/길항제와 같은 여러 저분자 연구 툴을 제공합니다. 이러한 연구 툴 제품군은 아래에 나와 있습니다.


Jia Cao et al.
Nature communications, 8(1), 131-131 (2017-07-27)
Diabetes and obesity are characterized by insulin resistance and chronic low-grade inflammation. An elevated plasma concentration of lipopolysaccharide (LPS) caused by increased intestinal permeability during diet-induced obesity promotes insulin resistance in mice. Here, we show that LPS induces endoplasmic reticulum
Veronica Garcia-Carpizo et al.
Epigenetics & chromatin, 11(1), 30-30 (2018-06-10)
The reported antitumor activity of the BET family bromodomain inhibitors has prompted the development of inhibitors against other bromodomains. However, the human genome encodes more than 60 different bromodomains and most of them remain unexplored. We report that the bromodomains
Xiao-Yan Zhu et al.
Molecular pain, 8, 84-84 (2012-11-28)
Neuropathic pain is detrimental to human health; however, its pathogenesis still remains largely unknown. Overexpression of pain-associated genes and increased nociceptive somato-sensitivity are well observed in neuropathic pain. The importance of epigenetic mechanisms in regulating the expression of pro- or