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PFI-4,≥98% (HPLC)

别名:PF-05363047, N-(1,3-Dimethyl-2-oxo-6-pyrrolidin-1-ylbenzimidazol-5-yl)-2-methoxybenzamide, N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxy-benzamide

Empirical Formula (Hill Notation): C21H24N4O3 CAS号: 900305-37-5 分子量: 380.44 PubChem化学物质编号: 329823828 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): PZ0307
CAS号: 900305-37-5
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$233.74

说明

包装

5, 25 mg in glass bottle
 

生化/生理作用

PFI-4 is an SGC chemical probe for the bromodomains of the BRPF (BRomodomain and PHD Finger containing) scaffolding protein BRPF1B. The BRPF proteins (BRPF1/2/3) assemble histone acetyltransferase (HAT) complexes of the MYST transcriptional coactivator family members MOZ and MORF. The BRPF1 protein is the scaffold subunit of the MYST acetyltransferase complex, which plays a crucial roles in DNA repair, recombination and replication as well as transcription activation. Mutations in MOZ, MORF, and BRPF1 have all been associated with cancer. BRPF1 exists in 2 different isoforms: BRPF1A and BRPF1B. PFI-4 specifically binds to BRPF1B with a Kd =13 nM as determined by ITC. It reduces recovery time in triple BRD cell construct in FRAP and is potent in cells with IC50 250nM, while showing no effect on BRPF1A. For full characterization details, please visit the PFI-4 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
PFI-4 是一种 SGC 化学探针,用于 BRPF(含 BRomodomain 和 PHD Finger)支架蛋白 BRPF1B 的溴结构域。 BRPF 蛋白 (BRPF1/2/3) 组装 MYST 转录共激活因子家族成员 MOZ 和 MORF 的组蛋白乙酰转移酶 (HAT) 复合物。 BRPF1 蛋白是 MYST 乙酰转移酶复合物的支架亚基,在 DNA 修复、重组和复制以及转录激活中起着至关重要的作用。 MOZ、MORF 和 BRPF1 的突变都与癌症有关。 BRPF1 存在两种不同的异构体:BRPF1A 和 BRPF1B。 PFI-4 与 BRPF1B 特异性结合,由 ITC 确定,Kd = 13 nM。 它减少了 FRAP 中三重 BRD 细胞构建体的恢复时间,并且在 IC50 为 250nM 的细胞中有效,同时对 BRPF1A 没有影响。 
 

特点和优势

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.
PFI-4 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
 

其他说明

This compound was developed by Pfizer for Gene Regulation research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
 

法律信息

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.
 

属性

质量水平

100

测定

≥98% (HPLC)

形式

powder

mfr. no.

Pfizer®

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear (warmed)

创始人

Pfizer

储存温度

room temp

SMILES string

CN(C1=CC(NC(C2=C(OC)C=CC=C2)=O)=C(N3CCCC3)C=C1N4C)C4=O

InChI

1S/C21H24N4O3/c1-23-17-12-15(22-20(26)14-8-4-5-9-19(14)28-3)16(25-10-6-7-11-25)13-18(17)24(2)21(23)27/h4-5,8-9,12-13H,6-7,10-11H2,1-3H3,(H,22,26)

InChI key

QCIJLRJBZDBVDB-UHFFFAOYSA-N

 

安全信息

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.常温阴凉避光
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16