基本信息

产品描述

PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.

靶点（IC50 & Targe）

BMI-1,

Ring1A

体外研究

PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation in vivo and in vitro. It inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks (DSBs), the retention of several DNA damage response proteins in foci that form around DSBs, and the repair of the DSBs. PRT4165 inhibits both RNF2 and RING 1A, which are partially redundant paralogues that together account for the E3 ubiquitin ligase activity found in PRC1 complexes, but not RNF8 nor RNF168. U2OS cells treated with increasing concentrations of PRT4165 show increasing numbers of cells in G2/M[2].

细胞实验

Cell lines: HeLa cells

Concentrations: 50 μM

Incubation Time: 5 h

Method: HeLa cells are transfected with Bmi1-FLAG, Ring1A and HA-ubiquitin. Twenty-four hours post transfection the cells are treated with either solvent (0.5% DMSO, 0.5% PEG400) or 50 μM PRT4165 for 5 hours. Bmi1-FLAG is immunoprecipitated from cell lysates, and conjugated ubiquitin is detected by Western-blot with anti-HA antibody.

(Only for Reference)

动物实验

Animal Models: CD-1 mice

Formulation: sesame oil containing 10% ethanol

Dosages: 4 mg/kg and 8 mg/kg

Administration: intraluminally injection

(Only for Reference)

参考文献

[1] Alchanati I, et al. PLoS One. 2009, 4(12):e8104.

[2] Ismail IH, et al. J Biol Chem. 2013, 288(37):26944-54.

[3] Fenghua Bian, et al. Sci Rep. 2016, 6: 26061.

产品说明

其他说明

Please note that sigma-aldrich provides this product to early discovery researchers as part of a collection of unique chemicals. sigma-aldrich does not collect analytical data for this product. Buyer assumes responsibility to confirm product identity and/or purity. All sales are final.
NOTWITHSTANDING ANY CONTRARY PROVISION CONTAINED IN SIGMA-ALDRICH′S STANDARD TERMS AND CONDITIONS OF SALE OR AN AGREEMENT BETWEEN SIGMA-ALDRICH AND BUYER, SIGMA-ALDRICH SELLS THIS PRODUCT "AS-IS" AND MAKES NO REPRESENTATION OR WARRANTY WHATSOEVER WITH RESPECT TO THIS PRODUCT, INCLUDING ANY (A) WARRANTY OF MERCHANTABILITY, (B) WARRANTY OF FITNESS FOR A PARTICULAR PURPOSE, OR (C) WARRANTY AGAINST INFRINGEMENT OF INTELLECTUAL PROPERTY RIGHTS OF A THIRD PARTY, WHETHER ARISING BY LAW, COURSE OF DEALING, COURSE OF PERFORMANCE, USAGE OF TRADE OR OTHERWISE.

基本信息

产品性质

安全信息

象形图
警示用语：	Warning
危险声明	H317
预防措施声明	P280
危险分类	Skin Sens. 1
储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

产品说明

生化/生理作用

PRT4165 is a potent inhibitor of PRC1 (polycomb-repressive complex 1)-mediated histone H2A ubiquitylation in vivo and in vitro. PRT4165 inhibits the in vitro histone H2A E3 ubiquitin ligase activity of PRC1 components RING1, RNF2, and a BMI1/RNF2 complex. PRT4165 also inhibits DNA double-strand breaks induced ubiquitylation of histone H2AX.

特点和优势

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基本信息

产品性质

安全信息

基本信息