PRT4165 E3 ubiquitin ligase inhibitor E3泛素连接酶抑制剂 31083-55-3

保存条件 ：零下20度

保质期 ：3年

英文名 ：PRT4165

库存 ：大量

供应商 ：上海惠诚生物科技有限公司

CAS号 ：31083-55-3

规格 ：10 mg/50 mg

PRT-4165 (31083-55-3) is an inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1). Inhibits self-ubiquitination (IC₅₀ = 3.9 μM) but does not increase cellular levels of either subunit. Blocks Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α.¹ PRT-4165 inhibits H2A/H2AX ubiquitination via blocking the E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex. Blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination in vitro and in vivo and as such represents a new tool for studying chromatin remodeling.²
PRT-4165(31083-55-3)是多梳抑制复合物1 (PRC1)亚基Bmi1/Ring1A的抑制剂。 抑制自身泛素化(IC50 = 3.9 μM)，但不增加细胞中任一亚基的水平。 阻断Bmi1/ ring1a介导的泛素化和药物诱导的拓扑异构酶2α 1降解 PRT-4165通过阻断RNF2和Bmi1/RNF2复合物的E3泛素连接酶活性来抑制H2A/H2AX泛素化。 体外和体内阻断多梳阻遏复合物(PRC) 1介导的组蛋白H2A泛素化，因此代表了研究染色质重塑的新工具 

References/Citations:

1) Alchanati et al. (2009), The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex – a potentially new drug target; PLoS One, 4 e8104
2) Ismail et al. (2013), A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks; J. Biol. Chem., 288 26944

CAS:
31083-55-3
Catalog Number:
10-1478
Activity:
E3 ubiquitin ligase inhibitor
Chemical Name:
2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione
Molecular Weight:
235.24
Molecular Formula:
C₁₅H₉NO₂
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 6 mg/ml with warming).
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT