CBL0137 (hydrochloride)

CBL0137 (hydrochloride)CAS号: 1197397-89-9分子式: C21H24N2O2 • HCl分子量: 372.9描述纯度储存/保存方法别名参考文献

产品描述
描述
Curaxins are small molecules that simultaneously activate p53 and inhibit NF-κB without causing detectable genotoxicity.1 CBL0137 is a water soluble and metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 value of 0.47 µM.1 It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-κB and promoting cancer cell death.1 CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Item No. 11690) in preclinical models of pancreatic cancer.1,2
纯度
≥98%
储存/保存方法
Store at -20℃
基本信息
别名
CBLC137;Curaxin 137;
参考文献
参考文献
1.Gasparian, A.V.,Burkhart, C.A.,Purmal, A.A., et al. Curaxins: Anticancer compounds that simultaneously suppress NF-κB and activate p53 by targeting FACT. Sci.Transl.Med. 3(95), (2011).

2.Burkhart, C.,Fleyshman, D.,Kohrn, R., et al. Curaxin CBL0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer. Oncotarget 5(22), 11038-11053 (2014).

分子结构图

CBL0137 (hydrochloride)