CAS:1227962-62-0Marinopyrrole A

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Synonyms: Maritoclax;(±)-Marinopyrrole A

Marinopyrrole A is a selective Mcl-1 inhibitor with IC50 of 10.1 μM and proapoptosis properties in some cancer cells.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1227962-62-0

储存条件

分子式

C22H12Cl4N2O4

运输

蓝冰

分子量

510.15

别名

Maritoclax;(±)-Marinopyrrole A

溶解度

DMSO	160.0 mg/mL (313.6 mM)
Water	280.0 mg/mL (548.9 mM)

动物实验配方

生物活性

描述Maritoclax is a selective Mcl-1 inhibitor with IC50 value of 10.1μM against the binding of a biotinylated Bim BH3 peptide to Mcl-1 protein, but with IC50 value>80μM for Bcl-X_L. Maritoclax induced cell death with EC50 value of 1.6μM in K562 cells retrovirally transduced Mcl-1-IRES-BimEL and also exhibited anti-proliferation against primary large-granular lymphocyte leukemia (LGLL) cells with EC50 values ranging in 4.64-40μM correlated to the Mcl-1 level. Maritoclax at dose ranging in 1.5-2.5μM induced proteasome-mediated Mcl-1 degradation in Mcl-1-IRES-BimEL K562 cells at 12h post treatment, without induction of Mcl-1 phosphorylation and Noxa expression. Maritoclax, at concentration of 2 or 2.5μM, synergistically sensitized lymphoma/leukemia K562 cells and Raji cells to ABT-737, respectively, at 24h post treatment^[1]. Also Maritoclax could exhibited cytotoxicity in Mcl-1-independent manner in cells such as RS4;11 human leukemia cell line which have previously been shown to be dependent on Bcl-2 for survival^[2].
作用机制Maritoclax blocks the binding of Bim BH3 α-helix to Mcl-1 and induces Mcl-1 degradation, thereby leading to Mcl-1-dependent apoptosis.^[1]
动物研究
剂量
Nude Mice^[3] (i.p.): 20 mg/kg

给药途径
i.p.