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Maritoclax

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Chemical Structure| 1227962-62-0 同义名 : Marinopyrrole-A;(±)-Marinopyrrole A
CAS号 : 1227962-62-0
货号 : A354912
分子式 : C22H12Cl4N2O4
纯度 : 97%
分子量 : 510.154
MDL号 : N/A
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(88.21 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Mcl-1
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-XL. 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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.80mL

1.96mL

0.98mL

19.60mL

3.92mL

1.96mL
参考文献

[1]Doi K, Li R, et al. Discovery of marinopyrrole A (maritoclax) as a selective Mcl-1 antagonist that overcomes ABT-737 resistance by binding to and targeting Mcl-1 for proteasomal degradation. J Biol Chem. 2012 Mar 23;287(13):10224-35.

[2]Eichhorn JM, Alford SE, et al. Purported Mcl-1 inhibitor marinopyrrole A fails to show selective cytotoxicity for Mcl-1-dependent cell lines. Cell Death Dis. 2013 Oct 24;4:e880.