货号：A354912同义名：
Marinopyrrole-A;(±)-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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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
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]
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