Marinopyrrole A (Synonyms: Marinopyrrole A) |
| Catalog No.GC15480 |
Marinopyrrole A (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
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Cas No.: 1227962-62-0
Sample solution is provided at 25 µL, 10mM.
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Marinopyrrole A is a selective inhibitor of Mcl-1 with IC50 value of 10.1μM [1].
Marinopyrrole A is a natural product froma species of marine-derived streptomycetes and is reported to be an antagonist of Mcl-1. Mcl-1 is a member of the anti-apoptotic Bcl-2 family, which is a well-validated drug target for cancer treatment. NMR titration experiments show that Marinopyrrole A can directly interact with Mcl-1. It can prevent Bim-BH3 peptides from binding to Mcl-1 but not Bcl-XL. The cell based assay shows a high selectivity of Marinopyrrole A. Treatment with Marinopyrrole A inhibit the viability of K562 cells transfected with Mcl-1 gene with EC50 value of 1.6μM. The selectivity is more than 40-fold greater over the cells transfected with Bcl-XL gene. Moreover, Marinopyrrole A can decreases Mcl-1 expression by increasing the cleavage of caspase-3 and PARP. Marinopyrrole A is also reported to completely restore the sensitivity of multidrug resistant leukemia cells to ABT-737 [1].
References:
[1] Doi K, Li R, Sung SS, 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, 287(13): 10224-35.
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