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Marinopyrrole A (Maritoclax) 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). Maritoclax blocks the binding of Bim BH3 α-helix to Mcl-1 but not Bcl-XL. Maritoclax markedly inhibits the viability of Mcl-1-IRES-BimEL cells (EC50=1.6 μM) with a selectivity greater than 40-fold over Bcl-2-IRES-BimEL (EC50=65.1 μM) and Bcl-XL-IRES-BimEL (EC50=70.0 μM) cells. Maritoclax induces cell death selectively in Mcl-1-dependent but not Bcl-2- or Bcl-XL-dependent leukemia cells. Maritoclax induces proteasome-mediated Mcl-1 degradation without induction of Mcl-1 phosphorylation and Noxa expression. Maritoclax inhibits Mcl-1 interaction with Bim in intact cells and triggers cytochrome c release from isolated mitochondria. Maritoclax synergistically sensitizes lymphoma/leukemia cells to ABT-737. Marinopyrrole A (3 μM) induced-cell death is associated with MCL1 decrease and translation inhibition. Marinopyrrole A induces a dephosphorylation of EIF4EBP1 concomitant to a decrease of EIF4E phosphorylation.
In vivo, Maritoclax administration at 20 mg/kg/d intraperitoneally causes significant U937 tumor shrinkage, as well as 36% tumors remission rate in athymic nude mice, without apparent toxicity to healthy tissue or circulating blood cells.
| Molecular Weight | 510.15 |
| Formula | C22H12Cl4N2O4 |
| CAS Number | 1227962-62-0 |
| Solubility (25°C) | DMSO: ≥ 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Bcl-2 Products |
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| ABT-263
ABT-263 (Navitoclax) is a potent, orally bioavailable inhibitor of the antiapoptotic Bcl-2 family members Bcl-2, Bcl-x (L), and Bcl-w. |
| ABT-737
ABT-737 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins, in small cell lung cancer. |
| AT-101
AT-101 (R-(-)-gossypol acetic acid) is a pan small molecule inhibitor of Bcl-2, Bcl-xL, and Mcl-1. |
| ABT-199
ABT-199 (Venetoclax) is a highly potent, orally bioavailable and BCL-2 inhibitor. ABT-199 is the first inhibitor targeting Bcl-2 and PPI. |
| TW-37
TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively. |
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