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Marinopyrrole A

Cat. No. M9095
Marinopyrrole A Structure
Synonym:

Maritoclax; (±)-Marinopyrrole

Size Price Availability Quantity
5mg USD 117 In stock
10mg USD 205 In stock
25mg USD 385 In stock
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Quality Control
  • Current batch:
  • Purity >97%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 510.15
Formula C22H12Cl4N2O4
CAS Number 1227962-62-0
Purity >97%
Solubility DMSO: ≥ 45 mg/mL
Storage at -20°C
References

Maritoclax induces apoptosis in acute myeloid leukemia cells with elevated Mcl-1 expression.
Doi K, et al. Cancer Biol Ther. 2014 Aug;15(8):1077-86. PMID: 24842334.

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.
Doi K, et al. J Biol Chem. 2012 Mar 23;287(13):10224-35. PMID: 22311987.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Marinopyrrole A, Maritoclax; (±)-Marinopyrrole supplier, Bcl-2, inhibitors

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