Marinopyrrole A (Maritoclax)

Catalog No.S7126

Marinopyrrole A (Maritoclax) Chemical Structure

Molecular Weight(MW): 510.15

Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM.

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Biological Activity

Description Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM.
Targets
Mcl-1 [1]
()
In vitro

Maritoclax induces Mcl-1 degradation via the proteasome system, which is associated with the pro-apoptotic activity of maritoclax. Maritoclax selectively kills Mcl-1-dependent, but not Bcl-2- or Bcl-XL-dependent, leukemia cells and markedly enhances the efficacy of ABT-737 against hematologic malignancies, including K562, Raji, and multidrug-resistant HL60/VCR, by ∼60- to 2000-fold at 1-2 μM. Maritoclax blocks the interaction between a biotin-labeled Bim-BH3 peptide and GST-Mcl-1 in a dose-dependent manner with an IC50 value of 10.1 μM, while it does not inhibit the binding of Bim-BH3 peptide to GST-Bcl-XL at concentrations up to 80 μM. Maritoclax induces caspase-3 activation by degradation of Mcl-1 protein. Treatment with maritoclax markedly reduces the half-life of Mcl-1 to ∼0.5 h as compared with nearly 3 h in control cells. Maritoclax has no apparent effect on Mcl-1 (Ser159/Thr163) phosphorylation, suggesting that maritoclax induces phosphorylation-independent Mcl-1 degradation[1]. Marinopyrrole A has potent concentration-dependent bactericidal activity against clinically relevant hospital- and community-acquired MRSA strains. Marinopyrrole A shows limited toxicity to mammalian cell lines (at >20× MIC)[2]. Maritoclax sensitivity is cell type specific. It is not effective in HeLa, HEK293, or MEF cells. Maritoclax is not a substrate for p-gp mediated drug efflux[3].

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[3].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: K562 cells
  • Concentrations: 2 μM
  • Incubation Time: 12 h
  • Method:

    K562 cells expressing Mcl-1-IRES-BimEL are treated with DMSO, 2 μM maritoclax alone, or in combination with 1 μM MG132 for 12 h. Cells are lysed in 1% Chaps buffer (1% Chaps, 150 mM NaCl, 10 mM Hepes, pH7.4) containing protease inhibitors. Cell lysates containing 350 μg of protein are incubated with 4 μl of rabbit anti-Mcl-1 antiserum or control pre-immune serum in 250 μl of the same lysis buffer at 4 °C overnight on a rotator. Immunoprecipitates are collected by adding 20 μl of protein A-Sepharose beads for 3 h at 4 °C, followed by centrifugation at 6,000 rpm for 30 s. The beads are washed five times with the same lysis buffer, boiled for 5 min in Laemmli sample buffer and analyzed by Western blotting.


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: Female athymic nude (NCI Athymic NCr-nu/nu 01B74) mice
  • Formulation: PTD
  • Dosages: 20 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (196.02 mM)
Ethanol 45 mg/mL (88.2 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 510.15
Formula

C22H12Cl4N2O4

CAS No. 1227962-62-0
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID