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Maritoclax (Synonyms: Marinopyrrole A)

Cat. No.: HY-15613 Purity: 99.97%
Handling Instructions

Maritoclax (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).

For research use only. We do not sell to patients.

Maritoclax Chemical Structure

Maritoclax Chemical Structure

CAS No. : 1227962-62-0

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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Maritoclax purchased from MCE. Usage Cited in: bioRxiv. 2020 May. 

    Maritoclax represses the anti-apoptotic proteins in a dose- and time-dependent manner.

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    • References

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    Description

    Maritoclax (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).

    IC50 & Target[1]

    Mcl-1

    10.1 μM (IC50)

    In Vitro

    Maritoclax (Marinopyrrole A) blocks the binding of Bim BH3 α-helix to Mcl-1 but not Bcl-XL. Maritoclax (Marinopyrrole A) 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 (Marinopyrrole A) induces cell death selectively in Mcl-1-dependent but not Bcl-2- or Bcl-XL-dependent leukemia cells. Maritoclax (Marinopyrrole A) induces proteasome-mediated Mcl-1 degradation without induction of Mcl-1 phosphorylation and Noxa expression. Maritoclax (Marinopyrrole A) inhibits Mcl-1 interaction with Bim in intact cells and triggers cytochrome c release from isolated mitochondria. Maritoclax (Marinopyrrole A) synergistically sensitizes lymphoma/leukemia cells to ABT-737[1]. Maritoclax (Marinopyrrole A) shows activity against all tested S. aureus strains, including glycopeptide-intermediate and vancomycin-resistant MRSA, and has potent activities against other Gram-positive organisms. In addition, Maritoclax (Marinopyrrole A) is active against H. influenzae but is inactive against other tested Gram-negative strains. Maritoclax (Marinopyrrole A) displays substantial concentration-dependent killing against MRSA strain TCH1516 and is far more rapid in its antibiotic action than either vancomycin or linezolid. Maritoclax exhibits a favorable therapeutic index, with 50% inhibitory concentrations (IC50) in excess of 20× above the MIC in each case: 32 to 64 μg/mL against HeLa cells and 8 to 32 μg/mL against L929 cells[2]. Maritoclax (Marinopyrrole A) (3 μM) induced-cell death is associated with MCL1 decrease and translation inhibition. Maritoclax (Marinopyrrole A) induces a dephosphorylation of EIF4EBP1 concomitant to a decrease of EIF4E phosphorylation[3]. Maritoclax (Marinopyrrole A) is much more effective against Bcl-2-dependent RS4;11 cells (IC50: 2 μM) when compared to Mcl-1-dependent HeLa cells (IC50: 20 μM)[4].

    Molecular Weight

    510.15

    Formula

    C₂₂H₁₂Cl₄N₂O₄

    CAS No.

    1227962-62-0

    SMILES

    OC1=CC=CC=C1C(C2=C(N3C(C(C4=CC=CC=C4O)=O)=CC(Cl)=C3Cl)C(Cl)=C(Cl)N2)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 43 mg/mL (84.29 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9602 mL 9.8010 mL 19.6021 mL
    5 mM 0.3920 mL 1.9602 mL 3.9204 mL
    10 mM 0.1960 mL 0.9801 mL 1.9602 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (4.90 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    Maritoclax (Marinopyrrole A) cytotoxicity is assessed by seeding 2×104 HeLa or L929 cells per well in sterile 96-well tissue culture-treated plates. After 24 h, the medium is replaced with fresh medium containing increasing concentrations of marinopyrrole A, and the plates are incubated at 37°C in 5% CO2 for 24 h. Cytotoxicity is assayed at 24 h by measuring the reduction of MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium] using the CellTiter 96 Aqueous nonradioactive cell proliferation assay according to the manufacturer's instructions.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.97%

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    Keywords:

    MaritoclaxMarinopyrrole ABcl-2 FamilyInhibitorinhibitorinhibit

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    Cat. No.:
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