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Marinopyrrole A (Maritoclax) Bcl-2 antagonist

Name: Marinopyrrole A (Maritoclax)
Brand: Selleck Chemicals
SKU: S7126
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S7126

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

Chemical Structure

Molecular Weight: 510.15

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Quality Control

Batch: Purity: 99.66%

99.66

Related Targets	Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Other Bcl-2 Inhibitors	Navitoclax (ABT-263) S63845 ABT-737 Obatoclax Mesylate (GX15-070) A-1331852 A-1210477 TW-37 A-1155463 Dihydrochloride AZD5991 UMI-77

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (196.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	510.15	Formula	C₂₂H₁₂Cl₄N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1227962-62-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C(C(=C1)C(=O)C2=CC(=C(N2C3=C(NC(=C3Cl)Cl)C(=O)C4=CC=CC=C4O)Cl)Cl)O

Mechanism of Action

Targets/IC₅₀/Ki	Mcl-1
In vitro	Maritoclax induces Mcl-1 degradation via the proteasome system, which is associated with its pro-apoptotic activity. It 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. This compound 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 it markedly reduces the half-life of Mcl-1 to ∼0.5 h as compared with nearly 3 h in control cells. It has no apparent effect on Mcl-1 (Ser159/Thr163) phosphorylation, suggesting that it induces phosphorylation-independent Mcl-1 degradation. Marinopyrrole A has potent concentration-dependent bactericidal activity against clinically relevant hospital- and community-acquired MRSA strains. It shows limited toxicity to mammalian cell lines (at >20× MIC). Its sensitivity is cell type specific. It is not effective in HeLa, HEK293, or MEF cells. This compound is not a substrate for p-gp mediated drug efflux.
In vivo	Marinopyrrole A (Maritoclax) administration at 20 mg/kg/d intraperitoneally causes significant U937 tumor shrinkage, as well as a 36% tumor remission rate in athymic nude mice, without apparent toxicity to healthy tissue or circulating blood cells.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22311987/ [2] https://pubmed.ncbi.nlm.nih.gov/21502631/ [3] https://pubmed.ncbi.nlm.nih.gov/24842334/

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