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Maritoclax

Catalog No. T11944 CAS 1227962-62-0

Synonyms: Marinopyrrole A

Maritoclax (Marinopyrrole A) (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor, shows <8 fold selectivity than BCL-xl (IC50 < 80 μM),with an IC50 value of 10.1 μM.

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Maritoclax, CAS 1227962-62-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 293.00
50 mg	In stock	$ 547.00
100 mg	In stock	$ 763.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 97.70%

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Description	Maritoclax (Marinopyrrole A) (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor, shows >8 fold selectivity than BCL-xl (IC50 > 80 μM),with an IC50 value of 10.1 μM.
Targets&IC50	MCL1:10.1 μM
In vitro	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].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].

Synonyms	Marinopyrrole A
Molecular Weight	510.15
Formula	C22H12Cl4N2O4
CAS No.	1227962-62-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 43 mg/mL (84.29 mM)

References and Literature

1. Doi K, et al. 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. J Biol Chem. 2012 Mar 23;287(13):10224-35. 2. Haste NM, et al. Pharmacological properties of the marine natural product marinopyrrole A against methicillin-resistant Staphylococcus aureus. Antimicrob Agents Chemother. 2011 Jul;55(7):3305-12. 3. Gomez-Bougie P, et al. The selectivity of Marinopyrrole A to induce apoptosis in MCL1high BCL2low expressing myeloma cells is related to its ability to impair protein translation. Br J Haematol. 2016 Aug 14. 4. Eichhorn JM, et al. Purported Mcl-1 inhibitor marinopyrrole A fails to show selective cytotoxicity for Mcl-1-dependent cell lines. Cell Death Dis. 2013 Oct 24;4:e880

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Hematonosis Compound Library Anti-Cancer Compound Library Cuproptosis Compound Library Covalent Inhibitor Library Apoptosis Compound Library Mitochondria-Targeted Compound Library PPI Inhibitor Library

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Keywords

Maritoclax 1227962-62-0 Apoptosis BCL Inhibitor Bcl-2 Family inhibit Marinopyrrole A inhibitor

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