Maritoclax

SKU: orb1309448

Description

Maritoclax

Research Area

Cell Biology

Key Properties

• CAS Number: 1227962-62-0
• MW: 510.15
• Purity: 99.87% (May vary between batches)
• Formula: C₂₂H₁₂Cl₄N₂O₄
• SMILES: Oc1ccccc1C(=O)c1[nH]c(Cl)c(Cl)c1-n1c(Cl)c(Cl)cc1C(=O)c1ccccc1O
• Target: Bcl-2 Family
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.92 mM);DMSO:43 mg/mL (84.29 mM)

Bioactivity

• Target IC50:
  MCL1:10.1 μM
• In Vitro:
  Maritoclax (Marinopyrrole A) (3 µM) induces cell death associated with MCL1 decrease and translation inhibition. It dephosphorylates EIF4EBP1 while reducing EIF4E phosphorylation. Maritoclax is significantly more effective against Bcl-2-dependent RS4;11 cells (IC50: 2 µM) compared to Mcl-1-dependent HeLa cells (IC50: 20 µM). It blocks Bim BH3 α-helix binding to Mcl-1 but not Bcl-XL, and markedly inhibits the viability of Mcl-1-IRES-BimEL cells (EC50=1.6 µM) with over 40-fold selectivity compared to Bcl-2-IRES-BimEL (EC50=65.1 µM) and Bcl-XL-IRES-BimEL (EC50=70.0 µM) cells. Maritoclax selectively induces cell death in Mcl-1-dependent leukemia cells and causes proteasome-mediated Mcl-1 degradation without inducing Mcl-1 phosphorylation or Noxa expression. It inhibits Mcl-1 interaction with Bim in intact cells, triggers cytochrome c release from isolated mitochondria, and synergistically sensitizes lymphoma/leukemia cells to ABT-737. Maritoclax is active against all tested S. aureus strains, including glycopeptide-intermediate and vancomycin-resistant MRSA, and has potent activity against other Gram-positive organisms, and H. influenzae but is inactive against tested Gram-negative strains. It shows substantial concentration-dependent killing against MRSA strain TCH1516 and acts more rapidly than vancomycin or linezolid. Maritoclax exhibits a favorable therapeutic index with IC50 values exceeding 20× above the MIC: 32–64 µg/mL against HeLa cells and 8–32 µg/mL against L929 cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bcl-2 Family, Maritoclax, Marinopyrrole A, Mcl-1, Inhibitor, inhibit

Compound Identifiers

PubChem CID

24797083