Product Details
| Product Name:
Maritoclax |
CAS No.:
1227962-62-0 |
| Purity:
99.87% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | Maritoclax |
| 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. |
| In vitro | Maritoclax (Marinopyrrole A) (3 μM) induces cell death associated with MCL1 decrease and translation inhibition. It dephosphorylates EIF4EBP1 while reducing EIF4E phosphorylation[3]. 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)[4]. 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[1]. 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[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 43 mg/mL (84.29 mM)
|
| Keywords | Inhibitor | Bcl-2 Family | inhibit | Maritoclax |
| Inhibitors Related | Gossypol (acetic acid) | (S)-(+)-Ibuprofen | Allethrin | Navitoclax | Docetaxel trihydrate | Gossypol | Triacetylresveratrol | Diphenyl disulfide | Lisaftoclax | Venetoclax | (E)-Ferulic acid | Thymoquinone |
| Related Compound Libraries | Cuproptosis Compound Library | Apoptosis Compound Library | Bioactive Compound Library | Hematonosis Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$38.00/1mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |
United States