Marinopyrrole A
Marinopyrrole A is a selective inhibitor of Mcl-1 with IC50 value of 10.1μM [1].
Marinopyrrole A is a natural product froma species of marine-derived streptomycetes and is reported to be an antagonist of Mcl-1. Mcl-1 is a member of the anti-apoptotic Bcl-2 family, which is a well-validated drug target for cancer treatment. NMR titration experiments show that Marinopyrrole A can directly interact with Mcl-1. It can prevent Bim-BH3 peptides from binding to Mcl-1 but not Bcl-XL. The cell based assay shows a high selectivity of Marinopyrrole A. Treatment with Marinopyrrole A inhibit the viability of K562 cells transfected with Mcl-1 gene with EC50 value of 1.6μM. The selectivity is more than 40-fold greater over the cells transfected with Bcl-XL gene. Moreover, Marinopyrrole A can decreases Mcl-1 expression by increasing the cleavage of caspase-3 and PARP. Marinopyrrole A is also reported to completely restore the sensitivity of multidrug resistant leukemia cells to ABT-737 [1].
References:
[1] Doi K, Li R, Sung SS, 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, 287(13): 10224-35.
Storage | Store at -20°C |
M.Wt | 510.15 |
Cas No. | 1227962-62-0 |
Formula | C22H12Cl4N2O4 |
Solubility | Soluble in DMSO |
SDF | Download SDF |
Canonical SMILES | OC1=CC=CC=C1C(C2=C(N3C(C(C4=CC=CC=C4O)=O)=CC(Cl)=C3Cl)C(Cl)=C(Cl)N2)=O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | Marinopyrrole A is a selective inhibitor of Mcl-1 with IC50 value of 10.1 μM . | |||||
Targets | Mcl-1 | |||||
IC50 | 10.1 μM |
Quality Control & MSDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
