84210-35-5
Chemical Structure
MK-4815
- CAS No.: 84210-35-5
- Formula:C15H25NO
- Molecular Weight:235.37
IUPAC Name: 2-(aminomethyl)-3,5-di-tert-butylphenol
InChIKey: ZUSLEOOZAITYGH-UHFFFAOYSA-N
SMILES: OC=1C=C(C=C(C1CN)C(C)(C)C)C(C)(C)C
Biological Activity: MK-4815 is an orally active small-molecule allosteric inhibitor of Falcilysin (FLN) with antimalarial activity. MK-4815 inhibits the viability of Plasmodium falciparum NF54 and Dd2 strains with IC50 values of 38 and 40 ng/mL, respectively. MK-4815 preferentially accumulates in erythrocytes containing mature trophozoite/schizont-stage parasites. MK-4815 preferentially binds to the partially closed conformation of FLN, shifting the FLN conformational equilibrium toward the partially closed state and restricting the hinge region-mediated transition from the partially closed state to the open state, thereby interfering with the catalytic cycle of FLN. MK-4815 can be used for malaria-related research[1][2].
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MK-4815 | MK-4815 is an orally active small-molecule allosteric inhibitor of Falcilysin (FLN) with antimalarial activity. MK-4815 inhibits the viability of Plasmodium falciparum NF54 and Dd2 strains with IC50 values of 38 and 40 ng/mL, respectively. MK-4815 preferentially accumulates in erythrocytes containing mature trophozoite/schizont-stage parasites. MK-4815 preferentially binds to the partially closed conformation of FLN, shifting the FLN conformational equilibrium toward the partially closed state and restricting the hinge region-mediated transition from the partially closed state to the open state, thereby interfering with the catalytic cycle of FLN. MK-4815 can be used for malaria-related research. | |||||||||||||||||||||
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References
- [1]. Powles MA, et al. MK-4815, a potential new oral agent for treatment of malaria. Antimicrobial agents and chemotherapy. 2012 May;56(5):2414-9. [Content Brief]
- [2]. Lin J, et al. Inhibition of falcilysin from Plasmodium falciparum by interference with its closed-to-open dynamic transition. Communications biology. 2024 Aug 31;7(1):1070.
