DSM1

A cell-permeable triazolopyrimidine compound that potently inhibits malaria parasite Plasmodium falciparum dihydroorotate dehydrogenase- (PfDHODH-) catalyzed electron transfer from FMNH₂ to Coenzyme Q₁₀ (CoQ or ubiquinone) in a potent (IC₅₀ = 47 nM), CoQ-competitive (K_i = 15 nM), and species-specific manner, without affecting PfDHODH-catalyzed electron transfer from DHO to FMN or the enzymatic activity of human DHODH (<5% inhibition at 100 µM). Reported to inhibit the proliferation of P. falciparum parasites (EC₅₀ = 79 nM against 3D7 strain) in vitro, including the drug-resistant strain Dd2 (EC₅₀ = 140 nM), while displaying no inhibitory potency against murine lymphocytic leukemia cell line L1210 even at concentrations as high as 10 µM. DSM1 is not recommended for in vivo use due to reduced plasma exposure upon repeat dosing in mice.

DHODH Inhibitor, DSM1, is a highly potent, competitive, tight-binding inhibitor of Plasmodium falciparum dihydroorotate dehydrogenase (IC₅₀ = 47 nM; K_i = 15 nM).

Cell permeable: yes

Primary Target
Pf*DHODH

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Guler, J.L., et al. 2013. PLoS Pathog.9, e1003375.

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CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)