For research use only. Not for therapeutic Use.
WR99210（Cat No.:I010084）is a potent dihydrofolate reductase (DHFR) inhibitor primarily used in malaria research, especially against Plasmodium species resistant to traditional antifolates. By targeting DHFR, WR99210 disrupts the folate pathway essential for parasite DNA synthesis and cell replication, effectively inhibiting parasite growth. Its efficacy against DHFR mutants makes it invaluable for studying drug-resistant malaria strains and exploring new antimalarial strategies. Beyond malaria, WR99210 is used in genetic engineering as a selectable marker in research involving DHFR gene mutations, contributing to advancements in parasitology and drug development.
| Catalog Number | I010084 |
| CAS Number | 47326-86-3 |
| Synonyms | WR99210; WR 99210; WR-99210;;1,6-Dihydro-6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,3,5-triazine-2,4-diamine |
| Molecular Formula | C14H18Cl3N5O2 |
| Purity | ≥95% |
| Target | Anti-infection |
| Solubility | Soluble in DMSO |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| IUPAC Name | 6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,3,5-triazine-2,4-diamine |
| InChI | InChI=1S/C14H18Cl3N5O2/c1-14(2)21-12(18)20-13(19)22(14)24-5-3-4-23-11-7-9(16)8(15)6-10(11)17/h6-7H,3-5H2,1-2H3,(H4,18,19,20,21) |
| InChIKey | MJZJYWCQPMNPRM-UHFFFAOYSA-N |
| SMILES | CC1(N=C(N=C(N1OCCCOC2=CC(=C(C=C2Cl)Cl)Cl)N)N)C |
| Reference | </br>1:Transfection of Babesia bovis by Double Selection with WR99210 and Blasticidin-S and Its Application for Functional Analysis of Thioredoxin Peroxidase-1. Asada M, Yahata K, Hakimi H, Yokoyama N, Igarashi I, Kaneko O, Suarez CE, Kawazu S.PLoS One. 2015 May 11;10(5):e0125993. doi: 10.1371/journal.pone.0125993. eCollection 2015. PMID: 25962142 Free PMC Article</br>2:Stable expression of green fluorescent protein and targeted disruption of thioredoxin peroxidase-1 gene in Babesia bovis with the WR99210/dhfr selection system. Asada M, Tanaka M, Goto Y, Yokoyama N, Inoue N, Kawazu S.Mol Biochem Parasitol. 2012 Feb;181(2):162-70. doi: 10.1016/j.molbiopara.2011.11.001. Epub 2011 Nov 15. PMID: 22108434 </br>3:Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination. Japrung D, Leartsakulpanich U, Chusacultanachai S, Yuthavong Y.Antimicrob Agents Chemother. 2007 Dec;51(12):4356-60. Epub 2007 Sep 17. PMID: 17875995 Free PMC Article</br>4:An amino acid substitution in the Babesia bovis dihydrofolate reductase-thymidylate synthase gene is correlated to cross-resistance against pyrimethamine and WR99210. Gaffar FR, Wilschut K, Franssen FF, de Vries E.Mol Biochem Parasitol. 2004 Feb;133(2):209-19. PMID: 14698433 </br>5:Novel Saccharomyces cerevisiae screen identifies WR99210 analogues that inhibit Mycobacterium tuberculosis dihydrofolate reductase. Gerum AB, Ulmer JE, Jacobus DP, Jensen NP, Sherman DR, Sibley CH.Antimicrob Agents Chemother. 2002 Nov;46(11):3362-9. PMID: 12384337 Free PMC Article</br>6:Pyrimethamine and WR99210 exert opposing selection on dihydrofolate reductase from Plasmodium vivax. Hastings MD, Sibley CH.Proc Natl Acad Sci U S A. 2002 Oct 1;99(20):13137-41. Epub 2002 Aug 27. PMID: 12198181 Free PMC Article</br>7:Novel alleles of the Plasmodium falciparum dhfr highly resistant to pyrimethamine and chlorcycloguanil, but not WR99210. Hankins EG, Warhurst DC, Sibley CH.Mol Biochem Parasitol. 2001 Sep 28;117(1):91-102. PMID: 11551635 </br>8:Mutagenesis of dihydrofolate reductase from Plasmodium falciparum: analysis in Saccharomyces cerevisiae of triple mutant alleles resistant to pyrimethamine or WR99210. Ferlan JT, Mookherjee S, Okezie IN, Fulgence L, Sibley CH.Mol Biochem Parasitol. 2001 Mar;113(1):139-50. PMID: 11254962 </br>9:Interaction of pyrimethamine, cycloguanil, WR99210 and their analogues with Plasmodium falciparum dihydrofolate reductase: structural basis of antifolate resistance. Rastelli G, Sirawaraporn W, Sompornpisut P, Vilaivan T, Kamchonwongpaisan S, Quarrell R, Lowe G, Thebtaranonth Y, Yuthavong Y.Bioorg Med Chem. 2000 May;8(5):1117-28. PMID: 10882022 </br>10:The antimalarial triazine WR99210 and the prodrug PS-15: folate reversal of in vitro activity against Plasmodium falciparum and a non-antifolate mode of action of the prodrug. Kinyanjui SM, Mberu EK, Winstanley PA, Jacobus DP, Watkins WM.Am J Trop Med Hyg. 1999 Jun;60(6):943-7. PMID: 10403325 |
