211816-91-0
Chemical Structure
CGP 40215
- CAS No.: 211816-91-0
- Formula:C17H19N9
- Molecular Weight:349.39
IUPAC Name: 8-(2-(4-benzhydrylpiperazin-1-yl)ethyl)-3-isobutyl-1-methyl-3,7-dihydro-1H-purine-2,6-dione
InChIKey: NSHBIZYDZBQOQB-WDBPGAOMSA-N
SMILES: N=C(C1=CC(/C=N/NC(N/N=C/C2=CC=CC(C(N)=N)=C2)=N)=CC=C1)N
Biological Activity: CGP 40215 is an S-adenosylmethionine decarboxylase inhibitor with an IC50 of 20.3 μM against Trypanosoma brucei brucei AdoMet decarboxylase. CGP 40215 blocks spermidine production and leads to putrescine accumulation. CGP 40215 inhibits polyamine biosynthesis in intact trypanosomes, acts synergistically with the ornithine decarboxylase inhibitor DFMO (HY-B0744) against CNS model infections, and ameliorates laboratory infections caused by multiple Trypanosoma brucei subspecies and Trypanosoma congolense isolates, including strains tolerant to standard trypanocides. CGP 40215 can be used for research on African trypanosomiasis and Chagas disease[1][2][3].
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CGP 40215 | CGP 40215 is an S-adenosylmethionine decarboxylase inhibitor with an IC50 of 20.3 μM against Trypanosoma brucei brucei AdoMet decarboxylase. CGP 40215 blocks spermidine production and leads to putrescine accumulation. CGP 40215 inhibits polyamine biosynthesis in intact trypanosomes, acts synergistically with the ornithine decarboxylase inhibitor DFMO (HY-B0744) against CNS model infections, and ameliorates laboratory infections caused by multiple Trypanosoma brucei subspecies and Trypanosoma congolense isolates, including strains tolerant to standard trypanocides. CGP 40215 can be used for research on African trypanosomiasis and Chagas disease. | |||||||||||||||||||||
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References
- [1]. Bacchi CJ, et al. In vivo trypanocidal activities of new S-adenosylmethionine decarboxylase inhibitors. Antimicrobial agents and chemotherapy. 1996 Jun;40(6):1448-53.
- [2]. Volkov OA, et al. Relief of autoinhibition by conformational switch explains enzyme activation by a catalytically dead paralog. eLife. 2016 Dec 15;5:e20198.
- [3]. Beswick TC, et al. Mechanisms of allosteric regulation of Trypanosoma cruzi S-adenosylmethionine decarboxylase. Biochemistry. 2006 Jun 27;45(25):7797-807.
