产品
编 号:F754797
分子式:C29H34ClN3O3
分子量:508.05
产品类型
结构图
CAS No: 2705545-47-5
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产品详情
生物活性:
TCMDC-135051 hydrochloride is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 hydrochloride prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 hydrochloride has antiparasiticidal activity (EC50=320 nM).
体外研究:
TCMDC-135051 hydrochloride shows potent activity against P. berghei sporozoites in a liver invasion and development assay in which the compound shows a pEC50 value of 6.17 (EC50=0.40 μM). The kinase assays using recombinant PvCLK3 (P. vivax) and PbCLK3 (P. berghei) show that TCMDC-135051 hydrochloride has near-equipotent inhibition at these two orthologs, with pIC50 values of 7.47 (IC50=0.033 μM) and 7.86 (IC50=0.013 μM), respectively.