1. Anti-infection
  2. Parasite
  3. TCMDC-135051 TFA

TCMDC-135051 TFA 是一种高选择性和有效性的蛋白激酶 PfCLK3 抑制剂,具有低的靶外毒性。TCMDC-135051 TFA 可以防止滋养体到裂殖体的转变,破坏转录并减少向蚊子载体的传播。TCMDC-135051 TFA 具有抗寄生虫活性 (EC50=320 nM)。

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TCMDC-135051 TFA Chemical Structure

TCMDC-135051 TFA Chemical Structure

CAS No. : 2571578-55-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TCMDC-135051 TFA is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 TFA prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 TFA has antiparasiticidal activity (EC50=320 nM)[1].

IC50 & Target

PfCLK3[1]

体外研究
(In Vitro)

TCMDC-135051 TFA 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) [1].
The kinase assays using recombinant PvCLK3 (P. vivax) and PbCLK3 (P. berghei) show that TCMDC-135051 TFA 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

585.61

Formula

C31H34F3N3O5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

TCMDC-135051 TFA 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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