1. Cell Cycle/DNA Damage
    Anti-infection
  2. CDK
    Parasite
  3. TCMDC-135051

TCMDC-135051 

Cat. No.: HY-126323
Handling Instructions

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

For research use only. We do not sell to patients.

TCMDC-135051 Chemical Structure

TCMDC-135051 Chemical Structure

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Description

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

IC50 & Target

PfCLK3[1]

In Vitro

TCMDC-135051 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 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].

Molecular Weight

471.59

Formula

C₂₉H₃₃N₃O₃

SMILES

O=C(O)C1=CC=C(C2=C3C(NC(C4=C(OC)C=CC(CN(CC)CC)=C4)=C3)=NC=C2)C=C1C(C)C

Shipping

Room temperature in continental US; may vary elsewhere

Storage

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

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TCMDC-135051
Cat. No.:
HY-126323
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