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TCMDC-135051

Catalog No. T13102   CAS 2413716-15-9

TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector.

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TCMDC-135051 Chemical Structure
TCMDC-135051, CAS 2413716-15-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 132.00
5 mg In stock $ 328.00
10 mg In stock $ 563.00
25 mg In stock $ 889.00
50 mg In stock $ 1,180.00
100 mg In stock $ 1,590.00
500 mg In stock $ 3,230.00
1 mL * 10 mM (in DMSO) In stock $ 343.00
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Purity: 98.21%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector.
In vitro In a liver invasion and development assay, TCMDC-135051 shows potent activity against P. berghei sporozoites 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 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
CAS No. 2413716-15-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 225 mg/mL (477.1 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Alam MM, et al. Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target. Science. 2019 Aug 30;365(6456). pii: eaau1682.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Parasitic Compound Library Highly Selective Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

TCMDC-135051 2413716-15-9 Others TCMDC135051 TCMDC 135051 inhibitor inhibit

 

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