| 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 |
| Molecular formula | C29H33N3O3 |
| CAS | 2413716-15-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 225 mg/mL (477.1 mM), Sonication is recommended. |
| References | 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. |