Chemical Structure : PfCLK3 inhibitor 4
CAS No.:
PfCLK3 inhibitor 4
(PfCLK3 covalent inhibitor)
Catalog No.: PC-23277Not For Human Use, Lab Use Only.
PfCLK3 inhibitor 4 is a potent, covalent inhibitor of Plasmodium falciparum CLK3 kinase (PfCLK3) with pIC50 of 8.02, covalently targets of PfCLK3 cys368, exhibits parasiticidal activity in P. falciparum 3D7 cell line with pEC50 of 7.1.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PfCLK3 inhibitor 4 is a potent, covalent inhibitor of Plasmodium falciparum CLK3 kinase (PfCLK3) with pIC50 of 8.02, covalently targets of PfCLK3 cys368, exhibits parasiticidal activity in P. falciparum 3D7 cell line with pEC50 of 7.1.
PfCLK3 inhibitor 4 shows excellent selectivity profile compared to TCMDC-135051.
PfCLK3 inhibitor 4 demonstrates constant activity against different stages of asexual P. falciparum parasites, compared with Artemisinin.
PfCLK3 inhibitor 4 arrests development and kills parasites at every stage in the erythrocytic life cycle.
Physicochemical Properties
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M.Wt
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519.00
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Formula
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C28H27ClN4O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-[2-(5-{[4-(2-Chloroacetyl)piperazin-1-yl]methyl}-2-methoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]benzoic Acid
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References
1. Brettell SB, et al. J Med Chem. 2024 Oct 23. doi: 10.1021/acs.jmedchem.4c01300.
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