Chemical Structure : DF-003
CAS No.:
2765462-07-3
DF-003
(DF003)
Catalog No.: PC-25504Not For Human Use, Lab Use Only.
DF-003 (DF003) is a potent, selective and ATP-competitive alpha-kinase 1 (ALPK1) inhibitor with IC50 of 1.5 nM and 16 nM for human ALPK1 and ROSAH disease-causing mutant ALPK1[T237M] respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
DF-003 (DF003) is a potent, selective and ATP-competitive alpha-kinase 1 (ALPK1) inhibitor with IC50 of 1.5 nM and 16 nM for human ALPK1 and ROSAH disease-causing mutant ALPK1[T237M] respectively.
DF-003 exhibits good selectivity for ALPK1 against a panel of 394 human kinases, >860-fold selectivity over the closest kinase.
DF-003 blocks induction of TIFAsome formation and chemokine/cytokine production by the ALPK1 agonist DF-006 (Cat. PC-47007).
DF-003 inhibits the kinase activity of ALPK1[T237M] and blocks NF-κB target gene expression induced by ALPK1[T237M], DF-003 suppresses (IC50 = 125 nM) the enhanced secretion of CXCL8 from HEK-293 cells overexpressing ALPK1[T237M].
DF-003 (3 mg/kg) inhibits retinal microglia and astrocyte activity in ROSAH mice.
DF-003 suppresses pro-inflammatory gene upregulation in the retina, optic nerve, and brain cortex of ROSAH model mice.
Physicochemical Properties
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M.Wt
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486.97
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Formula
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C24H21ClF2N4OS
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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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(S)-N-(4-(2-(4-chlorophenyl)but-3-yn-2-yl)thiazol-2-yl)-2,6-difluoro-4-(piperazin-1-yl)benzamide
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References
1. Fan J, et al. Discovery of a selective alpha-kinase 1 inhibitor for the rare genetic disease ROSAH syndrome. Nat Commun. 2025 Sep 9;16(1):8251.
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