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首页-小分子抑制剂&激动剂-Others-Other Targets-DF-003
DF-003

Chemical Structure : DF-003

CAS No.: 2765462-07-3

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DF-003 (DF003)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 486.97
分子式 C24H21ClF2N4OS
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-N-(4-(2-(4-chlorophenyl)but-3-yn-2-yl)thiazol-2-yl)-2,6-difluoro-4-(piperazin-1-yl)benzamide

参考文献

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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