ISM5939 | ENPP1 inhibitor | Probechem Biochemicals

Chemical Structure : ISM5939

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ISM5939 (ISM-5939)

货号: PC-24673Not For Human Use, Lab Use Only.

ISM5939 is a potent and selective, orally bioavailable ENPP1 inhibitor with IC50 of 0.63 nM against the 2,3-cGAMP degradation and 9.28 nM against ATP hydrolysis.

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生物&药学活性

ISM5939 is a potent and selective, orally bioavailable ENPP1 inhibitor with IC50 of 0.63 nM against the 2,3-cGAMP degradation and 9.28 nM against ATP hydrolysis.
ISM5939 is competitive with the natural substrates of ENPP1.
ISM5939 displays >3400-fold selectivity over ENPP2 and ENPP3, does not exhibit any significant agonistic or antagonistic effects against 44 clinically relevant off-targets, including GPCRs, ion channels, enzymes, nuclear receptors, and key transporters.
ISM5939 has mean IC50 of 40 nM for maintaining extracellular cGAMP levels in the presence of ENPP1-expressing cancer cells, including MDA-MB-231 breast cancer cells and H1792 lung adenocarcinoma cells.
ISM5939 stabilizes tumor-secreted cGAMP and orchestrates non-cell autonomous STING activation in antigen-presenting cells.
ISM5939 synergizes with targeting the PD-1/PD-L1 axis and chemotherapy in suppressing tumor growth with good tolerance, in murine syngeneic models across cancer types.

物理化学性质&存储条件

分子量	427.45
分子式	C20H18FN5O3S
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	5-fluoro-6-((6-methoxy-2-methyl-7-phenyl-1H-imidazo[4,5-c]pyridin-1-yl)methyl)pyridine-3-sulfonamide

参考文献

1. Congying Pu, et al. Nat Commun. 2025 May 23;16(1):4793.

ISM5939 (ISM-5939)

生物&药学活性

物理化学性质&存储条件

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ISM5939 (ISM-5939)

生物&药学活性

物理化学性质&存储条件

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