HA344 | PKM2/IMPDH inhibitor | Probechem Biochemicals

Chemical Structure : HA344

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HA344 (HA 344)

货号: PC-49688Not For Human Use, Lab Use Only.

HA344 (HA 344) is a dual covalent inhibitor of pyruvate kinase M2 (PKM2) and inosine monophosphate dehydrogenase (IMPDH), efficiently inhibits cutaneous metastatic melanoma (CMM).

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生物&药学活性

HA344 (HA 344) is a dual covalent inhibitor of pyruvate kinase M2 (PKM2) and inosine monophosphate dehydrogenase (IMPDH), efficiently inhibits cutaneous metastatic melanoma (CMM).
HA344 inhibits glycolysis and purine metabolism and induces cell death that is rescued by pyruvate in CMM cell lines.
HA344 directly inhibits PKM glycolytic enzymatic activity with IC50 of 1 uM in vitro, mutant PKM2 C424L is no longer inhibited by HA344.
HA344 efficiently targeted vemurafenib-sensitive and vemurafenib-resistant CMM cells.
HA344 (5 mg/kg/day) reduced tumor growth in mice xenografted with CMM.

物理化学性质&存储条件

分子量	357.37
分子式	C18H19N3O5
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	ethyl 5-(3-ethoxy-3-oxoprop-1-yn-1-yl)-1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylate

参考文献

1. Zerhouni M, et al. Cancer Res. 2021 Jul 15;81(14):3806-3821.

HA344 (HA 344)

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HA344 (HA 344)

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