EHT 5372 | DYRK1A inhibitor | Probechem Biochemicals

Chemical Structure : EHT 5372

CAS No.: 1425945-63-6

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EHT 5372 (EHT5372)

货号: PC-21494Not For Human Use, Lab Use Only.

EHT 5372 is a highly potent and selective inhibitor of DYRKs family kinases with IC50s of 0.22, 0.28, 10.8, 93.2 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, respectively.

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5 mg	￥2980	In stock
10 mg	￥4580	In stock
25 mg	￥7280	In stock
100 mg		Get quote

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生物&药学活性

EHT 5372 is a highly potent and selective inhibitor of DYRKs family kinases with IC50s of 0.22, 0.28, 10.8, 93.2 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, respectively.
EHT 5372 also inhibits CLK1, CLK2, CLK4, GSK-3α, and GSK-3β with IC50 of 22.8, 88.8, 59.0, 7.44, and 221 nM for CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively.
EHT 5372 demonstrates good selectivity over 339 tested kinases, with inhibitory activities displayed toward the CMGC group only.
EHT 5372 inhibits DYRK1A-induced Tau phosphorylation at multiple AD-relevant sites in biochemical and cellular assays.
EHT 5372 also normalizes both Aβ-induced Tau phosphorylation and DYRK1A-stimulated Aβ production.
EHT 5372 inhibits DYRK1A-induced Tau phosphorylation, Aβ production and Aβ effects on phospho-Tau, including Tau aggregation.

物理化学性质&存储条件

分子量	404.27
分子式	C17H11Cl2N5OS
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	methyl 9-(2,4-dichlorophenylamino) thiazolo[5,4-f]quinazoline-2-carbimidate

参考文献

1. Foucourt A, et al. Molecules. 2014 Sep 26;19(10):15411-39.

EHT 5372 (EHT5372)

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物理化学性质&存储条件

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EHT 5372 (EHT5372)

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