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首页-小分子抑制剂&激动剂-Tyrosine Kinase-DYRK-Leucettinib-21
Leucettinib-21

Chemical Structure : Leucettinib-21

CAS No.: 2732859-75-3

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Leucettinib-21 (LCTB-21)

货号: PC-21506Not For Human Use, Lab Use Only.

Leucettinib-21 is a potent, selective DYRKs and CLKs kinases with IC50 of 2.4, 6.7, 12, 33, and 5 nM for DYRK1A, DYRK1B, CLK1, CLK2, and CLK4, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Leucettinib-21 is a potent, selective DYRKs and CLKs kinases with IC50 of 2.4, 6.7, 12, 33, and 5 nM for DYRK1A, DYRK1B, CLK1, CLK2, and CLK4, respectively.
Leucettinib-21 weakly inhibits DYRK2/3/4, and CLK3 (IC50=200-1000 nM), inhibits only weakly inhibits some kinases (RPS6KA4, CDK7, DMPK) in a panel of 468 kinases at 1 uM.
Leucettinib-21 shows Kd values of 0.272 and 0.388 nM for DYRK1A and CLK1, respectively, 26 and 22 times lower than that for Leucettine L41 (Cat#PC-61025).
Leucettinib-21 triggers a dose-dependent inhibition of endogenous DYRK1A catalytic activity in HT-22 mouse hippocampal neuronal cells with IC50 of 36 nM.
Leucettinib-21 (0-10 uM) inhibits the phosphorylation of reported DYRK1A substrate sites in SH-SY5Y cells, such as Thr286-cyclin D1 and Thr212-Tau, protects cyclin D1 from proteolytic degradation, leading to its accumulation.
Leucettinib-21 (0.4 mg/kg, oral gavage daily, 10 days) corrects memory disorders in the Down syndrome mouse model Ts65Dn, a classical animal model of Down syndrome (DS).

物理化学性质&存储条件

分子量 358.46
分子式 C18H22N4O2S
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

(R,Z)-5-(benzo[d]thiazol-6-ylmethylene)-2-((1-methoxy-4-methylpentan-2-yl)amino)-3,5-dihydro-4H-imidazol-4-one

参考文献

1. Mattias F. Lindberg, et al. Journal of Medicinal Chemistry, 2023.

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