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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-AMPK-HTH-02-006
HTH-02-006

Chemical Structure : HTH-02-006

CAS No.:

HTH-02-006

货号: PC-73284Not For Human Use, Lab Use Only.

HTH-02-006 is a potent, selective reversible inhibitor of NUAK1/2 with binding IC50 of 8/126 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HTH-02-006 is a potent, selective reversible inhibitor of NUAK1/2 with binding IC50 of 8/126 nM, respectively.
HTH-02-006 reduces MYPT1(S445) phosphorylation in HuCCT-1 cells, suggesting NUAK1/2 inhibition.
HTH-02-006 ameliorates YAP(S127A)-induced hepatomegaly, and reduces MYPT1(S445) phosphorylation.
HTH-02-006 delays the outgrowth of YAP-induced HuCCT-1 xenograft tumors in nude mice.
HTH-02-006 downregulated E2F, EMT, and MYC hallmark gene sets after NUAK2 inhibition in PC cells.
HTH-02-006 slowed tumor growth and proliferation rates in a syngeneic allograft model and in radical prostatectomy patient derived explants.
HTH-02-006 treatment led to inactivation of YAP and the downregulation of NUAK2 and MYC protein levels.

物理化学性质&存储条件

分子量 588.450
分子式 C25H29IN6O3
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

N-(3-((5-iodo-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin4-yl)oxy)phenyl)propionamide

参考文献

1. Weiwei Fu, et al. Mol Carcinog. 2022 Mar;61(3):334-345.

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