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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Nur77 (NR4A1)-TMPA
TMPA

Chemical Structure : TMPA

CAS No.: 1258275-73-8

TMPA

货号: PC-26967Not For Human Use, Lab Use Only.

TMPA is a specific, high-affinity Nur77 antagonist that binds directly to Nur77ligand-binding domain (LBD) with KD of 0.25 uM, antagonizes the Nur77-LKB1 interaction, induces LKB1 nuclear export to activate AMPKα.

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

生物&药学活性

TMPA is a specific, high-affinity Nur77 antagonist that binds directly to Nur77ligand-binding domain (LBD) with KD of 0.25 uM, antagonizes the Nur77-LKB1 interaction, induces LKB1 nuclear export to activate AMPKα.
TMPA enhances rather than downregulates the phosphorylation of AMPKα in hepatic LO2 cells in both dose- and time-dependent manners.
TMPA has a strong affinity for both Nur77 and LBD in the quenching experiments but not for monomeric or heterotrimeric AMPKα, AMPKβ, AMPKγ or LKB1.
TMPA does not show any effect on Nur77 transactivation activity.
TMPA affects subcellular localization of LKB1 through phosphorylation at Ser428 in LO2 cells.
TMPA is capable of lowering blood glucose in HFD- and STZ-induced diabetic mice.

物理化学性质&存储条件

分子量 380.48
分子式 C21H32O6
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 2-(2,3,4-trimethoxy-6-octanoylphenyl)acetate

参考文献

1. Zhan YY, et al. Nat Chem Biol. 2012 Nov;8(11):897-904.

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