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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-HIF/HIF Prolyl-hydroxylase-ZG-2291
ZG-2291

Chemical Structure : ZG-2291

CAS No.: 2962103-40-6

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ZG-2291 (ZG2291)

货号: PC-22619Not For Human Use, Lab Use Only.

ZG-2291 is a highly potent, selective and in vivo active factor inhibiting HIF (FIH) inhibitor with Ki of 65.3 nM, 39-fold selective over PHD2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ZG-2291 is a highly potent, selective and in vivo active factor inhibiting HIF (FIH) inhibitor with Ki of 65.3 nM, 39-fold selective over PHD2.
ZG-2291 induces conformational flipping of Tyr102.
ZG-2291 has a high affinity to FIH with a Kd of 99.7 nM in ITC assays, with much weaker binding to PHD2 with a Kd of 5.58 uM.
ZG-2291 is highly selective for FIH over all the other 2OG-dependent JmjC KDMs, including KDM3A,KDM4A, KDM4C, and KDM4D.
ZG-2291 regulates FIH-dependent HIF target gene expressionin cells.
ZG-2291 promotes thermogenesis and improves lipid accumulation in 3T3-L1-derived adipocytes, decrease cellular TG levels and reduce lipid accumulation, soimproving cellular lipid homeostasis.
ZG-2291 (10 mg/kg) protects against obesity, ameliorates symptoms of obesity and associated metabolic dysfunction in ob/ob mice.
ZG-2291 strongly upregulates the uncoupling protein 1 (UCP1) inwhite adipose tissue, so triggering thermogenesis and ameliorating obesity.

物理化学性质&存储条件

分子量 373.75
分子式 C17H12ClN3O5
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

(5-(3-(3-chlorophenyl)isoxazol-5-yl)-3-hydroxypicolinoyl)glycine

参考文献

1. Wu Y, et al. Angew Chem Int Ed Engl. 2024 Jun 26:e202410438.

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