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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-IMPDH-Sappanone A
Sappanone A

Chemical Structure : Sappanone A

CAS No.: 102067-84-5

Sappanone A (IMPDH2 inhibitor)

货号: PC-70216Not For Human Use, Lab Use Only.

Sappanone A is a homoisoflavanone found in Caesalpinia sappan, a potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with Kd of 3.944 nM, almost 10 times lower than the Kd of binding to IMPDH1.

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

生物&药学活性

Sappanone A is a homoisoflavanone found in Caesalpinia sappan, a potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with Kd of 3.944 nM, almost 10 times lower than the Kd of binding to IMPDH1.
Sappanone A significantly suppresses the releases of NO (IC50=4.12 uM), TNF-α, IL-6, and PGE2 and decreases the gene expressions of TNF-α, IL-6, IL-1β, MCP-1, iNOS, and COX-2 in BV-2 cells.
Sappanone A inhibits neuroinflammatory responses with high drug safety and less side effects in vivo.

物理化学性质&存储条件

分子量 284.26
分子式 C16H12O5
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

(3E)-3-(3,4-Dihydroxybenzylidene)-7-hydroxy-2,3-dihydro-4H-chromen-4-one

参考文献

1. Liao LX, et al. Proc Natl Acad Sci U S A. 2017 Jul 18;114(29):E5986-E5994.

2. Kang L, et al. Int Immunopharmacol. 2016 Sep;38:246-51.

3. Lee S, et al. Int Immunopharmacol. 2015 Sep;28(1):328-36.

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