CHIR-090

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Chemical Structure| 728865-23-4 同义名 : -
CAS号 : 728865-23-4
货号 : A106028
分子式 : C24H27N3O5
纯度 : 99%+
分子量 : 437.488
MDL号 : MFCD22665727
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(9.14 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+water 0.1 mg/mL clear

PO 0.5% CMC-Na 60 mg/mL suspension

生物活性
描述 The deacetylation of UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine (UDP-3-O-acyl-GlcNAc) by LpxC deacetylase is the committed reaction of lipid A biosynthesis. CHIR-090, a novel N-aroyl-l-threonine hydroxamic acid, is a competitive, two-step, slow, tight-binding inhibitor of Aquifex aeolicus LpxC. Similar to A. aeolicus LpxC, CHIR-090 inhibits E. coli LpxC by a two-step, time-dependent mechanism with a low nM Ki (1.0 - 1.7 nM for A. aeolicus LpxC versus 4.0 nM for E. coli LpxC). For LpxCs from other Gram-negative organisms, H. pylori LpxC, P. aeruginosa LpxC and N. meningitidis LpxC were inhibited 75 % or more by 4 nM CHIR-090 when enzyme was used to start the reactions. Given the relative resistance of W3110RL towards CHIR-090 (MIC of 100 μg/mL versus 0.25 μg/mL for W3110), conclusion can be made that CHIR-090 is indeed highly selective for LpxC in E. coli K-12[2].
作用机制 CHIR-090 contains a hydroxamate moiety coordinating the catalytic zinc ion. The binding of CHIR-090 is further strengthened through interactions with conserved hydrophilic and hydrophobic residues in the active site[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.43mL

2.29mL

1.14mL

22.86mL

4.57mL

2.29mL
参考文献

[1]Structure of the deacetylase LpxC bound to the antibiotic CHIR-090: Time-dependent inhibition and specificity in ligand binding

[2]Inhibition of lipid A biosynthesis as the primary mechanism of CHIR-090 antibiotic activity in Escherichia coli