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CHIR-090 {[allProObj[0].p_purity_real_show]}

货号:A106028

CHIR-090是一种 LpxC 脱乙酰酶抑制剂,具有抗微生物活性,Ki 值为 4.0 nM。它用于抑制脂多糖合成。

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CHIR-090 化学结构 CAS号:728865-23-4
CHIR-090 化学结构
CAS号:728865-23-4
CHIR-090 3D分子结构
CAS号:728865-23-4
CHIR-090 化学结构 CAS号:728865-23-4
CHIR-090 3D分子结构 CAS号:728865-23-4
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CHIR-090 纯度/质量文件 产品仅供科研

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CHIR-090 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].

CHIR-090 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

CHIR-090 实验方案

计算器
存储液制备 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

CHIR-090 技术信息

CAS号728865-23-4
分子式C24H27N3O5
分子量 437.49
SMILES Code O=C(N[C@H](C(NO)=O)[C@H](O)C)C1=CC=C(C#CC2=CC=C(CN3CCOCC3)C=C2)C=C1
MDL No. MFCD22665727
别名
运输蓝冰
InChI Key FQYBTYFKOHPWQT-VGSWGCGISA-N
Pubchem ID 11546620
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

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

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