MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

CHIR-090

CAS No. : 728865-23-4

MCE 国际站：CHIR-090

产品活性：CHIR-090是一种有效，缓慢，亲和力强的 LpxC 脱乙酰酶抑制剂。它与 E. coli LpxC 结合的 K_i 值为 4.0 nM。

研究领域：Anti-infection

作用靶点：Bacterial  |  Antibiotic

In Vitro: CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase from the hyperthermophile Aquifex aeolicus, and it has excellent antibiotic activity against P. aeruginosa and E. coli, as judged by disk diffusion assays. CHIR-090 is also a two-step slow, tight-binding inhibitor of Escherichia coli LpxC with K_i=4 nM. CHIR-090 at low nM levels inhibits LpxC orthologues from diverse Gram-negative pathogens, including Pseudomonas aeruginosa, Neisseria meningitidis, and Helicobacter pylori. In contrast, CHIR-090 is a relatively weak competitive and conventional inhibitor (lacking slow, tight-binding kinetics) of LpxC from Rhizobium leguminosarum (K_i=340 nM), a Gram-negative plant endosymbiont that is resistant to this compound. An E. coli construct in which the chromosomal lpxC gene is replaced by R. leguminosarum lpxC is resistant to CHIR-090 up to 100 μg/mL, or 400 times above the minimal inhibitory concentration for wild-type E. coli. CHIR-090, a very potent, slow, tight-binding inhibitor of Aquifex aeolicus LpxC, the sequence of which is 31 % identical to E. coli LpxC. CHIR-090 has remarkable antibiotic activity against E. coli and P. aeruginosa, comparable to ciprofloxacin, as judged by disk diffusion assays.

In Vivo: CHIR-090 is a potent antibiotic against E. coli and inhibits E. coli LpxC activity in vitro in the low nM range. E. coli W3110 colonies resistant to 1 μg/mL CHIR-090 are not observed without prior chemical mutagenesis. A strain of E. coli W3110 is able to grow on LB agar plates containing 1 to 10 μg/mL CHIR-090, which is 4 to 40 times above the MIC of 0.25 μg/mL under our conditions for wild-type E. coli W3110. The doubling time of W3110RL is 40 min in the presence of 1 μg/mL CHIR-090, which is exactly the same rate as wild-type in the absence of inhibitor. Wild-type cells stopped growing after about 2 h in the presence of 1 μg/mL CHIR-090.

相关产品：Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  Antibacterial Compound Library  |  Antibiotics Library  |  Myricetin 3-O-α-L-arabinopyranoside  |  (1R,2S,7R)-Sitafloxacin-d₄ hydrochloride  |  Nebacumab  |  Doxorubicin-¹³C,d₃ TFA  |  Gepotidacin  |  Amycolatopsin A  |  Antibiotic A-33853  |  Estradiol hemihydrate  |  Sulbactam-d₂ sodium  |  Antimicrobial agent-5  |  NBTIs-IN-4  |  Proanthocyanidins  |  Anticancer agent 120  |  Azlocillin sodium salt  |  Antitubercular agent-13  |  Toyocamycin  |  Lenampicillin hydrochloride  |  Hispolon  |  PC58538  |  SPR206 acetate  |  Caracemide  |  Antimicrobial agent-10  |  Doxycycline calcium  |  Antibacterial agent 138  |  Staurosporine  |  Dihydrostreptomycin sulfate  |  Ciclopirox olamine  |  Rubropunctamine  |  Topoisomerase IV inhibitor 2  |  Psoracorylifol C

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。