2. Anti-infection
  3. Bacterial
  4. FabI-IN-1

FabI-IN-1 是一种 FabI (烯酰-酰基载体蛋白还原酶) 抑制剂，对 E. coli FabI 的 Ki 为 0.32 μM。FabI-IN-1 对包括 Escherichia coli (MIC = 6.25 μM) 和 Klebsiella pneumoniae 在内的革兰氏阴性菌具有抑制活性。FabI-IN-1 可拯救大蜡螟幼虫免受致死性 Escherichia coli 感染。FabI-IN-1 与 Colistin (HY-113678) 联合对 Escherichia coli 发挥协同作用。FabI-IN-1 可用于革兰氏阴性菌感染的研究。

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FabI-IN-1

FabI-IN-1 Chemical Structure

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FabI-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FabI-IN-1 is a FabI (enoyl-acyl carrier protein reductase) inhibitor with a Ki of 0.32 μM against E. coli FabI. FabI-IN-1 inhibits exhibits activity against Gram-negative bacteria including Escherichia coli (MIC = 6.25 μM) and Klebsiella pneumoniae. FabI-IN-1 rescues Galleria mellonella larvae from lethal Escherichia coli infection. FabI-IN-1 exerts a synergistic effect with Colistin (HY-113678) against Escherichia coli. FabI-IN-1 can be used for the research of gram-negative bacterial infection[1].

体外研究
(In Vitro)

FabI-IN-1 (Compound 11) (2 μM) 可强效抑制重组 E. coli FabI 酶，其初步 Ki 为 0.32 μM，且在 2 μM 浓度下的抑制率可达 80.3%[1]。
FabI-IN-1 (24 h) 可抑制多种革兰氏阴性菌株的生长，孵育 24 h 后其 MIC 值范围为 6.25 μM 至 75 μM[1]。
FabI-IN-1 (72 h) 对哺乳动物细胞表现出较低的体外细胞毒性，72 h 孵育后在 HepG2 细胞中的 IC50 值为 106 ± 13 μM，在 Hs27 细胞中的 IC50 值为 240 ± 9 μM[1]。
FabI-IN-1 (1.25-5.01 μM; 24 h) 与多黏菌素联合对 E. coli ATCC25922 表现出协同抗菌活性，其 FICI 为 0.25，且在 1.25 μM 和 5.01 μM 浓度下可使 Colistin (HY-113678) 的 MIC 降低 4 倍[1]。
FabI-IN-1 (25 μM; 24 h) 对 E. coli ATCC25922 表现出杀菌活性，可在 24 h 内清除所有活菌且未出现耐药性产生的迹象[1]。
FabI-IN-1 (200 μM; 48 h) 对 E. coli ATCC25922 的 MPC 为 200 μM，且自发耐药突变的发生率较低，为 2×10-8 至 9×10-9[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

FabI-IN-1 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Human HepG2 hepatocarcinoma cells, human Hs27 normal fibroblast cells
Concentration: Serial dilutions (IC50 determination)
Incubation Time: 72 h
Result: Demonstrated an IC50 of 106 ± 13 μM in HepG2 cells.
Demonstrated an IC50 of 240 ± 9 μM in Hs27 cells.
体内研究
(In Vivo)

FabI-IN-1 (Compound 11) (0.563-5.63 mg/kg；血腔内注射；单剂量；感染后 1 小时) 可显著提高感染 E. coli 的大蜡螟幼虫的存活率[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Greater wax moth (final instar larvae, average weight 350 mg, inoculated with Escherichia coli ATCC25922)[1]
Dosage: 0.563 mg/kg; 1.13 mg/kg; 2.81 mg/kg; 5.63 mg/kg
Administration: Intrahemocoelic injection; single dose; 1 hour post-infection
Result: Exhibited 70% survival rate at 0.563 mg/kg, which was not statistically significant compared to the nontreated infected group.
Achieved 75% survival rate at 1.13 mg/kg, which was significantly different from the nontreated infected group.
Demonstrated survival efficacy equivalent to Ciprofloxacin (HY-B0356) (20 mg/kg) at 2.81 mg/kg, with no statistically significant difference.
Showed no significant toxic effects relative to the PBS-only injected group up to 72 hours post-treatment at 5.63 mg/kg.
分子量

315.16

Formula

C14H14BN3O3S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

FabI-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FabI-IN-1BacterialGram-negative bacteriaE. coli FabIKlebsiella pneumoniaeAcinetobacter baumanniiEscherichia coliGalleria mellonellaHs27 cellsFabIHepG2 cellsSalmonella enterica ser. TyphimuriumInhibitorinhibitorinhibit

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