Bischloroanthrabenzoxocinone
(Synonyms: BABX, (―)-Bischloroanthrabenzoxocinone) 目录号 : GC42943
An inhibitor of FAS-II
Cas No.:866022-28-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bacterial type II fatty acid synthesis (FAS-II) is mediated by a series of enzymes, each of which may be targeted by potential antibiotics. Bischloroanthrabenzoxocinone (BABX) is an inhibitor of FAS-II, blocking fatty acid synthesis in S. aureus and E. coli with IC50 values of 11.4 and 35.3 µg/ml, respectively. It inhibits the growth of S. aureus and permeable E. coli strains with minimum inhibitory concentrations ranging from 0.2-0.4 µg/ml. BABX also displays binding to liver X receptors (LXRs), inhibiting agonist binding in an LXRα-scintillation proximity assay (IC50 = 10 µM).
| Cas No. | 866022-28-8 | SDF | |
| 别名 | BABX, (―)-Bischloroanthrabenzoxocinone | ||
| Canonical SMILES | CC1=CC(OC)=CC2=C1[C@]([H])(O3)C4=C(O)C5=C(C=C4C[C@@]3(C)O2)C(C)(C)C6=C(Cl)C(O)=C(Cl)C(O)=C6C5=O | ||
| 分子式 | C28H24Cl2O7 | 分子量 | 543.4 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8403 mL | 9.2013 mL | 18.4026 mL |
| 5 mM | 0.3681 mL | 1.8403 mL | 3.6805 mL |
| 10 mM | 0.184 mL | 0.9201 mL | 1.8403 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Determination of selectivity and efficacy of fatty acid synthesis inhibitors
J Biol Chem 2005 Jan 14;280(2):1669-77.PMID:15516341DOI:10.1074/jbc.M406848200.
Type II fatty acid synthesis (FASII) is essential to bacterial cell viability and is a promising target for the development of novel antibiotics. In the past decade, a few inhibitors have been identified for this pathway, but none of them lend themselves to drug development. To find better inhibitors that are potential drug candidates, we developed a high throughput assay that identifies inhibitors simultaneously against multiple targets within the FASII pathway of most bacterial pathogens. We demonstrated that the inverse t(1/2) value of the FASII enzyme-catalyzed reaction gives a measure of FASII activity. The Km values of octanoyl-CoA and lauroyl-CoA were determined to be 1.1 +/- 0.3 and 10 +/- 2.7 microM in Staphylococcus aureus and Bacillus subtilis, respectively. The effects of free metals and reducing agents on enzyme activity showed an inhibition hierarchy of Zn2+ > Ca2+ > Mn2+ > Mg2+; no inhibition was found with beta-mercaptoethanol or dithiothreitol. We used this assay to screen the natural product libraries and isolated an inhibitor, Bischloroanthrabenzoxocinone (BABX) with a new structure. BABX showed IC50 values of 11.4 and 35.3 microg/ml in the S. aureus and Escherichia coli FASII assays, respectively, and good antibacterial activities against S. aureus and permeable E. coli strains with minimum inhibitory concentrations ranging from 0.2 to 0.4 microg/ml. Furthermore, the effectiveness, selectivity, and the in vitro and in vivo correlations of BABX as well as other fatty acid inhibitors were elucidated, which will aid in future drug discovery.