Dihydronovobiocin
目录号 : GC47228
A coumarin antibiotic
Cas No.:29826-16-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Dihydronovobiocin is a coumarin antibiotic and derivative of novobiocin .1 It is active against the bacteria S. aureus, S. haemolyticus, D. pneumoniae, S. typhosa, K. pneumoniae, and P. multocida (MICs = 0.6, 2, 0.6, 10, 10, and 3 µg/ml, respectively).2 Dihydronovobiocin inhibits DNA gyrase subunit B with an IC50 value of 64.5 nM.3
1.Berger, J., and Batcho, A.D.Coumarin - glycoside antibioticsJ. Chromatogr. Lib.15101-158(1978) 2.Hoeksema, H.Dihydronovobiocin and derivatives thereof3,175,9441-9(1965) 3.Gevi, M., and Domenici, E.A scintillation proximity assay amenable for screening and characterization of DNA gyrase B subunit inhibitorsAnal. Biochem.300(1)34-39(2002)
| Cas No. | 29826-16-2 | SDF | |
| Canonical SMILES | O[C@H]1[C@H](OC2=CC=C(C(O)=C(NC(C3=CC(CCC(C)C)=C(O)C=C3)=O)C(O4)=O)C4=C2C)OC(C)(C)[C@H](OC)[C@H]1OC(N)=O | ||
| 分子式 | C31H38N2O11 | 分子量 | 614.6 |
| 溶解度 | DMF: soluble,DMSO: soluble,Ethanol: soluble,Methanol: soluble | 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 | 1.6271 mL | 8.1354 mL | 16.2707 mL |
| 5 mM | 0.3254 mL | 1.6271 mL | 3.2541 mL |
| 10 mM | 0.1627 mL | 0.8135 mL | 1.6271 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。
Demonstrating Ligandability of the LC3A and LC3B Adapter Interface
J Med Chem 2021 Apr 8;64(7):3720-3746.PMID:33769048DOI:10.1021/acs.jmedchem.0c01564.
Autophagy is the common name for a number of lysosome-based degradation pathways of cytosolic cargos. The key components of autophagy are members of Atg8 family proteins involved in almost all steps of the process, from autophagosome formation to their selective fusion with lysosomes. In this study, we show that the homologous members of the human Atg8 family proteins, LC3A and LC3B, are druggable by a small molecule inhibitor novobiocin. Structure-activity relationship (SAR) studies of the 4-hydroxy coumarin core scaffold were performed, supported by a crystal structure of the LC3A Dihydronovobiocin complex. The study reports the first nonpeptide inhibitors for these protein interaction targets and will lay the foundation for the development of more potent chemical probes for the Atg8 protein family which may also find applications for the development of autophagy-mediated degraders (AUTACs).
A scintillation proximity assay amenable for screening and characterization of DNA gyrase B subunit inhibitors
Anal Biochem 2002 Jan 1;300(1):34-9.PMID:11743689DOI:10.1006/abio.2001.5406.
DNA gyrase is the target of coumarin and cyclothialidine antibacterials, which bind to the B subunit of the enzyme (GyrB). Currently available GyrB inhibitors have not been clinically successful, but their high in vitro potency against DNA gyrase has raised interest in the development of novel noncoumarin antibacterials acting at the same site. We report the development of a simple scintillation proximity assay (SPA) for the study of binding interactions between coumarin or noncoumarin antibacterials and GyrB, which prevents the needs of separation steps and can be run in microtiter plate formats. The assay is based on the detection of the binding of a radioligand, [3H]Dihydronovobiocin, to a biotin-labeled 43-kDa fragment of GyrB (biotin-GyrB43), which is captured by streptavidin-coated SPA beads. The typical assay was conducted in 96-well microtiter plates, with final concentration of 10 nM for biotin-GyrB43, 20 nM for [3H]Dihydronovobiocin, and 33 microg of SPA beads/well. From saturation experiments, an equilibrium dissociation constant (K(d)) for Dihydronovobiocin of 8.10 nM was found. Displacement studies gave 50% inhibitory concentrations (IC(50)) of 42, 64, and 11 nM for novobiocin, Dihydronovobiocin, and the cyclothialidine analogue GR122222X, respectively, consistent with previous findings. The assay was found to be robust to dimethyl sulfoxide up to 5% (v/v) and can be used for high-throughput screens of large chemical collections in the search of novel DNA gyrase inhibitors.