Kasugamycin (hydrochloride)是一种对多种细菌具有活性的氨基糖苷类抗生素。
Cas No.:19408-46-9
Sample solution is provided at 25 µL, 10mM.
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Kasugamycin (hydrochloride) is an aminoglycosidic antibiotic against many different bacteria [1]. Kasugamycin binds to the 30S ribosomal subunit and the 70S ribosome of Escherichia coli, inhibiting the translation of typical transcripts with the 5' untranslated region (5'-UTR) containing the Shine-Dalgarno (SD) sequence[2]. Kasugamycin has been widely used to inhibit the growth of Escherichia coli, as well as for conducting studies on drug resistance or sensitivity analysis[3].
In vitro, Kasugamycin treatment for 24 hours significantly inhibited the growth of Pectobacterium aroidearum, with an EC50 value of 20.14μg/ml[4]. Treatment with Kasugamycin (250ng/ml) for 48 hours can eliminate the ERK and AKT activation stimulated by chitinase 3-like-1 (CHI3L1) in Calu-3 cells, and inhibit the uptake of the pseudovirus carrying the Omicron S protein mutation by Calu-3 cells[5].
In vivo, Kasugamycin treatment via intraperitoneal injection at a dose of 100mg/kg (every other day) for 30 days inhibited bleomycin-stimulated pulmonary fibrosis in mice and reduced the collagen accumulation[6]. Daily intraperitoneal injection of 400mg/kg dose of Kasugamycin combined with 10mg/kg/day rifampicin (p.o.) for 2 weeks significantly reduced the bacterial load in the lungs of mice infected with Mycobacterium tuberculosis[7].
References:
[1] Umezawa H, Okami Y, Hashimoto T, et al. A new antibiotic, kasugamycin[J]. The Journal of Antibiotics, Series A, 1965, 18(2): 101-103.
[2] Okuyama A, Tanaka N, KOMAI T. The binding of kasugamycin to the Escherichia coli ribosomes[J]. The Journal of Antibiotics, 1975, 28(11): 903-905.
[3] Lange C, Lehr M, Zerulla K, et al. Effects of kasugamycin on the translatome of Escherichia coli[J]. PloS one, 2017, 12(1): e0168143.
[4] Xiong C, Zhou X, Tu Y, et al. Kasugamycin disrupts membrane transport and reduces virulence in Pectobacterium aroidearum to control konjac soft rot[J]. Phytopathology Research, 2025, 7(1): 52.
[5] Kamle S, Ma B, Lee C M, et al. Host chitinase 3-like-1 is a universal therapeutic target for SARS-CoV-2 viral variants in COVID-19[J]. Elife, 2022, 11: e78273.
[6] Lee J H, Lee C M, Lee J H, et al. Kasugamycin is a novel chitinase 1 inhibitor with strong antifibrotic effects on pulmonary fibrosis[J]. American Journal of Respiratory Cell and Molecular Biology, 2022, 67(3): 309-319.
[7] Chaudhuri S, Li L, Zimmerman M, et al. Kasugamycin potentiates rifampicin and limits emergence of resistance in Mycobacterium tuberculosis by specifically decreasing mycobacterial mistranslation[J]. Elife, 2018, 7: e36782.
Kasugamycin (hydrochloride)是一种对多种细菌具有活性的氨基糖苷类抗生素[1]。Kasugamycin结合大肠杆菌的30S核糖体亚基和70S核糖体，抑制含有Shine-Dalgarno（SD）序列的5'非翻译区（5'-UTR）的典型转录本的翻译[2]。Kasugamycin已被广泛用于抑制大肠杆菌的生长，以及进行耐药性或敏感性分析的研究[3]。
在体外，Kasugamycin处理24小时显著抑制了Pectobacterium aroidearum的生长，EC50值为20.14μg/ml [4]。使用250ng/ml的Kasugamycin处理48小时，可消除chitinase 3-like-1 (CHI3L1)刺激的Calu-3细胞中ERK和AKT的激活，并抑制Calu-3细胞对携带Omicron S蛋白突变假病毒的摄取[5]。
在体内，每隔一天腹腔注射100mg/kg剂量的Kasugamycin，持续30天，抑制了博来霉素刺激的小鼠肺纤维化并减少了胶原沉积[6]。每日腹腔注射400mg/kg剂量的Kasugamycin，联合口服10mg/kg/day剂量的利福平，持续两周，显著降低了感染结核分枝杆菌小鼠肺部的细菌负荷[7]。
| Cell experiment [1]: | |
Cell lines | Calu-3 cells |
Preparation Method | Calu-3 cells were cultured in DMEM medium supplemented with high glucose, l-glutamine, minimal essential media nonessential amino acids, penicillin/streptomycin, and 10% fetal bovine serum. Calu-3 cells (1×106 cells) were plated using 4-well chamber slides and subjected to incubation for 24h, and then infected with pseudoviruses (containing Omicron S protein) for 48h in the presence of Kasugamycin (250ng/ml) and rhCHI3L1 (250ng/ml), followed by evaluation of pseudovirus infection of Calu-3 cell. |
Reaction Conditions | 250ng/ml; 48h |
Applications | Kasugamycin treatment inhibit uptake of omicron pseudotyped viral variants by Calu-3 cell. |
| Animal experiment [2]: | |
Animal models | C57BL/6 (Tgfbrap1−/−) mice |
Preparation Method | 8 weeks old male C57BL/6 (Tgfbrap1−/−) mice were raised under specific pathogen-free (SPF) conditions, placed in separate ventilated cages, with a room temperature of 20-23℃ and a light cycle of 12 hours of light/12 hours of darkness. Mice were challenged with bleomycin (i.p.; 0.25U/mouse) together with Kasugamycin (100mg/kg; every other day; i.p.) for 30 days. Then the mice were sacrificed 2 days after the last Kasugamycin treatment, and the lung lysates were prepared and used to analysis. |
Dosage form | 100mg/kg; every other day for 30 days; i.p. |
Applications | Kasugamycin treatment inhibited bleomycin-stimulated pulmonary fibrosis in mice and reduced the collagen accumulation. |
References: | |
| Cas No. | 19408-46-9 | SDF | |
| 别名 | 春雷霉素盐酸盐; Ksg hydrochloride | ||
| 化学名 | 3-O-[2-amino-4-[(carboxyiminomethyl)amino]-2,3,4,6-tetradeoxy-α-D-arabino-hexopyranosyl]-D-chiro-inositol, monohydrochloride | ||
| Canonical SMILES | O[C@H]1[C@@H](O)[C@H](O)[C@H](O)[C@@H](O[C@@]2([H])O[C@H](C)[C@@H](NC(C(O)=O)=N)C[C@@H]2N)[C@@H]1O.Cl | ||
| 分子式 | C14H25N3O9 • HCl | 分子量 | 415.8 |
| 溶解度 | ≥ 41.6mg/mL in Water with gentle warming | 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 | 2.405 mL | 12.025 mL | 24.05 mL |
| 5 mM | 481 μL | 2.405 mL | 4.81 mL |
| 10 mM | 240.5 μL | 1.2025 mL | 2.405 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。
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- Purity: >90.00% Appearance: A solid
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