4"-Isovalerylspiramycin I - CAS:267662-22-6

您当前的位置：

4"-Isovalerylspiramycin I (Synonyms:Isovalerylspiramycin I; Shengjimycin E)

目录号 : KM32608 CAS No. : 267662-22-6

Data Sheet 产品使用指南

4"-Isovalerylspiramycin I (Isovalerylspiramycin I) 是一种拓扑异构酶 1 (TOP1) 抑制剂和抗肿瘤剂。4"-Isovalerylspiramycin I 可直接结合 TOP1，抑制 DNA 复制并诱导 DNA 损伤。4"-Isovalerylspiramycin I 可下调磷酸化 CHEK1 及 ATR/CHEK1 DNA 损伤修复通路，阻断 DNA 修复并加重 DNA 损伤。4"-Isovalerylspiramycin I 可抑制骨肉瘤细胞的增殖、迁移及侵袭。4"-Isovalerylspiramycin I 可诱导骨肉瘤细胞凋亡 (apoptosis) 及细胞周期阻滞。4"-Isovalerylspiramycin I 对耐甲氧西林金黄色葡萄球菌具有抗菌活性。4"-Isovalerylspiramycin I 可用于骨肉瘤、上呼吸道细菌感染及耐甲氧西林金黄色葡萄球菌感染的研究。

规格	价格	是否有货	数量
50mg	询价	In-stock

加入购物车大包装询价

Other Forms of Rapamycin:

4"-Isovalerylspiramycin I In-stock
S-Methyl thiomethanesulfonate In-stock
Ceftolozane sulfate In-stock
4,8-DiMeIQx In-stock
Azidocillin In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

4"-Isovalerylspiramycin I (Isovalerylspiramycin I) is a topoisomerase 1 (TOP1) inhibitor and an antitumor agent. 4"-Isovalerylspiramycin I directly binds to TOP1, suppresses DNA replication, and induces DNA damage. 4"-Isovalerylspiramycin I downregulates phosphorylated CHEK1 and the ATR/CHEK1 DNA damage repair pathway, blocks DNA repair, and augments DNA damage. 4"-Isovalerylspiramycin I suppresses proliferation, migration, and invasion of osteosarcoma cells. 4"-Isovalerylspiramycin I induces apoptosis and cell cycle arrest in osteosarcoma cells. 4"-Isovalerylspiramycin I exerts antibacterial activity against methicillin-resistant Staphylococcus aureus. 4"-Isovalerylspiramycin I can be used for the research of osteosarcoma, upper respiratory bacterial infections, and methicillin-resistant Staphylococcus aureus infection.

体外研究

After incubation for 24 hours, 4 "- Isollerylspiramycin I (0-50 µM; 24 h) can dose dependently inhibit the proliferation of 143B and Saos-2 human osteosarcoma cells, with IC50 values of 8.7 µM and 17.8 µM, respectively. Overexpression of TOP1 can reverse this effect [1].
4 "- Isollerylspiramycin I (2.5-20 µM; 24 h) dose dependently inhibits the migration ability of 143B and Saos-2 human osteosarcoma cells after 24 hours of incubation; This effect can be reversed by overexpression of TOP1 [1].
4 "- Isollerylspiramycin I (2.5-20 µM; 24-hour pre treatment) can dose dependently inhibit the invasive ability of 143B and Saos-2 human osteosarcoma cells [1].
After 24 hours of incubation, 4 "- Isollerylspiramycin I (2.5-20 µM; 24 h) can dose dependently inhibit DNA replication in human osteosarcoma cells 143B and Saos-2, as confirmed by a decrease in EdU incorporation [1].
After incubation for 24 hours, 4 "- Isollerylspiramycin I (2.5-20 µM; 24 h) can dose dependently induce apoptosis in human osteosarcoma cell lines 143B and Saos-2 [1].
4 "- Isolelyspiramycin I (2.5-20 µM; 24 h) dose dependently altered the expression of pro apoptotic and anti apoptotic proteins in 143B and Saos-2 human osteosarcoma cells, incubated for 24 hours [1].
After 24 hours of incubation, the expression of G0/G1 cell cycle regulatory proteins was dose dependently downregulated in human osteosarcoma cells 143B and Saos-2 using 4 "- Isolaleylspiramycin I (2.5-20 µM; 24 h).
4 "- Isollerylspiramycin I (10-20 µM; 18 h) can directly bind to intracellular TOP1 in 143B and Saos-2 human osteosarcoma cells, and improve the thermal stability of TOP1 after incubation for 18 hours [1].
4 "- Isovalerylspiramycin I (0.125 μg/mL) has an inhibitory effect on methicillin-resistant Staphylococcus aureus CMCC 5342, with a MIC of 0.125 μg/mL.

Cell Proliferation Assay

Cell Line:	143B and Saos-2
Concentration:	0-40 µM (143B, TOP1-overexpressing 143B); 0-50 µM (Saos-2, TOP1-overexpressing Saos-2)
Incubation Time:	24 hours
Result:	Inhibited 143B and Saos-2 cell proliferation in a dose- and time-dependent manner, with IC₅₀ values of 8.7 µM (143B) and 17.8 µM (Saos-2) after 24 h. Increased IC₅₀ values to 19.2 µM (TOP1-overexpressing 143B) and 30.6 µM (TOP1-overexpressing Saos-2) after 24 h, reversing the antiproliferative effect.

Cell Migration Assay

Cell Line:	143B and Saos-2
Concentration:	2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:	24 hours
Result:	Reduced wound closure in both 143B and Saos-2 cells in a dose-dependent manner, inhibiting cell migration. Reversed this inhibitory effect on migration when TOP1 was overexpressed.

Cell Invasion Assay

Cell Line:	143B and Saos-2
Concentration:	2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:	24 hours(pre-treatment)
Result:	Reduced the number of invading 143B and Saos-2 cells in a dose-dependent manner. Reversed this inhibitory effect on invasion when TOP1 was overexpressed.

Apoptosis Analysis

Cell Line:	143B and Saos-2
Concentration:	2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:	24 hours
Result:	Induced dose-dependent apoptosis in both 143B and Saos-2 cells, with apoptosis rates reaching ~30% (143B at 10 µM) and ~30% (Saos-2 at 20 µM).

Western Blot Analysis

Cell Line:	143B and Saos-2
Concentration:	2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:	24 hours
Result:	Downregulated BCL-2 protein expression and upregulated cleaved caspase-3 and BAX protein expression in both 143B and Saos-2 cells in a dose-dependent manner. Reduced protein expression of CDK4 and Cyclin D1 in both 143B and Saos-2 cells in a dose-dependent manner.

Cell Cycle Analysis

Cell Line:	143B and Saos-2
Concentration:	2.5-10 µM (143B); 5-20 µM (Saos-2)
Incubation Time:	24 hours
Result:	Induced a dose-dependent increase in the percentage of cells in the G0/G1 phase, with a corresponding decrease in the S-phase population in both 143B and Saos-2 cells.

体内研究

4 "- Isollerylspiramycin I (60 mg/kg; i.p.; every 1 day; 30 days) significantly inhibited subcutaneous osteosarcoma tumor growth and lung metastasis in female M-NSG mice, with good tolerance [1].

Animal Model:	M-NSG mice (female, 4-6 weeks old, ~20 g) injected with 143B cells.
Dosage:	60 mg/kg
Administration:	i.p.; every 1 day; 30 days
Result:	Significantly inhibited increases in tumor volume in 143B xenografts. Showed no significant difference in mouse body weight compared to controls, indicating good tolerability. Reduced TOP1 expression in tumor tissues via immunohistochemical staining. Significantly inhibited osteosarcoma lung metastasis via lung H&E staining.

分子式

C₄₈H₈₂N₂O₁₅

分子量

927.17

CAS号

267662-22-6

中文名称

异戊酰螺旋霉素I

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Data Sheet

产品使用指南

[1]. Jinrong Liang, et al. Isovalerylspiramycin I inhibits proliferation, migration and invasion of osteosarcoma cells by targeting Topoisomerase 1 and suppressing the ataxia telangiectasia and Rad3-related/checkpoint kinase 1 pathway. Clin. Transl. Disc. 2023;3:e203.

[2]. Ma C, et al. Construction of 4"-isovalerylspiramycin-I-producing strain by in-frame partial deletion of 3-O-acyltransferase gene in Streptomyces spiramyceticus WSJ-1, the bitespiramycin producer. Curr Microbiol. 2011;62(1):16-20.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

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

每只动物给药体积

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，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

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，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

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 ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：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。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器