Novobiocin Sodium (NSC 2382)

别名: Albamycin,Cathomycin,NSC 2382 中文名称:新生霉素钠

Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin)是一种非常有效的细菌DNA旋转酶和人体有机阴离子转运体,作用于hOAT1,hOAT3和hOAT4,Ki分别为14.87±0.40μM, 4.77±1.12μM 和 90.50±7.50μM。

Novobiocin Sodium (NSC 2382) Chemical Structure

Novobiocin Sodium (NSC 2382) Chemical Structure

CAS: 1476-53-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1071.68 现货
50mg RMB 787.79 现货
1g RMB 5487.3 现货
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客户使用Selleck的Novobiocin Sodium (NSC 2382)发表文献13

客户使用该产品的1个实验数据

产品质控

批次: 纯度: 99.91%
99.91

Novobiocin Sodium (NSC 2382)相关产品

Antineoplastic and Immunosuppressive Antibiotics抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MELN Function assay 200 uM 18 hrs Inhibition of estradiol-induced ER-mediated transcription in MELN cells by measuring luciferase activity at 200 uM after 18 hrs 17979263
yeast PP30 Function assay 100 uM 3 hrs Inhibition of human HSP90alpha expressed in yeast PP30 cells co-expressing HSF-lacZ reporter assessed as inhibition of heat stress-induced response at 100 uM after 3 hrs 21129982
SKBR3 Function assay 1000 uM 18 hrs Inhibition of HSP90 in human SKBR3 cells assessed as aggregation of intracellular HER2 at 1000 uM after 18 hrs by DAPI staining-based immunofluorescence microscopic analysis 23859777
SH-SY5Y Neuroprotection assay 10 nM Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release at 10 nM 19138859
BL21 (DE3) pLysS Function assay 100 mins Inhibition of 6-His-tagged Mycobacterium smegmatis GyrB expressed in Escherichia coli BL21 (DE3) pLysS cells incubated for 100 mins in presence of ATP by malachite green dye based ATP assay, IC50=0.18μM 25129171
BL21 (DE3) pLysS Function assay 100 mins Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells after 100 mins by inorganic phosphate release detection based malachite green reagent assay, IC50=0.18μM 25801151
BL21 (DE3) pLysS Function assay 100 mins Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in ATPase activity incubated for 100 mins by inorganic phosphate detection assay, IC50=0.18μM 26318054
BL21 (DE3) pLysS Function assay 120 mins Inhibition of Mycobacterium smegmatis 155 6His-tagged DNA gyrase B catalytic domain ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inorganic phosphate release after 120 mins in presence of ATP by malachite green dye based, IC50=0.046μM 27371925
MCF7-MX Function assay TP_TRANSPORTER: inhibition of mitoxantrone efflux in BCRP-expressing MCF7-MX cells, IC50=25μM 16460798
SH-SY5Y Neuroprotection assay Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50=0.04839μM 19138859
SH-SY5Y Neuroprotection assay Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release 19138859
LNCaP-LN3 Antiproliferative assay Antiproliferative activity against human LNCaP-LN3 cells, IC50=1.05μM 21129982
Sf9 Function assay Inhibition of Escherichia coli His6-tagged ParC/ParE expressed in baculovirus-infected Sf9 cells by gel electrophoresis, IC50=0.21μM 21235241
点击查看更多细胞系数据

生物活性

产品描述 Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin)是一种非常有效的细菌DNA旋转酶和人体有机阴离子转运体,作用于hOAT1,hOAT3和hOAT4,Ki分别为14.87±0.40μM, 4.77±1.12μM 和 90.50±7.50μM。
靶点
Topoisomerase II [1] Topoisomerase IV [1]
体外研究(In Vitro)
体外研究活性

Novobiocin和Hsp90结合,改变分子伴侣对geldanamycin和radicicol的亲和力,造成关键调节Hsp90依赖性激酶,包括V形的Src,RAF-1,和P185(ErbB2)在体内外的损耗。Novobiocin干扰共伴侣Hsc70和p23对Hsp90的结合。[1]

Novobiocin以浓度依赖性方式特异性地抑制血红素调节eIF2alpha激酶(HRI)的成熟。Novobiocin诱导Hsp90和CDC37从未成熟HRI解离,而Hsp90的共分子伴侣P23,FKBP52,和蛋白磷酸酶5仍然与未成熟HRI相结合。[2]

Novobiocin引起特征形态和生化变化,导致细胞死亡,显示出后生动物细胞凋亡。[3]

Novobiocin,一个HSP90抑制剂,可降低SMYD3的表达并剂量依赖性抑制MDA-MB-231人乳腺癌细胞的增殖和迁移Novobiocin能抑制乳腺癌细胞的迁移,这可能涉及SMYD3的下调。[4]

Novobiocin,一个aminocoumarin抗生素,干扰了热休克蛋白90和缺氧诱导因子依赖的基因表达,从而损害了细胞的存活。Novobiocin(500 μM)导致[Ca(2 +)] i的显著增加,减少前向散射,增加膜联蛋白-V结合并增强ceramide的形成。Novobiocin刺激红细胞死亡,至少部分是因为细胞外Ca(2+)的进入和ceramide的形成。[5]

化学信息&溶解度

分子量 634.61 分子式

C31H35N2O11.Na

CAS号 1476-53-5 SDF Download Novobiocin Sodium (NSC 2382) SDF
Smiles CC1=C(C=CC2=C1OC(=O)C(=C2O)NC(=O)C3=CC(=C(C=C3)[O-])CC=C(C)C)OC4C(C(C(C(O4)(C)C)OC)OC(=O)N)O.[Na+]
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( (157.57 mM); DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : 100 mg/mL

Ethanol : 100 mg/mL

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

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)

mg/kg g μL

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Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法: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。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

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。

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