计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 2 篇同行评审文献引用。
概述
λmax 305(MeOH)(Lit.) A benzoquinoid antibiotic that inhibits p60c-src tyrosine kinase and c-myc gene expression in murine lymphoblastoma cells. Geldanamycin has antiproliferative and antitumor effects. Rapidly depletes p185c-erbB2 protein tyrosine kinase in breast carcinoma cells. Binds to HSP90 and disrupts Raf1-HSP90 complex leading to destabilization of Raf1. Inhibits basal and hypoxia-induced expression of c-Jun (IC50 = 75 nM) and abolishes hypoxia-induced increase in c-Jun N-terminal kinase activity. Also known to selectively destabilize mutated p53 protein from a number of breast, leukemia, and prostate cell lines. A benzoquinoid antibiotic that is a potent inhibitor of pp60src tyrosine kinase. Geldanamycin has antiproliferative and antitumor effects. Inhibits basal and hypoxia-induced expression of c-Jun (IC50 = 75 nM) and abolishes hypoxia-induced increase in c-Jun N-terminal Kinase activity. Binds to HSP90 and disrupts raf1-HSP90 complex leading to destabilizing of Raf1. Also destabilizes mutant p53 protein from a number of breast, leukemic, and prostate cell lines. Inhibits c-myc expression in murine lymphoblastoma cells. Approximately ten-fold more potent than herbimycin A
Information
Geldanamycin (NSC 122750) Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with K d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARD
In vitro
Geldanamycin binds in the ATP-binding site in the N-terminus domain of Hsp90s (residues 1-220). Geldanamycin inhibits the ATPase activity of Hsp90 in a dose-dependent manner. Geldanamycin causes a dose-dependent G2 arrest and reversible inhibiton o f entry into the S phase in A2780 human ovarian cell line. This inhibition is accompanied by p53 increase and finally demonstrated to be p53 dependent. Geldanamycin causes polyubiquitination and proteasomal degradation of the p185 receptor protein-tyrosin kinase and shows a IC50 with 70 nM. [3, 4] Geldanamycin is a typical anti-tumor reagent, shows a mean GI50 with 0.18 μM against the panel of 60 human tumor cell lines.
In vivo
Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice.
Cell Data
cell lines：MDA-MB-468, MCF-7, HCC1954, MDA-MB-231, SKBr-3, Cal-51, and BT-20 breast cancer cells
Concentrations：0.001-10 μM
Incubation Time：3 hours
Powder Purity:≥97%
规格
英文别名
2-Azabicyclo[16.3.1]docosa-4,6,10,18,21-pentaene-3,20,22-trione, 9,13-dihydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-, 9-carbamate
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Geldanamycin (NSC 122750)
生化机理
格尔德霉素（NSC 122750）是一种现有的天然 HSP90 抑制剂，其Kd值为 1.2 μM，可特异性地破坏糖皮质激素受体（GR）/HSP 关联。格尔德霉素可通过减少宿主的炎症反应来减轻病毒感染引起的急性肺损伤（ALI）/急性呼吸窘迫综合征（ARDS）。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
热休克蛋白 90 alpha 家族 B 类成员 1 抑制剂
名称和识别符
EC号
805-356-8
分子类型
小分子
Isomeric SMILES
C[C@H]1C[C@@H]([C@@H]([C@H](/C=C(/[C@@H]([C@H](/C=C\C=C(\C(=O)NC2=CC(=O)C(=C(C1)C2=O)OC)/C)OC)OC(=O)N)\C)C)O)OC
关联CAS
MeSH Entry Terms
geldanamycin;geldanomycin
分子量
560.64
Reaxy-Rn
26145919
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26145919&ln=
技术文档
高级数据
关联靶点（人）
TRAP1
Tchem
热休克蛋白 75 kDa，线粒体(Heat shock protein 75 kDa, mitochondrial)
(1 活性数据)
HSP90AA1
Tchem
热休克蛋白 HSP 90-alpha(Heat shock protein HSP 90-alpha)
(20 活性数据)
HSP90AB1
Tchem
热休克蛋白 HSP 90-beta(Heat shock protein HSP 90-beta)
(8 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 62 mg/mL warmed with 50ºC Water: bath (102.19 mM); Water: Insoluble; Ethanol: Insoluble;
熔点
255°C
安全和危险性（GHS）
WGK Germany
2
RTECS
LX8920000
个人防护装备
Eyeshields,Gloves,type N95 (US),type P1 (EN143) respirator filter
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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