格爾德霉素|T6343|TargetMol

8篇文獻(xiàn)

價(jià)格	￥413	￥593	￥987
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2026-05-08

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產(chǎn)品詳情

中文名稱:格爾德霉素	英文名稱:Geldanamycin
CAS:30562-34-6	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Keep away from direct sunlight,Keep away from moisture Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
純度規(guī)格: 99.16%	產(chǎn)品類別: 抑制劑
貨號(hào): T006\|T6343

Product Introduction

Bioactivity

名稱	Geldanamycin
描述	Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR)/HSP association.
細(xì)胞實(shí)驗(yàn)	Exponentially growing cells are treated with Geldanamycin and at various times DNA synthesis is assessed by incorporation of bromodeoxyuridine (BrdUrd) and flow cytometric analysis. No marked difference in total cell number is noted during this time course for treated and untreated cultures. BrdUrd (10 μM) is incorporated over a 4-h incubation period at 37 °C and cells are harvested and fixed in 70% ethanol. After denaturation of the DNA with 2 N HC1, cells are incubated with an anti-BrdUrd mouse monoclonal antibody followed by a fluorescein isothiocyanate (FITC)-linked goat anti-mouse IgG. Cells are stained for 30 minutes at room temperature with propidium iodide and analysed by flow cytometry using a Coulter EPICS Profile Analyzer. (Only for Reference)
激酶實(shí)驗(yàn)	Isothermal Titration Calorimetry (ITC) of Nucelotide Binding: The titration experiments are performed using the MSC system. In each experiment, 16 aliquots of 15 μL of geldanamycin (300 μM in 1% DMSO) are injected into 1.3 mL of protein (31 μM in 20 mMTris-HCl, pH 7.5, 1 mMEDTA) at 25 °C, and the resulting data are fit after subtracting the heats of dilution. Heats of dilution are determined in separate experiments from addition of geldanamycin into buffer and buffer into protein. No evidence for binding of DMSO in the nucleotide binding site is observed. Titration data are fit using a nonlinear least-squares curve-fitting algorithm with three floating variables: stoichiometry, binding constant (Kb) 1/Kd), and change of enthalpy of interaction (ΔH°). Dissociation constants estimated for geldanamycin binding to intact yeast Hsp90 is 1.22 μM, and for binding to Hsp90 N-terminal domain is 0.78 μM. No meaningful heat is observed with binding to the C-terminal fragment.
體外活性	Geldanamycin通過(guò)與Hsp90s N-末端結(jié)構(gòu)域（殘基1-220）中的ATP結(jié)合位點(diǎn)結(jié)合，劑量依賴性地抑制Hsp90的ATP酶活性。[1] 在A2780人類卵巢細(xì)胞系中，Geldanamycin引起劑量依賴的G2階段阻滯和S期進(jìn)入的可逆抑制，該抑制伴隨p53的增加，并最終證明是依賴于p53的。[2] Geldanamycin導(dǎo)致p185受體蛋白酪氨酸激酶的多泛素化和蛋白酶體降解，顯示出70 nM的IC50。[3, 4] 作為典型的抗腫瘤試劑，Geldanamycin對(duì)60種人類腫瘤細(xì)胞系的平均GI50為0.18 μM。[5]
體內(nèi)活性	Geldanamycin（50 mg/kg）在FRE/erbB-2小鼠中對(duì)pl85相關(guān)的磷酸化酪氨酸水平顯示出30%的抑制作用。[6]
存儲(chǔ)條件	Keep away from direct sunlight,Keep away from moisture Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 49 mg/mL (87.4 mM), Heating is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字	TyrosineKinases \| Tyrosine Kinases \| p185 \| NSC-122750 \| NSC122750 \| Inhibitor \| inhibit \| InfluenzaVirus \| Influenza Virus \| HSP90 \| HSP \| Heat shock proteins \| Geldanamycin \| Bacterial \| Antibiotic
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相關(guān)庫(kù)	抑制劑庫(kù) \| 微生物天然產(chǎn)物庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 激酶抑制劑庫(kù) \| 抗癌天然產(chǎn)物庫(kù) \| 抗病毒庫(kù) \| 天然產(chǎn)物庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 酪氨酸激酶分子庫(kù) \| 高通量篩選天然產(chǎn)物庫(kù) \| 抗感染天然產(chǎn)物庫(kù)

關(guān)鍵字：格爾德霉素;NSC 122750;TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過(guò)在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過(guò)五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （14年）	注冊(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國(guó)（陶術(shù)生物）

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公司成立：14年
注冊(cè)資本：566.2651萬(wàn)人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場(chǎng)三路28號(hào)4樓

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