化合物 RepSox|T6337

3篇文獻(xiàn)

價(jià)格	￥222	￥297	￥497
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:化合物 RepSox	英文名稱:RepSox
CAS:446859-33-2	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.62%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T6337

Product Introduction

Bioactivity

名稱	RepSox
描述	RepSox (ALK5 Inhibitor II) is a TGFβR-1/ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23/4 nM). RepSox induces adipogenesis in MEFs cells.
細(xì)胞實(shí)驗(yàn)	RepSox is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 1%) before use[1]. To test anti-TGF-β activity of compounds, HepG2 cells are seeded in 96 well microplates at a concentration of 35000 cells per well in 200 μL of serum-containing medium. The microplates are then placed for 24 h in a cell incubator at 37°C, 5% CO2 atm. RepSox dissolved in DMSO are then added at concentrations of 50 nM to 10 μM (final concentration of DMSO 1%) for 30 min prior to the addition of recombinant TGF-β (1 ng/mL). After an overnight incubation, the cells are washed with PBS and lysed by addition of 10 μL of passive lysis buffer. Inhibition of luciferase activity relative to control groups is used as a measure of compound activity. A concentration?response curve is constructed from which an IC50 value is determined graphically[1].
激酶實(shí)驗(yàn)	The kinase domain of ALK5 is cloned by PCR and expressed in a baculovirus/Sf9 cells system. The protein is 6-His tagged in the C terminus and purified by affinity chromatography using a Ni2+column, and the obtained material is used to assess compound activity in an autophosphorylation assay. Purified enzyme (10 nM) is incubated in 50 μL of Tris buffer (Tris 50 mM, pH 7.4; NaCl, 100 mM; MgCl2, 5 mM; MnCl2, 5 mM; and DTT, 10 mM). The enzyme is preincubated with different concentrations of RepSox (0.1% DMSO final concentration in the test) for 10 min at 37°C. The reaction is then initiated by the addition of 3 μM ATP (0.5 μCi γ-33P-ATP). After 15 min at 37°C, phosphorylation is stopped by the addition of SDS?PAGE sample buffer (50 mM Tris-HCl, pH 6.9, 2.5% glycerol, 1% SDS, and 5% β-mercaptoethanol). The samples are boiled for 5 min at 95°C and run on a 12% SDS?PAGE. Dried gels are exposed to a phosphor screen overnight. ALK5 autophosphorylation is quantified using a Storm imaging system[1].
體外活性	方法：小鼠胚胎成纖維細(xì)胞 MEFs 用 RepSox (10 μM) 處理 10 天，使用 oil red O 染色檢測(cè)細(xì)胞脂肪。結(jié)果：RepSox 處理的 MEFs 中出現(xiàn)了許多脂肪細(xì)胞樣細(xì)胞，脂滴的 oil red O 染色證實(shí)了脂肪細(xì)胞分化。[1] 方法：綿羊成纖維細(xì)胞用 RepSox (10-25 nM) 處理 3 天，使用顯微鏡觀察細(xì)胞形態(tài)。結(jié)果：在 RepSox 處理三天后，綿羊成纖維細(xì)胞獲得了顯著不同的形態(tài)，并從紡錘形轉(zhuǎn)變?yōu)榫哂懈嗑凼募?xì)長(zhǎng)形狀。[2]
體內(nèi)活性	方法：為檢測(cè)對(duì)腸內(nèi)神經(jīng)膠質(zhì)細(xì)胞 EGCs 分化的影響，將 RepSox (3-10 mg/kg in 0.5% CMC-Na) 腹腔注射給 GFAP-Cre:Rosa26-tdTomato 小鼠，每天一次，持續(xù)兩周。結(jié)果：RepSox 可以促進(jìn) EGCs 轉(zhuǎn)化為神經(jīng)元，并改善體內(nèi)胃腸道運(yùn)動(dòng)。[3] 方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 RepSox (5-20 mg/kg) 腹腔注射攜帶骨肉瘤 143B 的 nude 小鼠模型，每?jī)商煲淮?，持續(xù)三周。結(jié)果：RepSox 有效地抑制了骨肉瘤的生長(zhǎng)，并且在裸鼠中具有低毒性。[4]
存儲(chǔ)條件	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 15 mg/mL (52.21 mM), Sonication is recommended.
關(guān)鍵字	TGF-β Receptor \| E 616452 \| E616452 \| RepSox \| SJN2511 \| Transforming growth factor beta receptors \| SJN-2511 \| Inhibitor \| inhibit
相關(guān)產(chǎn)品	Monocrotaline \| Pirfenidone \| Ceritinib \| A 83-01 \| Chromenone 1 \| LY-364947 \| BMP signaling agonist sb4 \| Alectinib hydrochloride \| SB-431542 \| Galunisertib \| Alantolactone \| Hydrochlorothiazide
相關(guān)庫(kù)	抑制劑庫(kù) \| 血管生成庫(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) \| 抗肝癌化合物庫(kù) \| 癌細(xì)胞分化化合物庫(kù) \| TGF-β/Smad靶點(diǎn)化合物庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 酪氨酸激酶分子庫(kù)

關(guān)鍵字： SJN 2511|||E-616452|||ALK5 Inhibitor II|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(zhuān)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(xiāo)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(lèi)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 （12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）

VIP 12年

公司成立：12年
注冊(cè)資本：566.2651萬(wàn)人民幣
企業(yè)類(lèi)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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