化合物 SB-505124|T2462|TargetMol

價(jià)格	￥258	￥367	￥576
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 SB-505124	英文名稱:SB-505124
CAS:694433-59-5	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.92%	產(chǎn)品類別: 抑制劑
貨號: T2462

Product Introduction

Bioactivity

名稱	SB-505124
描述	SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.
細(xì)胞實(shí)驗(yàn)	Cell viability is measured as described by Laping et al., 2002 or by using the modified tetrazolium salt WST-1. XTT assay: The cells are serum-deprived for 24 hours and then treated with SB505124 for 48 hours to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 hours with XTT labeling and electron coupling reagent according to the manufacturer's directions. Live cells with active mitochondria produce an orange-colored product, formazan, which is detected using a plate reader at between A450 nm and A500 nm with a reference wavelength greater than 600 nm. The absorbance values correlate with the number of viable cells. Modified tetrazolium salt WST-1: Approximately 2000 cells are seeded in 96-well dishes in 100 μL of 0.2% FBS phenol red-free media overnight. The cells are treated with 50 μL of SB505124 (to achieve the final concentrations indicated) for 30 minutes before being treated with or without TGF-β1 and TNF-α to a final volume of 200 μL. Cell growth is measured at the indicated time points by incubating each well with 10 μL of WST-1 for 3 hours at 37 °C. Metabolically active cells cleave WST-1 to water-soluble formazan, which is directly quantitated with an enzyme-linked immunosorbent assay plate reader. Each experiment is done at least twice, and treatment for each cell line is done in triplicate.(Only for Reference)
激酶實(shí)驗(yàn)	In Vitro Protein Kinase Assay : Kinase assays are performed as described by Laping et al., 2002 using the kinase domain of ALK5 and full-length N-terminal fused GST-Smad3. Kinase assays are performed with 65 nM GST-ALK5 and 184 nM GST-Smad3 in 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 1 mM dithiothreitol, and 3 μM ATP. Reactions are incubated with 0.5 μCi of [33P]γATP for 3 hours at 30 °C. Phosphorylated protein is captured on P-81 paper , washed with 0.5% phosphoric acid, and counted by liquid scintillation. Alternatively, Smad3 or Smad1 protein is also coated onto FlashPlate Sterile Basic Microplates. Kinase assays are then performed in FlashPlates with same assay conditions using either the kinase domain of ALK5 with Smad3 as substrate or the kinase domain of ALK6 (BMP receptor) with Smad1 as substrate. Plates are washed three times with phosphate buffer and counted by TopCount.
體外活性	在兔GFS模型中,SB505124降低了GFS手術(shù)部位的眼內(nèi)壓（IOP）水平并減少了結(jié)膜下細(xì)胞浸潤和瘢痕形成.在他克莫司（TAC）治療的小鼠和FK12EC KO小鼠中,SB505124抑制內(nèi)皮細(xì)胞TGF-β受體的活化和腎小動(dòng)脈玻璃樣變性的誘導(dǎo).
體內(nèi)活性	SB505124被鑒定為ALK4和ALK5的可逆ATP競爭性和選擇性ALK抑制劑。SB-505124抑制緊密相關(guān)的ALK4,IC50為129 nM,選擇性比作用于ALK5低2.5倍。SB-505124濃度高達(dá)10 μM時(shí)也不抑制ALK2。SB-505124抑制COS-1細(xì)胞內(nèi)源性Smad2磷酸化。ALK4和ALK5激活Smad1和Smad2,加入SB-505124抑制激活。SB-505124作用于HepG2人類肝癌細(xì)胞,C2C12小鼠成肌細(xì)胞和Mv1Lu水貂肺細(xì)胞,濃度依賴性抑制轉(zhuǎn)化生長因子-β誘導(dǎo)的Smad2磷酸化。SB-505124有效抑制轉(zhuǎn)化生長因子-β和活化素誘導(dǎo)CAGA12-熒光素酶和ARE-熒光素酶受體結(jié)構(gòu)的活力,這種作用存在濃度依賴性。在人臍靜脈內(nèi)皮細(xì)胞（HUVEC）中,SB505124（500 nM）阻斷TGF-β1對F-actin組裝的影響,并阻止TGF-β誘導(dǎo)的ROS產(chǎn)生。
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 50 mg/mL (149.08 mM), Sonication is recommended. 1eq. HCl : 33.5 mg/mL (100 mM)
關(guān)鍵字	SB505124 \| SB-505124 \| SB 505124 \| Transforming growth factor beta receptors \| TGF-β Receptor \| 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	抑制劑庫 \| 抗癌活性化合物庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| 細(xì)胞因子抑制劑庫 \| 激酶抑制劑庫 \| 抗肥胖化合物庫 \| TGF-β/Smad靶點(diǎn)化合物庫 \| 膜蛋白靶向化合物庫 \| 酪氨酸激酶分子庫

關(guān)鍵字： SB-505124|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （12年）	注冊資本	566.265100萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(yè)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：12年
注冊資本：566.265100萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場三路238號8樓

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