鹽酸MRT68921|T5356|TargetMol

價(jià)格	￥262	￥588	￥925
包裝	1mg	5mg	10mg

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:鹽酸MRT68921	英文名稱:MRT68921 HCl
CAS:2070014-87-6	品牌: TargetMol
產(chǎn)地: 美國(guó)	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: 99.86%	產(chǎn)品類別: 抑制劑
貨號(hào): T5356

Product Introduction

Bioactivity

名稱	MRT68921 HCl
描述	MRT68921 hydrochloride is a potent inhibitor of both ULK1 and ULK2 (IC50s: 2.9 and 1.1 nM, respectively).
細(xì)胞實(shí)驗(yàn)	Immortalized wild-type mouse embryonic fibroblasts (MEFs) have been described previously. MEFs and 293T cells were grown in DMEM, supplemented with 10% fetal bovine serum and penicillin/streptomycin, and cultured at 37 °C, 5% CO2. For induction of autophagy, cells were typically grown to 75% confluency, washed twice, and incubated in Earle's balanced salt solution (EBSS) for 1 h (or complete medium as a control) unless indicated. MRT67307 (10 μM), MRT68921 (1 μM), AZD8055 (1 μM), or bafilomycin A1 (50 nM) was included where indicated. Transfection and transduction were as described [1].
激酶實(shí)驗(yàn)	Initial ULK1 kinase assays were performed with GST-ULK1, produced in Sf9 cells. For other experiments, recombinant GST-ULK1 (wild type, kinase-dead (K46I), and M92T and M92Q) was expressed in 293T cells, purified, and eluted from a glutathione-Sepharose column. Kinase assays were carried out in 50 mM Tris-HCl, pH 7.4, 10 mM magnesium acetate, 0.1 mM EGTA, and 0.1% β-mercaptoethanol, containing 30 μM cold ATP, and 0.5 μCi of [γ-32P]ATP for 5 min at 25 °C. Prior to ATP addition, reaction mixes were prewarmed to 25 °C for 5 min. Reactions were stopped by the addition of sample buffer, followed by SDS-PAGE, transfer to nitrocellulose, and analysis by autoradiography and immunoblot. For IC50 curve measurements, kinase assays were performed, using myelin basic protein as a substrate [1].
體外活性	MRT68921 is the most potent inhibitor of both ULK1 and ULK2, with greater than a 15-fold reduction in the IC50 for ULK1 (2.9 nM) and greater than a 30-fold reduction for ULK2 (1.1 nM). MRT68921 (1 μM) was sufficient to reduce phospho-ATG13 to control levels, and in line with the in vitro IC50 values [1]. Pre-incubating the cells for 30 min with the ULK1 inhibitor MRT68921 at the optimal concentration of 100 nM prevented the forskolin-induced CYTO-ID staining. The same effect was observed with siRNA against ULK1 [2].
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 4.71 mg/mL (10 mM), Sonication is recommended. H2O : 10 mg/mL
關(guān)鍵字	MRT68921 HCl \| MRT-68921 HCl
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相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 自噬庫(kù) \| 激酶抑制劑庫(kù) \| 抗COVID-19化合物庫(kù) \| 表型篩選靶點(diǎn)鑒定庫(kù)

關(guān)鍵字：鹽酸MRT68921|TargetMol

公司簡(jiǎn)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(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)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(kù)，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(tái)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。

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公司成立：12年
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