MRT68921 HCl

製品コードS7949 バッチS794904

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H34N6O·xHCl
分子量 434.58 (free base) CAS No. 2070014-87-6
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 10 mg/mL
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 95% corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
in vitro

MRT68921 specifically disrupts autophagosome maturation and thus blocks autophagic flux through ULK1 inhibition. [1]
in vivo

MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ Kinase Assays
Initial ULK1 kinase assays are performed with GST-ULK1, produced in Sf9 cells, which is described on the MRC-PPU Reagents website. For other experiments, recombinant GST-ULK1 (wild type, kinase-dead (K46I), and M92T and M92Q) is expressed in 293T cells, purified, and eluted from a glutathione-Sepharose column. Kinase assays are 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 are prewarmed to 25 °C for 5 min. Reactions are stopped by the addition of sample buffer, followed by SDS-PAGE, transfer to nitrocellulose, and analysis by autoradiography and immunoblot.
細胞アッセイ 細胞株 MEFs and 293T cells
濃度 1 μM
反応時間 1 h
実験の流れ

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) in the presence or absence of 10 μM MRT67307, 1 μM MRT68921, or 50 nM bafilomycin A1 and followed by lysis and immunoblotting with the indicated antibodies.
動物実験 動物モデル Female BALB/c mice
投薬量 20 mg/kg
投与方法 s.c.

カスタマーフィードバック

, , Methods Enzymol. 2017, 587:391-404

Data from [Data independently produced by , , Mol Carcinog, 2018, 57(3):319-332]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Exposure of the inner mitochondrial membrane triggers apoptotic mitophagy [ Cell Death Differ, 2024, 10.1038/s41418-024-01260-2] PubMed: 38396150
Chronic hypoxia stabilizes 3βHSD1 via autophagy suppression [ Cell Rep, 2024, 43(1):113575] PubMed: 38181788
ATG7/GAPLINC/IRF3 axis plays a critical role in regulating pathogenesis of influenza A virus [ PLoS Pathog, 2024, 20(1):e1011958] PubMed: 38227600
ULK2 Is a Key Pro-Autophagy Protein That Contributes to the High Chemoresistance and Disease Relapse in FLT3-Mutated Acute Myeloid Leukemia [ Int J Mol Sci, 2024, 25(1)646] PubMed: 38203816
TECPR1 is activated by damage-induced sphingomyelin exposure to mediate noncanonical autophagy [ EMBO J, 2023, 42(17):e113105] PubMed: 37409525
Phosphorylation of phase-separated p62 bodies by ULK1 activates a redox-independent stress response [ EMBO J, 2023, e113349.] PubMed: 37306101
PROX1 induction by autolysosomal activity stabilizes persister-like state of colon cancer via feedback repression of the NOX1-mTORC1 pathway [ Cell Rep, 2023, S2211-1247(23)00530-2] PubMed: 37224811
Tubeimoside-2 Triggers Methuosis in Hepatocarcinoma Cells through the MKK4-p38α Axis [ Pharmaceutics, 2023, 15(4)1093] PubMed: 37111582
mTOR inhibition attenuates chemosensitivity through the induction of chemotherapy resistant persisters [ Nat Commun, 2022, 13(1):7047] PubMed: 36396656
Autophagy and lipid droplets are a defense mechanism against toxic copper oxide nanotubes in the eukaryotic microbial model Tetrahymena thermophila [ Sci Total Environ, 2022, 847:157580] PubMed: 35882336

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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