MRT68921 HCl

製品コードS7949 バッチS794904

印刷

化学情報

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）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.500mg/ml (1.15mM)	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.
Clear solution	5% DMSO 1 95% corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.500mg/ml (1.15mM)	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.

* <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
キナーゼアッセイ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/25833948/
https://pubmed.ncbi.nlm.nih.gov/32873786/

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：

Excessive autophagic degradation of MYLK3 causes sunitinib-induced cardiotoxicity [ Autophagy, 2025, 1-20.]	PubMed: 40568844
Inhibiting autophagy selectively prunes dysfunctional tumor vessels and optimizes the tumor immune microenvironment [ Theranostics, 2025, 15(1):258-276]	PubMed: 39744218
Image-based temporal profiling of autophagy-related phenotypes [ Autophagy Rep, 2025, 4(1)2484835]	PubMed: 40291494
Exposure of the inner mitochondrial membrane triggers apoptotic mitophagy [ Cell Death Differ, 2024, 10.1038/s41418-024-01260-2]	PubMed: 38396150
Synthetic lethality of combined ULK1 defection and p53 restoration induce pyroptosis by directly upregulating GSDME transcription and cleavage activation through ROS/NLRP3 signaling [ J Exp Clin Cancer Res, 2024, 43(1):248]	PubMed: 39215364
Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728]	PubMed: 39264808
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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。