MRT67307 HCl

製品コードS7948 バッチS794801

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

C₂₆H₃₆N₆O₂· xHCl

分子量

464.6 (free-base)

CAS No.

1781882-89-0

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

92 mg/mL

Water

92 mg/mL

Ethanol

92 mg/mL

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。	4.600mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 92 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of 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。	0.770mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 15.4 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	MRT67307 は、IC50 がそれぞれ 160 nM および 19 nM の強力なデュアル IKKϵ および TBK1 阻害剤です。MRT67307 は ULK1 および ULK2 を強力に阻害し、オートファジーをブロックします。
in vitro	In macrophages, MRT67307 prevents the phosphorylation of IRF3 and the production of IFNβ. In wild-type MEFs, MRT67307 enhances the IL-1-stimulated phosphorylation of p105 at Ser933 and RelA at both Ser468 and Ser536, and also enhances IL-1-stimulated activation of NF-κB-dependent gene transcription. MRT67307 increases IL-10 production and suppresses proinflammatory cytokine production via a cAMP response element-Binding protein (CREB)-regulated transcriptional coactivator (CRTC) 3 Dependent Mechanism. In addition, MRT67307 inhibit ULK and block autophagy in MEF cells.

製品説明

MRT67307 は、IC50 がそれぞれ 160 nM および 19 nM の強力なデュアル IKKϵ および TBK1 阻害剤です。MRT67307 は ULK1 および ULK2 を強力に阻害し、オートファジーをブロックします。

in vitro

In macrophages, MRT67307 prevents the phosphorylation of IRF3 and the production of IFNβ. In wild-type MEFs, MRT67307 enhances the IL-1-stimulated phosphorylation of p105 at Ser933 and RelA at both Ser468 and Ser536, and also enhances IL-1-stimulated activation of NF-κB-dependent gene transcription. MRT67307 increases IL-10 production and suppresses proinflammatory cytokine production via a cAMP response element-Binding protein (CREB)-regulated transcriptional coactivator (CRTC) 3 Dependent Mechanism. In addition, MRT67307 inhibit ULK and block autophagy in MEF cells.

プロトコル(参考用のみ)

キナーゼアッセイ	Protein kinase assays
キナーゼアッセイ	Substrates and kinases are diluted in 50 mM Tris/HCl (pH 7.5), 0.1% 2-mercaptoethanol, 0.1 mM EGTA and 10 mM magnesium acetate. Reactions are initiated with [γ-³²P]ATP (2500 c.p.m./pmol) to a final concentration of 0.1 mM and terminated after 15 min at 30 °C by the addition of SDS and EDTA (pH 7.0) to final concentrations of 1.0% (w/v) and 20 mM respectively. After heating for 5 min at 100 °C and separation by SDS/PAGE, the phosphorylated proteins are detected by autoradiography.
細胞アッセイ	細胞株	MEFs and 293T cells
	濃度	10 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.

参考

https://pubmed.ncbi.nlm.nih.gov/21138416/
https://pubmed.ncbi.nlm.nih.gov/23033494/
https://pubmed.ncbi.nlm.nih.gov/25833948/

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 Med Rep, 2018, 17(2):3085-3091]

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：

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Type I Interferon Regulates a Coordinated Gene Network to Enhance Cytotoxic T Cell-Mediated Tumor Killing. [ Cancer Discov, 2020, 10(3):382-393]	PubMed: 31974171
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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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