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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26H36N6O2· xHCl |
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分子量 | 464.6 (free-base) | CAS No. | 1781882-89-0 | |
Solubility (25°C)* | 体外 | DMSO | 92 mg/mL warmed with 50ºC water bath | |
Water | 92 mg/mL | |||
Ethanol | 92 mg/mL | |||
* <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. |
製品説明 | MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy. |
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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. [1] 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. [2] In addition, MRT67307 inhibit ULK and block autophagy in MEF cells. [3] |
キナーゼアッセイ | Protein kinase assays | |
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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. |
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, , Methods Enzymol. 2017, 587:391-404
Data from [Data independently produced by , , Mol Med Rep, 2018, 17(2):3085-3091]
mRNAs encoding self-DNA reactive cGAS enhance the immunogenicity of lipid nanoparticle vaccines [ mBio, 2023, 10.1128/mbio.02506-23] | PubMed: 37937842 |
A Chemical Proteomics Approach to Discover Regulators of Innate Immune Signaling [ Viruses, 2023, 15(5)1112] | PubMed: 37243198 |
Thymosin α-1 Reverses M2 Polarization of Tumor-Associated Macrophages during Efferocytosis [ Cancer Res, 2022, 82(10):1991-2002] | PubMed: 35364609 |
Revisiting the Mongolian Gerbil Model for Hepatitis E Virus by Reverse Genetics [ Microbiol Spectr, 2022, e0219321] | PubMed: 35230152 |
Human TBK1 deficiency leads to autoinflammation driven by TNF-induced cell death [ Cell, 2021, S0092-8674(21)00885-0] | PubMed: 34363755 |
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 |
Deubiquitinase USP35 restrains STING-mediated interferon signaling in ovarian cancer [ Cell Death Differ, 2020, 10.1038/s41418-020-0588-y] | PubMed: 32678307 |
HSV-1 and Zika Virus but Not SARS-CoV-2 Replicate in the Human Cornea and Are Restricted by Corneal Type III Interferon [ Cell Rep, 2020, 33(5):108339] | PubMed: 33147451 |
SARS-CoV-2 Infects Human Engineered Heart Tissues and Models COVID-19 Myocarditis [ bioRxiv, 2020, 2020.11.04.364315] | PubMed: 33173875 |
Spatiotemporal Control of ULK1 Activation by NDP52 and TBK1 during Selective Autophagy [ Mol Cell, 2019, 74(2):347-362.e6] | PubMed: 30853401 |
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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