MRT67307 HCl

Catalog No.S7948 Batch:S794802

Technical Data

Formula

C₂₆H₃₆N₆O₂· xHCl

Molecular Weight

464.6 (free-base)

CAS No.

1781882-89-0

Solubility (25°C)*

In vitro

DMSO

100 mg/mL

Water

100 mg/mL

Ethanol

10 mg/mL

In vivo (Add solvents to the product individually and in order)

Clear solution	saline	100.000mg/ml (215.24mM)	Taking the 1 mL working solution as an example, add 100 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
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.

* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

Targets

TBK1 ^[1] (Cell-free assay)	IKKϵ ^[1] (Cell-free assay)
19 nM	160 nM

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]

Protocol (from reference)

Kinase Assay:^{^[1]}	Protein kinase assays 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.
Cell Assay:^[3]	Cell lines MEFs and 293T cells Concentrations 10 μM Incubation Time 1 h Method 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.

Kinase Assay:^{^[1]}

Protein kinase assays
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.

Cell Assay:^[3]

Cell lines
MEFs and 293T cells
Concentrations
10 μM
Incubation Time
1 h
Method
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.

References

Customer Product Validation

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

: Data from [ , , Mol Med Rep, 2018, 17(2):3085-3091 ]

Selleck's MRT67307 HCl has been cited by 19 publications

TLR4 endocytosis and endosomal TLR4 signaling are distinct and independent outcomes of TLR4 activation [ EMBO Rep, 2025, 10.1038/s44319-025-00444-2]	PubMed: 40204912
TBK1-Zyxin signaling controls tumor-associated macrophage recruitment to mitigate antitumor immunity [ EMBO J, 2024, 10.1038/s44318-024-00244-9]	PubMed: 39304793
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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.