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MRT67307

SKU: orb1310941

Description

MRT67307 is a potent kinase inhibitor targeting TBK1, IKKε, SIKs, and ULK1/2, thereby blocking autophagy. It modulates innate immune responses in macrophages by suppressing IRF3 phosphorylation and IFN-β while enhancing TLR-induced IL-10 and IL-1ra. This tool compound is widely used in autophagy and immunology research, applicable in both in vitro and in vivo experimental models.
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Research Area

Cell Biology, Signal Transduction

Images & Validation

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MRT67307

Key Properties

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CAS Number1190378-57-4
MW464.6
Purity99.84% (May vary between batches)
FormulaC26H36N6O2
SMILESO=C(NCCCNc1nc(Nc2cccc(CN3CCOCC3)c2)ncc1C1CC1)C1CCC1
TargetAutophagy,IκB/IKK
SolubilityEthanol:83 mg/mL (178.65 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.1 mM);DMSO:120 mg/mL (258.29 mM)

Bioactivity

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Target IC50
ULK1:45 nM|ULK2:38 nM|TBK1:190 nM|IKKϵ: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. 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.
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Cell Research
Cells are rinsed in ice-cold PBS and extracted in lysis buffer (50 mM Tris·HCl at pH 7.4, 1 mM EDTA, 1 mM EGTA, 50 mM NaF, 5 mM sodium pyrophosphate, 10 mM sodium β-glycerol 1-phosphate, 1 mM DTT, 1 mM sodium orthovanadate, 0.27mol/Lsucrose, 1% (vol/vol) Triton X-100, 1 μg/mL aprotinin, 1 μg/ mL leupeptin, and 1 mM phenylmethylsulphonyl fluoride). Cell extracts are clarified by centrifugation at 14,000 × g for 10 min at 4°C, and protein concentrations are determined by using the Bradford assay. FLAG-CRTC3 is purified on anti-FLAG M2 agarose, whereas endogenous CRTC3 is immunoprecipitated from cell extracts by using anti-CRTC3 raised against the peptide CWKEEKHPGFR (S277D bleed 2) and coupled to Protein GSepharose. To detect proteins in cell lysates, 20 μg of protein extract is separated by SDS/PAGE. After transfer to PVDF membranes, proteins are detected by immunoblotting and visualized by treating the blots with ECL followed by autoradiography. The following antibodies are used for immunoblotting: pSer133 CREB, pSer171 CRTC2, total CRTC2, GAPDH, total STAT3, pTyr705 STAT3, FLAG (M2 clone), CRTC3, HA (3F10), and 14-3-3; and antibodies against pSer329 (S256D bleed 2) and pSer370 (S253D bleed 2) of CRTC3 are raised against the phosphopeptides GLQSSRpSNPSIQ and RLFSLpSNPSLST.
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Storage & Handling

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Storagekeep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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IκB, IkB, IkB/IKK, IKK, IKKϵ, IKKε, MRT 67307, MRT67307, MRT-67307, MRT67307 HCl, Autophagy, ULK2, ULK1, ULK, transduction, signal, TBK1, TBK-1

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Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
44464263 ↗

Key Properties

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No computed properties available.

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MRT67307 (orb1310941)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 120.00
5 mg
$ 120.00
10 mg
$ 170.00
25 mg
$ 300.00
50 mg
$ 530.00
100 mg
$ 740.00
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