Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
MRT67307 (MRT-67307; MRT 67307) is a novel and potent inhibitor for multiple kinases such as TBK1, IKKε , MARK1-4 and NUAK1 with potential antineoplastic activity. It inhibits TBK1, IKKε , MARK1-4 and NUAK1 with IC50s of 19, 160, 27-52 and 230nM, respectively.
ln Vitro |
MRT67307 inhibits TBK1 and IKKε in vitro at 0.1 mM ATP with IC50 values of 160 and 19 nM, respectively, but not IKKα or IKKβ, not even at 10 μM [1]. MRT67307 (2 μM) inhibits bone marrow-derived macrophages (BMDM) from phosphorylating IRF3. Poly (I:C) does not prevent JNK or p38 MAPK from being activated by MRT67307 (2 μM)[1]. MRT67307 (1 nM–10 μM) inhibits macrophages' ability to produce IFNβ [1]. It just takes 10 μM of MRT67307 to bring phosphorylated ATG13 down to control levels [2]. In mouse embryonic fibroblasts (MEFs), autophagy is inhibited by MRT67307 (10 μM) [2]. In 293T cells, TBK1/IKKε-induced CYLD phosphorylation is eliminated by MRT67307 (5 μM; 4 h) [3].
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ln Vivo |
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Cell Assay |
Western Blot Analysis[3]
Cell Types: 293T cells Tested Concentrations: 5 µM Incubation Duration: 4 hrs (hours) Experimental Results: Abrogated TBK1/IKKε-induced CYLD phosphorylation. |
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Animal Protocol |
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References |
[1]. Clark K, et al. Novel cross-talk within the IKK family controls innate immunity. Biochem J. 2011 Feb 15;434(1):93-104.
[2]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. [3]. Zhu Z, et al. Inhibition of KRAS-driven tumorigenicity by interruption of an autocrine cytokine circuit. 26.37Cancer Discov. 2014 Apr;4(4):452-65. |
Molecular Formula |
C26H36N6O2
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Molecular Weight |
464.6 (free-base)
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CAS # |
1190378-57-4
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Related CAS # |
MRT67307 hydrochloride;2095432-39-4;MRT67307 dihydrochloride;1781882-89-0
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SMILES |
O=C(NCCCNC1=NC(NC2=CC=CC(CN3CCOCC3)=C2)=NC=C1C4CC4)C5CCC5
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
MRT67307 and MRT68921 inhibit ULK and block autophagy in cells.J Biol Chem.2015 May 1;290(18):11376-83. th> |
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MRT68921 specifically blocks autophagic flux through ULK1 inhibition.J Biol Chem.2015 May 1;290(18):11376-83. td> |
ULK inhibition also disrupts autophagosome maturation.J Biol Chem.2015 May 1;290(18):11376-83. td> |