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NF-Κb IκB/IKK MRT67307 HCl (1190378-57-4(free base))

MRT67307 HCl (1190378-57-4(free base))

Catalog No. T5162   CAS T5162

MRT67307 is a kinase inhibitor of TBK1, MARK1-4, IKKε, and NUAK1 (IC50: 19, 27-52, 160, and 230 nM, respectively).

MRT67307 HCl (1190378-57-4(free base)), CAS T5162
Pack Size Availability Price/USD Quantity
2 mg In stock 50.00
5 mg In stock 69.00
10 mg In stock 115.00
25 mg In stock 264.00
50 mg In stock 476.00
100 mg In stock 596.00
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Purity 98.52%
Biological Description
Chemical Properties
Storage & Solubility Information
Description MRT67307 is a kinase inhibitor of TBK1, MARK1-4, IKKε, and NUAK1 (IC50: 19, 27-52, 160, and 230 nM, respectively).
Targets&IC50 IKK? : ic50 160 nM (cell free) ,   TBK1 : ic50 19 nM (cell free) ,   ULK1 : ic50 45 nM (cell free) ,   ULK2 : ic50 38 nM (cell free)
Kinase Assay Substrates and kinases were diluted in 50 mM Tris/HCl (pH 7.5), 0.1% 2-mercaptoethanol, 0.1 mM EGTA and 10 mM magnesium acetate. Reactions were 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 were detected by autoradiography [1].
Cell Research
Immortalized wild-type mouse embryonic fibroblasts (MEFs) have been described previously. 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) unless indicated. MRT67307 (10 μM), MRT68921 (1 μM), AZD8055 (1 μM), or bafilomycin A1 (50 nM) was included where indicated. Transfection and transduction were as described [2].
Molecular Weight 501.07
Formula C26H37ClN6O2
CAS No. T5162

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 50 mg/mL

Water: 10 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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. Clark K, et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):161986-91. 4. Zhao L, Xia M, Wang K, et al. A Long Non-coding RNA IVRPIE Promotes Host Antiviral Immune Responses Through Regulating Interferon β1 and ISG Expression[J]. Frontiers in Microbiology. 2020, 11: 260.

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