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Submit ReviewMRT 67307 dihydrochloride is a salt inducible kinase (SIK) inhibitor (IC50 values are 67, 250 and 430 nM for SIK2, SIK1 and SIK3 respectively) and a potent inhibitor of ULK1 and 2 (IC50 values of 45 and 38 nM, respectively). MRT 67307 dihydrochloride also inhibits TBK1, MARK1-4, IKKε and NUAK1 (IC50 values are 19, 27-52, 160 and 230 nM respectively). Has no effect on IKKα or IKKβ. Induces IL-10 secretion and inhibits TNF-α and IL-6 secretion in bacterial LPS-stimulated macrophages. Also enhances IL-1-induced activation of NFκB-dependent gene transcription in mouse embryonic fibroblast (MEF) cells. Inhibits autophagy.
分子量 | 537.52 |
公式 | C26H36N6O2.2HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 1781882-89-0 |
PubChem ID | 90489013 |
InChI Key | ZIKXPHATVRPOQG-UHFFFAOYSA-N |
Smiles | O=C(C5CCC5)NCCCNC1=C(C4CC4)C=NC(NC2=CC(CN3CCOCC3)=CC=C2)=N1.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 10.75 | 20 | |
DMSO | 53.75 | 100 |
以下数据基于产品分子量 537.52。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.86 mL | 9.3 mL | 18.6 mL |
5 mM | 0.37 mL | 1.86 mL | 3.72 mL |
10 mM | 0.19 mL | 0.93 mL | 1.86 mL |
50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
参考文献是支持产品生物活性的出版物。
Clark et al (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc.Natl.Acad.Sci.U.S.A. 109 16986 PMID: 23033494
Clark et al (2011) Novel cross-talk within the IKK family controls innate immunity. Biochem.J. 434 93 PMID: 21138416
Smith et al (2011) The role of TBK1 and IKKe in the expression and activation of Pellino 1. Biochem.J. 434 537 PMID: 21204785
Galluzzi et al (2017) Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. 16 487 PMID: 28529316
Petherick et al (2015) Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J.Biol.Chem. 290 28726 PMID: 26614783
If you know of a relevant reference for MRT 67307 dihydrochloride, please let us know.
关键词: MRT 67307 dihydrochloride, MRT 67307 dihydrochloride supplier, MRT67307, dihydrochloride, salt, inducible, kinase, SIK, inhibitors, inhibits, TBK1, IKKε, IKKepsilon, IKKe, MARK, NUAK, ULK1, 2, autophagy, Other, Kinases, Autophagy, TANK, binding, (TBK), 5134, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 MRT 67307 dihydrochloride 的部分引用包括:
Alison et al (2020) LAP-like non-canonical autophagy and evolution of endocytic vacuoles in pancreatic acinar cells. Autophagy 16 1314-1331 PMID: 31651224
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