包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Canonical SMILES | O=C(C1CCC1)NCCCNC2=NC(NC3=CC(CN4CCOCC4)=CC=C3)=NC=C2C5CC5.Cl |
分子式 | C26H36N6O2 • XHCl |
分子量 | 464.6 |
溶解度 | DMF: 5 mg/ml,DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml,DMSO: 3 mg/ml,Ethanol: 2 mg/ml |
储存条件 | -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s = 250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).1,2,3,4MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages.1,3Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy.4 1.Clark, K., Peggie, M., Plater, L., et al.Novel cross-talk within the IKK family controls innate immunityBiochem. J.434(1)93-104(2011) 2.Clark, K., Takeuchi, O., Akira, S., et al.The TRAF-associated protein TANK facilitates cross-talk within the IkappaB kinase family during Toll-like receptor signalingProc. Natl. Acad. Sci. USA108(41)17093-17098(2011) 3.Clark, K., MacKenzie, K.F., Petkevicius, K., et al.Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophagesProc. Natl. Acad. Sci. USA109(42)16986-16991(2012) 4.Petherick, K.J., Conway, O.J.L., Mpamhanga, C., et al.Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagyJ. Biol. Chem.290(18)11376-11383(2015) |