| Description | MRT 67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells. |
| In vitro | MRT 67307 dihydrochloride 在体外0.1 mM ATP的条件下，对IKKϵ和TBK1的抑制IC50分别为160和19 nM，但即使在10 μM浓度下也不抑制IKKα或IKKβ[1]。在2 μM浓度下，MRT 67307 dihydrochloride 能防止骨髓来源的巨噬细胞（BMDMs）中IRF3的磷酸化。同样浓度下，它不抑制多磷酸肌醇（poly(I:C)）激活的JNK或p38 MAPK[1]。MRT 67307 dihydrochloride 在1 nM至10 μM浓度范围内能防止巨噬细胞中IFNβ的产生[1]。10 μM浓度足以将phospho-ATG13降至对照水平[2]，并在小鼠胚胎成纤维细胞（MEFs）中阻断自噬[2]。在5 µM浓度和4小时处理下，能在293T细胞中消除TBK1/IKKε诱导的CYLD磷酸化[3]。 |
| molecular weight | 537.53 |
| Molecular formula | C26H38Cl2N6O2 |
| CAS | 1781882-89-0 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 82.8 mg/mL (154 mM) |
| References | 1. 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 2. Clark et al (2011) Novel cross-talk within the IKK family controls innate immunity. Biochem.J. 434 93 3. Smith et al (2011) The role of TBK1 and IKKe in the expression and activation of Pellino 1. Biochem.J. 434 537 4. Galluzzi et al (2017) Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. |