
簡要描述:MRT68921 1190379-70-4MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively). Through its effects on ULK1, MRT68921 blocks autophagy in cells
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| 品牌 | absin | CAS | 1190379-70-4 |
|---|---|---|---|
| 分子式 | C25H34N6O | 純度 | ≥98% |
| 分子量 | 434.6 | 貨號 | abs819431 |
| 規(guī)格 | 5mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is an inhibitor of ULK1 and ULK2 | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
MRT68921 1190379-70-4
| 產(chǎn)品描述 | |
| 描述 | MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively). Through its effects on ULK1, MRT68921 blocks autophagy in cells, driving the accumulation of stalled early autophagosomal structures. |
| 純度 | ≥98% |
| 儲存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 可溶性/溶解性 | DMSO : 10 mg/mL, warmed |
| 生物活性 | |
| 靶點 | ULK1,ULK2 |
| In vitro(體外研究) | ULK1, a serine/threonine protein kinase, is essential for the initial stages of autophagy. MRT68921 inhibits ULK1 and ULK2 in vitro and block autophagy in cells. MRT68921 is the most potent inhibitor of both ULK1 and ULK2, with greater than a 15-fold reduction in the IC50 for ULK1 (2.9 nm) and greater than a 30-fold reduction for ULK2 (1.1 nm). Autophagy-inhibiting capacity of the compounds is specifically through ULK1. ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation. |
| 參考文獻 | |
| 參考文獻 | 1.Petherick, K.J.,Conway, O.J.L.,Mpamhanga, C., et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J. Biol. Chem. 290(18), 11376-11383 (2015). |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | CardiovascularHeartAutophagyOther MetabolismPathways and ProcessesMitochondrial MetabolismMitophagy fission and fusion NeuroscienceProcesses NeuroscienceNeurology processNeurogenesis Signal TransductionProtein PhosphorylationSer / Thr KinasesOther Kinases Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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