PKC inhibitor
CAS：82-08-6
分子式：C30H28O8
分子量：516.55
纯度：98%
存储：Store at -20°C

Background:

Rottlerin was originally identified as an inhibitor of PKCδ (IC50 = 3 μM), but can also inhibit CAM kinase III and a wide range of protein kinases, including PRAK and MAPKAP-K2 (IC50s = 1.9 and 5 μM, respectively).[1],[2] It can act as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1.[3] Rottlerin has also been shown to have neuroprotective effects in an MPTP animal model of Parkinson’s disease.[4]

Reference:

[1]. McGovern, S.L., and Shoichet, B.K. Kinase inhibitors: Not just for kinases anymore Journal of Medicinal Chemistry 46, 1478-1483 (2003).
[2]. Davies, S.P., Reddy, H., Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors Biochem. J. 351(1), 95-105 (2000).
[3]. Balgi, A.D., Fonseca, B.D., Donohue, E., et al. Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling PLoS One 4(9), 1-15 (2009).
[4]. Zhang, D., Anantharam, V., Kanthasamy, A., et al. Neuroprotective effect of protein kinase Cδ inhibitor rottlerin in cell culture and animal models of Parkinson’s disease Journal of Pharmacology and Experimental Therapeutics 322(3), 913-922 (2007).