Rottlerin (Synonyms: Mallotoxin, NSC 94525, NSC 56346) |
| Katalog-Nr.GC10820 |
Rottlerin, ein aus Mallotus Philippinensis gereinigtes Naturprodukt, ist ein spezifischer PKC-Inhibitor mit IC50-Werten fÜr PKCδ von 3-6 μM, PKCα,β,γ von 30-42 μM, PKCε,η,ζ von 80-100 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1982/8/6
Sample solution is provided at 25 µL, 10mM.
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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).
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