基本信息
分子式 | C30H28O8 |
分子量 | 516.55 |
熔点 | >200 |
MDL编码 | MFCD00017361 |
EINECS 编号 | 201-395-4 |
存储条件 | Store at 2-8℃ |
产品描述
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation[1][2][3].
靶点(IC50 & Targe)
PKCδ3, μM (IC50, Porcine spleen)
PKCγ, 40 μM (IC50, baculovirus-infected Sf9 insect cells)
PKCη, 82 μM (IC50, baculovirus-infected Sf9 insect cells)
PKCε, 100 μM (IC50, baculovirus-infected Sf9 insect cells)
PKA, 78 μM (IC50, catalytic subunit from porcine heart)
PKCα, 30 μM (IC50, baculovirus-infected Sf9 insect cells)
PKCβ, 42 μM (IC50, baculovirus-infected Sf9 insect cells)
PKCζ, 100 μM (IC50, baculovirus-infected Sf9 insect cells)
CKII, 30 μM (IC50, holoenzyme expressed in E.coli)
CaM kinase III, 5.3 μM (IC50, EF-2 kinase activity in cytosol of murine pancreas)
体外研究
Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC[2].
Rottlerin (20 μM) exhibits cell proliferation in HMVEC[2].
Western Blot Analysis[2]
体内研究
Rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth in Balb C nude mice with no toxicity[3].
Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP)[3].
参考文献
[1]. Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28;199(1):93-8.
[2]. Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des. 2011 Jun;77(6):460-70.
[3]. Minzhao Huang, et al. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated from KrasG12D mice. Cancer Letters 353 (2014) 32-40.
安全信息
图形或危害标志 | |
提示语 | Warning |
危险说明 | H302 |
防范说明 | P301+P312 |
WGK | 3 |
RTECS | AM6913800 |
百灵威科技