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.