RottlerinRottlerin
MedChemExpress (MCE)
HY-18980
82-08-6
Mallotoxin
NSC 56346
NSC 94525
98.39%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
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. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.
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].
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].
PKCδ 3 μM (IC50, Porcine spleen) PKCα 30 μM (IC50, baculovirus-infected Sf9 insect cells) PKCγ 40 μM (IC50, baculovirus-infected Sf9 insect cells) PKCβ 42 μM (IC50, baculovirus-infected Sf9 insect cells) PKCη 82 μM (IC50, baculovirus-infected Sf9 insect cells) PKCζ 100 μM (IC50, baculovirus-infected Sf9 insect cells) PKCε 100 μM (IC50, baculovirus-infected Sf9 insect cells) CaM kinase III 5.3 μM (IC50, EF-2 kinase activity in cytosol of murine pancreas) CKII 30 μM (IC50, holoenzyme expressed in E.coli) PKA 78 μM (IC50, catalytic subunit from porcine heart) HIV-1
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[1]. Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28
199(1):93-8. [Content Brief]
[2]. Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des. 2011 Jun
77(6):460-70. [Content Brief]
[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.
[4]. María Rosa López-Huertas, et al. Protein kinase Ctheta is a specific target for inhibition of the HIV type 1 replication in CD4+ T lymphocytes. J Biol Chem. 2011 Aug 5
286(31):27363-77. [Content Brief]
[5]. Zoé Lama, et al. Kinase inhibitors tyrphostin 9 and rottlerin block early steps of rabies virus cycle. Antiviral Res. 2019 Aug
168:51-60. [Content Brief]