Rottlerin is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.
Rottlerin (20 μM) shows cell proliferation in HMVEC. Rottlerin (20 μM, 2/6/24 hours) dramatically reduces the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC .
Rottlerin inhibits tumor cell proliferation and causes apoptosis through activation of caspase-3 and cleavage of the poly polymerase. 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 .