| Description | Rottlerin (NSC-56346) 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. |
| In vitro | Rottlerin（20 μM）表现出在HMVEC中促进细胞增殖的作用。Rottlerin（20 μM，施加时间分别为2、6、24小时）显著且依时间递增地降低初代HMVEC中cyclin D-1 mRNA水平[2]。 |
| In vivo | Rottlerin 通过激活caspase-3和切割poly聚合酶抑制肿瘤细胞增殖并诱导凋亡。Rottlerin（20 mg/kg，灌胃，每周5天，每天一次，持续6周）在不产生毒性的情况下[3], 抑制了Balb C裸鼠中AsPC-1胰腺肿瘤的生长。 |
| Target activity | PKCα:30 μM(baculovirus-infected Sf9 insect cells), PKCη:82 μM(baculovirus-infected Sf9 insect cells), PKCδ:3 μM(Porcine spleen), PKCγ:40 μM(baculovirus-infected Sf9 insect cells), PKA:78 μM, PKCζ:100 μM(baculovirus-infected Sf9 insect cells), PKCε:100 μM(baculovirus-infected Sf9 insect cells), CK2:30 μM(holoenzyme expressed in E.coli), PKCβ:42 μM(baculovirus-infected Sf9 insect cells) |
| Synonyms | Mallotoxin, NSC 56346, 粗糠柴苦素, NSC 94525 |
| molecular weight | 516.54 |
| Molecular formula | C30H28O8 |
| CAS | 82-08-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 2 mg/mL (3.87 mM), Sonication is recommended. |
| References | 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. |