Rottlerin 是可从 Mallotus Philippinensis 中的到的一种天然产物， 是 PKC 的一个特异性抑制剂，其对 PKCδ 的 IC50 值为 3-6 μM， PKCα，β，γ 的为 30-42 μM，PKCε，η，ζ 为 80-100 μM。Rottlerin 可作为线粒体直接解偶联剂，通过编写那个 mTOR1 上游的信号级联刺激自噬。Rottlerin 通过活化 caspase 3 诱导细胞凋亡。Rottlerin 抑制 HIV-1 整合和狂犬病病毒 (RABV) 感染。
| CAS No. | 82-08-6 |
| 生物活性 | 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. |
| 分子式 | C30H28O8 |
| 分子量 | 516.54 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : 12.5 mg/mL (24.20 mM; ultrasonic and warming and heat to 60°C) |
| 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. Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP). |
| 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. Rottlerin (20 μM) exhibits cell proliferation in HMVEC. |
| 文献 | •J Virol. 2021 Oct 27;JVI0134421. |
| 纯度及产品资料 | 98% |
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