Rottlerin

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Rottlerin

CAS No. : 82-08-6

MCE 国际站：Rottlerin

产品活性：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，通过靶向mTORC1 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。

研究领域：Epigenetics  |  TGF-beta/Smad  |  Autophagy  |  Apoptosis  |  Anti-infection

作用靶点：PKC  |  Autophagy  |  Apoptosis  |  HIV  |  RABV

In Vitro: 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.

In Vivo: 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).

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