Rottlerin
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 10mg | ¥1191.00 | 现货 | |
| 50mg | ¥4062.00 | 现货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
Rottlerin 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[1].
Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner and exhibits cell proliferation in HMVEC[2].
In Balb C nude mice, rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth with no toxicity. Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP)[3].
References:
[1]. Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun, 1994, 199(1): 93-8.
[2]. Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des, 2011, 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, 2014, 353(1): 32-40.
产品性质
| 物理外观 | A yellow to orange solid |
| CAS号 | 82-08-6 |
| 分子式 | C30H28O8 |
| 分子量 | 516.55 |
| 化学名称 | (Z)-1-(6-(3-acetyl-2,4,6-trihydroxy-5-methylbenzyl)-5,7-dihydroxy-2,2-dimethyl-2H-chromen-8-yl)-3-phenylprop-2-en-1-one |
| 溶解度 | insoluble in EtOH; insoluble in H2O; ≥23.6 mg/mL in DMSO |
| SMILES | OC1=C2C(OC(C)(C)C=C2)=C(C(/C=C\C3=CC=CC=C3)=O)C(O)=C1CC(C(O)=C(C)C(O)=C4C(C)=O)=C4O |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | Rottlerin 是一种从 Mallotus Philippinensis 中提纯的天然产物,是一种特异性 PKC 抑制剂,对 PKCδ 的 IC50 值为 3-6 μM,对 PKCα,β,γ 的 IC50 值为 30-42 μM,对 PKCε,η,ζ 的 IC50 值为 80-100 μM。Rottlerin 是一种直接的线粒体解耦剂,通过靶向 mTORC1 上游的信号级联刺激自噬。Rottlerin 可通过激活 caspase 3 诱导细胞凋亡。Rottlerin 可抑制 HIV-1 整合和狂犬病毒(RABV)感染。 |




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