| 产品描述: | Rottlerin (Mallotoxin, NSC 56346, NSC 94525)是一种从 Mallotus Philippinensis 纯化出来的天然化合物,一种特效的 Protein kinase 的抑制剂,对PKCδ(来自杆状病毒感染的Sf9昆虫细胞)、PKCδ(来自猪脾)和CaM kinase III的IC50值分别为3 μM、6 μM和5.3 μM。Rottlerin 还可以抑制PKCα、PKCγ、PKCβ、PKCη、CKII和PKA,其IC50值分别为30 μM、40 μM、42 μM、82 μM、30 μM和78 μM |
| 靶点: |
PKCδ(Cell-free assay):3 μM; CKIII(Cell-free assay):5.3 μM; PKCα(Cell-free assay):30 μM; CKII(Cell-free assay):30 μM; PKCγ(Cell-free assay):40 μM;PKCβ(Cell-free assay):42 μM;PKA(Cell-free assay):78 μM;PKCη(Cell-free assay):82 μM;CaMK; Apoptosis; Others; HIVProtease; PKA; PKC; Autophagy |
| 体内研究: |
A xenograft model of pancreatic cancer is prepared by injection of 2×106 HPAF-II cells subcutaneously into nude mice. A substantial amount of Rottlerin is detected in tumor and plasma in mice fed Rottlerin diet. These data indicate that Rottlerin is efficiently absorbed in vivo and suggest a strong potential for Rottlerin as a preventive or adjuvant supplement for pancreatic cancer. |
| 细胞实验: |
Cell lines: HPAF-II cells Concentrations: 25 μM Incubation Time: 3 h, 24 h Method: The accumulation of Rottlerin is examined in HPAF-II cells treated with 25 μM Rottlerin, and the fate of Rottlerin in the incubation media. Cells are collected at 3 and 24 h after Rottlerin stimulation and conditioned media are taken at 0.5, 1.0, 3.0, 6.0 and 24 h (n=4 for each time point). Samples are prepared immediately for HPLC analysis without further storage. |
| 动物实验: |
Animal Models: nude mice injected with HPAF-II cells Dosages: 120 mg/kg Administration: Oral gavage |
| 参考文献: |
1. M Gschwendt, et al. Biochem Biophys Res Commun. 1994 Feb 28;199(1):93-8. 2. Qing-Yi Lu, et al. J Chromatogr Sep Tech. 2013 Jan 1;4(1):100062. |
| 溶解性: |
Soluble in DMSO、Ethanol |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.936 ml |
9.68 ml |
19.36 ml |
| 5 mM |
0.387 ml |
1.936 ml |
3.872 ml |
| 10 mM |
0.194 ml |
0.968 ml |
1.936 ml |
| 50 mM |
0.039 ml |
0.194 ml |
0.387 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |