粗糠柴苦素
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- CAS号:
- 82-08-6
- 英文名:
- ROTTLERIN
- 英文别名:
- MALLOTOXIN;kamalin;NSC 94525;NSC 56346;ROTTLERIN;Rottierin;Rottlerin,98%;Rottlerin, 98% 10MG;Rottlerin (Mallotoxin;4’,6’-trihydroxy-5’-methyl-methyl)-2
- 中文名:
- 粗糠柴苦素
- 中文别名:
- 咖马林;罗特林;粗糠紫苦素;粗糠柴毒素;粗糠柴苦素;咖马林/粗糠柴苦素;化合物DIBAC4(3);(E)-1-(6-(3-乙酰基-2,4,6-三羟基-5-甲基苄基)-5,7-二羟基-2,2-二甲基-2H-苯并吡喃-8-己)-3-苯基丙-2-烯-1-酮
- CBNumber:
- CB4260488
- 分子式:
- C30H28O8
- 分子量:
- 516.54
- MOL File:
- 82-08-6.mol
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粗糠柴苦素化学性质
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熔点:
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200 °C
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沸点:
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521.39°C (rough estimate)
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密度:
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1.2051 (rough estimate)
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折射率:
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1.4900 (estimate)
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储存条件:
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2-8°C
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溶解度:
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Soluble in DMSO (up to 50 mg/ml).
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形态:
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Powder
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酸度系数(pKa):
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6.92±0.40(Predicted)
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颜色:
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Orange to brown
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稳定性:
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Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
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LogP:
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8.660 (est)
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CAS 数据库:
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82-08-6(CAS DataBase Reference)
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粗糠柴苦素性质、用途与生产工艺
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。
| Target | Value |
PKCδ
(Cell-free assay)
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3 μM
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CKIII
(Cell-free assay)
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5.3 μM
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PKCα
(Cell-free assay)
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30 μM
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CKII
(Cell-free assay)
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30 μM
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PKCγ
(Cell-free assay)
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40 μM
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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.
Western Blot Analysis
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Cell Line:
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Primary HMVEC (Human Microvascular Endothelial Cell).
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Concentration:
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20 μM.
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Incubation Time:
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2, 6, 24 hours.
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Result:
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Dramatically decreased the cyclin D-1 mRNA levels in a time-dependent manner. After 2 h of treatment, the mRNA level was reduced to 50% of the control, to circa 40% after 6 h, and to 20% after 24 h. Consistently, a similar trend was observed in the protein levels, where the decrease was circa 50% after 2 h, 80% after 6 h, and to almost undetectable levels after 24 h.
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Cell Proliferation Assay
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Cell Line:
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Primary HMVEC (Human Microvascular Endothelial Cell).
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Concentration:
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20 μM.
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Incubation Time:
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24/48 hours.
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Result:
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Exhibited a strong growth inhibition, with a reduction in thymidine incorporation respect to the control cells (DMSO 0.1%) of circa 75% and 80%, respectively.
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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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Animal Model:
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Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×10
6
cells mixed with Matrigel, 50:50 ratio) injection.
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Dosage:
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0 or 20 mg/kg.
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Administration:
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Gavage 5 days per week, once daily, for 6 weeks.
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Result:
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Inhibited AsPC-1 pancreatic tumor growth in Balb C nude mice and had no effect
on the body weight of AsPC-1 tumor-bearing mice.
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粗糠柴苦素
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-18980 | Rottlerin | | 1 mg | 369元 |
| 2024/01/25 | HY-18980 | Rottlerin | | 5 mg | 812元 |
粗糠柴苦素
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粗糠柴苦素国内生产厂家
82-08-6, 粗糠柴苦素 相关搜索:
- Protein Kinase
- Aromatic Phenols
- 天然产物
- 试剂盒-细胞分析试剂盒
- 合成材料中间体
- 植物提取物
- BioChemical
- Cell Biology
- Cell Signaling and Neuroscience
- Serine/Threonine Kinase Inhibitors
- Protein Kinase C, Calcium/Calmodulin-dependent protein Kinase (PKC and CaMK)
- Kinase/Phosphatase Biology
- C30H28O8
- 1982-8-6
- (E)-1-(6-(3-乙酰基-2,4,6-三羟基-5-甲基苄基)-5,7-二羟基-2,2-二甲基-2H-苯并吡喃-8-己)-3-苯基丙-2-烯-1-酮
- 化合物DIBAC4(3)
- 罗特林
- 粗糠柴毒素
- 粗糠柴苦素
- 咖马林
- 咖马林/粗糠柴苦素
- 粗糠紫苦素
- 82-08-6
- Rottierin
- (E)-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
- kamalin
- MALLOTOXIN
- Rottlerin (Mallotoxin
- NSC 94525
- NSC 56346
- ROTTLERIN
- Rottlerin, 98% 10MG
- Rottlerin,98%
- (E)-1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one
- 1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2h-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one
- 2-Propen-1-one, 1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-, (2E)-
- acetophenone,3’-((8-cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2h-1-benzopyran-6-yl)
- 4’,6’-trihydroxy-5’-methyl-methyl)-2
- 3'-[(8-CINNAMOYL-5,7-DIHYDROXY-2,2-DIMETHYL-2H-1-BENZOPYRAN-6-YL)METHYL]-2',4',6'-TRIHYDROXY-5'-METHYLACETOPHENONE