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粗糠柴苦素
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性质
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粗糠柴苦素
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CAS No. 82-08-6
分子式 C30H28O8
分子量 516.54
英文名称 ROTTLERIN
中文同义词 粗糠紫苦素;咖马林/粗糠柴苦素;咖马林;粗糠柴苦素;粗糠柴毒素;罗特林;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
基本信息
产品名称
粗糠柴苦素
中文同义词
粗糠紫苦素,咖马林/粗糠柴苦素,咖马林,粗糠柴苦素,粗糠柴毒素,罗特林,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
英文名称
ROTTLERIN
英文同义词
MALLOTOXIN;3'-[(8-CINNAMOYL-5,7-DIHYDROXY-2,2-DIMETHYL-2H-1-BENZOPYRAN-6-YL)METHYL]-2',4',6'-TRIHYDROXY-5'-METHYLACETOPHENONE;4’,6’-trihydroxy-5’-methyl-methyl)-2;acetophenone,3’-((8-cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2h-1-benzopyran-6-yl);kamalin;ROTTLERIN;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)-;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
CAS No.
82-08-6
分子式
C30H28O8
分子量
516.54
EINECS号
201-395-4
MDL NO.
MFCD00017361
性质
LogP
8.660 (est)
密度
1.2051 (rough estimate)
形态
粉末
沸点
521.39°C (rough estimate)
熔点
200 °C
颜色
橙色至棕色
折射率
1.4900 (estimate)
储存条件
2-8°C
酸度系数(pKa)
6.92±0.40(Predicted)
溶解度
溶于DMSO(高达50mg/ml)。
稳定性
DMSO中的溶液可在-20°下稳定储存1个月。
CAS 数据库
82-08-6(CAS DataBase Reference)
用途
靶点
TargetValue 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
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). Animal Model: Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×10 6 cells mixed with Matrigel, 50:50 ratio) injection. Dosage: 0 or 20 mg/kg. Administration: Gavage 5 days per week, once daily, for 6 weeks. Result: 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.
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. Western Blot Analysis Cell Line: Primary HMVEC (Human Microvascular Endothelial Cell). Concentration: 20 μM. Incubation Time: 2, 6, 24 hours. Result: 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. Cell Proliferation Assay Cell Line: Primary HMVEC (Human Microvascular Endothelial Cell). Concentration: 20 μM. Incubation Time: 24/48 hours. Result: 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.
生物活性
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。
安全信息
RTECS号
AM6913800
WGK Germany
3
安全说明
海关编码
危险品标志
Xn
危险类别码
编辑结构
18612996721 400-400-1062016
中文名称:
粗糠柴苦素
英文名称:
ROTTLERIN
CAS NO.:
82-08-6
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0769-89974612
中文名称:
粗糠柴苦素
英文名称:
ROTTLERIN
CAS NO.:
82-08-6
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中文名称:
粗糠柴苦素
英文名称:
ROTTLERIN
CAS NO.:
82-08-6
信息错误报告 82-08-6
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