粗糠柴苦素
中文名称:粗糠柴苦素
英文名称:ROTTLERIN
CAS号:82-08-6
分子式:C30H28O8
分子量:516.54
EINECS号:201-395-4
Mol文件:82-08-6.mol
粗糠柴苦素 性质
| 熔点 | 200 °C |
|---|---|
| 沸点 | 521.39°C (rough estimate) |
| 密度 | 1.2051 (rough estimate) |
| 折射率 | 1.4900 (estimate) |
| 储存条件 | 2-8°C |
| 溶解度 | 溶于DMSO（高达50mg/ml）。 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 6.92±0.40(Predicted) |
| 颜色 | 橙色至棕色 |
| 稳定性 | DMSO中的溶液可在-20°下稳定储存1个月。 |
| LogP | 8.660 (est) |
| CAS 数据库 | 82-08-6(CAS DataBase Reference) |
粗糠柴苦素 用途与合成方法
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) | 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 |
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. |
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. |
粗糠柴苦素 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | 32849 | 粗糠柴毒素 | 82-08-6 | 10mg | 1818 |
| 2024-11-08 | HY-18980 | 5 mg | 812 |
粗糠柴苦素供应商 更多
北京百灵威科技有限公司
联系电话：010-82848833 400-666-7788
产品介绍：
中文名称：粗糠柴苦素
英文名称：Rottlerin, 98%
CAS：82-08-6
纯度：98%
包装信息：10MG
备注：化学试剂、精细化学品、医药中间体、材料中间体
武汉易泰科技有限公司上海分公司
联系电话：821-50328103-801 18930552037
产品介绍：
中文名称：粗糠柴苦素
英文名称：Rottlerin;3'-[(8-CinnaMoyl-5,7-dihydroxy-2,2-diMethyl-2H-1-benzopyran-6-yl)Methyl]-2',4',6'-trihydroxy-5'-Methylacetophenone
CAS：82-08-6
纯度：99% HPLC
包装信息：1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
上海同田生物技术有限公司
联系电话：021-51320588
产品介绍：
英文名称：ROTTLERIN(RG)
CAS：82-08-6
纯度：NLT 95% HPLC
包装信息：10Mg;20Mg;50Mg;100Mg to graMs.Not More than tens of graMs.
备注：ASB-00018380-005
TargetMol中国（陶术生物）
联系电话：021-021-33632979 15002134094
产品介绍：
中文名称：粗糠柴苦素
英文名称：Rottlerin
CAS：82-08-6
纯度：99.44%
包装信息：5mg/RMB 671;10mg/RMB 996;25mg/RMB 2320
Sigma-Aldrich西格玛奥德里奇(上海)贸易有限公司
联系电话：021-61415566 800-8193336
产品介绍：
英文名称：Rottlerin
CAS：82-08-6
纯度：>=95% (HPLC)
包装信息：10MG
备注：R5648-10MG
