3-[1-[3-(1H-咪唑-1-基)丙基]-1H-吲哚-3-基]-4-(苯氨基)-1H-吡咯-2,5-二酮
- CAS号:257879-35-9
- 英文名:PKCβ Inhibitor
- 中文名:3-[1-[3-(1H-咪唑-1-基)丙基]-1H-吲哚-3-基]-4-(苯氨基)-1H-吡咯-2,5-二酮
- CBNumber:CB12628270
- 分子式:C24H21N5O2
- 分子量:411.46
- MOL File:257879-35-9.mol
- 溶解度 :DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: 1 mg/ml; PBS (pH 7.2): 0.25 mg/ml
- 形态 :A solid
- 颜色 :Yellow to orange
3-[1-[3-(1H-咪唑-1-基)丙基]-1H-吲哚-3-基]-4-(苯氨基)-1H-吡咯-2,5-二酮性质、用途与生产工艺
- 生物活性 PKCβ inhibitor 1 是有效的,ATP 竞争性和选择性 PKCβ 抑制剂,对人 PKCβ1 和 PKCβ2 的 IC50 分别为 21 和 5 nM。与 PKCβ2 相比,PKCβ inhibitor 1 对其他 PKC 同工酶 (PKCα、PKCγ 和 PKCε) 具有 60 倍以上的选择性。
-
靶点
human PKCβ1
21 nM (IC 50 )
human PKCβ2
5 nM (IC 50 )
PKCα
331 nM (IC 50 )
-
体外研究
PKCβ inhibitor 1 (0-30 μM; 48 hours) suppresses tumor cell proliferation in a time- and dose-dependent manner.
PKCβ inhibitor 1 (14 μM; 2-48 hours) induces apoptosis in 2F7 cells.
PKCβ inhibitor 1 (15 μM; 2-48 hours) inhibits cell cycle progression in 2F7 and BCBL-1 cells.
PKCβ (15 or 14 μM, respectively; 2-48 hours) inhibitor 1 reduces the expression of phospho-PKCβ in BCBL-1 and 2F7 cells.
PKCβ inhibitor 1(0-48 hours) suppresses GSK3β, mTOR, and S6 phosphorylation.Cell Proliferation Assay
Cell Line: 2F7, BCBL-1 cells Concentration: 0, 5, 10, 20, and 30 μM Incubation Time: 48 hours Result: A dose-dependent reduction in viability of the 2F7 and BCBL-1 cells starting at 5 μM and increasing with elevated inhibitor concentration. Apoptosis Analysis
Cell Line: 2F7 cells Concentration: 14 μM Incubation Time: 2-48 hours Result: Apoptotic induction in 2.1% of the 2F7 cells above background after 2 hours of treatment, increasing through 48 hours of treatment. Cell Cycle Analysis
Cell Line: BCBL-1 Cells Concentration: 15 μM (the IC 50 ) Incubation Time: 2-48 hours Result: Inhibits cell cycle progression in 2F7 and BCBL-1 cells. Western Blot Analysis
Cell Line: BCBL-1 and 2F7 cell lines Concentration: 15 or 14 μM (at the IC 50 respectively) Incubation Time: 2-48 hours Result: The expression of phospho-PKCβ in BCBL-1 and 2F7 cells reduced.
- 更新日期:2024/11/08
- 产品编号:HY-13335
- 产品名称:3-[1-[3-(1H-咪唑-1-基)丙基]-1H-吲哚-3-基]-4-(苯氨基)-1H-吡咯-2,5-二酮 PKCβ inhibitor 1
- CAS编号:257879-35-9
- 包装:500μg
- 价格:1100元
- 更新日期:2024/11/08
- 产品编号:HY-13335
- 产品名称:3-[1-[3-(1H-咪唑-1-基)丙基]-1H-吲哚-3-基]-4-(苯氨基)-1H-吡咯-2,5-二酮 PKCβ inhibitor 1
- CAS编号:257879-35-9
- 包装:1mg
- 价格:1800元
- 公司名称:TargetMol Chemicals Inc.
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