257879-35-9

中文名称 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

英文名称 PKCβ Inhibitor

CAS 257879-35-9

分子式 C24H21N5O2

分子量 411.46

MOL 文件 257879-35-9.mol

更新日期 2023/03/20 15:41:23

257879-35-9 结构式

基本信息物理化学性质安全数据 3-[1-[3-(1H-咪唑-1-基)丙基]-1H-吲哚-3-基]-4-(苯氨基)-1H-吡咯-2,5-二酮价格(试剂级) 常见问题列表

基本信息

中文别名

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

英文别名

KUN79359
PKCβ Inhibitor
PKCβ inhibitor 1
3-anilino-4-[1-(3-imidazol-1-ylpropyl)indol-3-yl]pyrrole-2,5-dione
1H-Pyrrole-2,5-dione, 3-[1-[3-(1H-imidazol-1-yl)propyl]-1H-indol-3-yl]-4-(phenylamino)-

物理化学性质

溶解度DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: 1 mg/ml; PBS (pH 7.2): 0.25 mg/ml

形态固体

颜色Yellow to orange

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302-H315-H319-H335

防范说明P261-P305+P351+P338

3-[1-[3-(1H-咪唑-1-基)丙基]-1H-吲哚-3-基]-4-(苯氨基)-1H-吡咯-2,5-二酮价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2024/04/30	HY-13335	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	257879-35-9	500μg	1100元
2024/04/30	HY-13335	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	257879-35-9	1mg	1800元
2024/04/30	HY-13335	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	257879-35-9	5mg	5200元

常见问题列表

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.