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

生物活性靶点体外研究 3-[1-[3-(1H-咪唑-1-基)丙基]-1H-吲哚-3-基]-4-(苯氨基)-1H-吡咯-2,5-二酮试剂级价格

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

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 :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.