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257879-35-9

中文名稱(chēng) 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
英文名稱(chēng) 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 結(jié)構(gòu)式 257879-35-9 結(jié)構(gòu)式

基本信息

中文別名
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
英文別名
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)-

物理化學(xué)性質(zhì)

溶解度DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: 1 mg/ml; PBS (pH 7.2): 0.25 mg/ml
形態(tài)固體
顏色Yellow to orange

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)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-2,5-二酮價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-133353-[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
257879-35-9500μg1100元
2024/11/08HY-133353-[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
257879-35-91mg1800元
2024/11/08HY-133353-[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
257879-35-95mg5200元

常見(jiàn)問(wèn)題列表

生物活性
PKCβ inhibitor 1 是有效的,ATP 競(jìng)爭(zhēng)性和選擇性 PKCβ 抑制劑,對(duì)人 PKCβ1 和 PKCβ2 的 IC50 分別為 21 和 5 nM。與 PKCβ2 相比,PKCβ inhibitor 1 對(duì)其他 PKC 同工酶 (PKCα、PKCγ 和 PKCε) 具有 60 倍以上的選擇性。
靶點(diǎn)

human PKCβ1

21 nM (IC 50 )

human PKCβ2

5 nM (IC 50 )

PKCα

331 nM (IC 50 )

體外研究

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.
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