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。
货号:ajcx32856
CAS:257879-35-9
分子式:C24H21N5O2
分子量：411.46
溶解度:DMSO : 250 mg/mL (607.59 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε)[1][2].

PKCβ inhibitor 1 (0-30 μM; 48 hours) suppresses tumor cell proliferation in a time- and dose-dependent manner[2].PKCβ inhibitor 1 (14 μM; 2-48 hours) induces apoptosis in 2F7 cells[2].PKCβ inhibitor 1 (15 μM; 2-48 hours) inhibits cell cycle progression in 2F7 and BCBL-1 cells[2].PKCβ (15 or 14 μM, respectively; 2-48 hours) inhibitor 1 reduces the expression of phospho-PKCβ in BCBL-1 and 2F7 cells[2].PKCβ inhibitor 1(0-48 hours) suppresses GSK3β, mTOR, and S6 phosphorylation[2].

[1]. Tanaka M, et al. Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4.
[2]. Saba NS, et al. Protein kinase C-beta inhibition induces apoptosis and inhibits cell cycle progression in acquired immunodeficiency syndrome-related non-hodgkin lymphoma cells. J Investig Med. 2012 Jan;60(1):29-38.