| Description | PKC-IN-1 is an ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM, respectively). |
| In vitro | PKC-IN-1 是一种有效的、与ATP竞争的、可逆的传统PKC酶抑制剂（包括PKCα、PKCβI、PKCβII、PKCθ、PKCγ、PKC mu 及PKCε，针对人类PKCβ和PKCα的Kis分别为5.3和10.4 nM，IC50值分别为2.3、8.1、7.6、25.6、57.5、314、808 nM）[1]。 |
| In vivo | 在Lewis大鼠中，PKC-IN-1以剂量依赖性显著降低了自身免疫性脑炎(EAE)模型中的最大EAE严重程度和结束时的严重程度[1]。 |
| Target activity | PKCγ (human):57.5 nM, PKCμ (human):314 nM, PKCε (human):808 nM, PKCβI (human):8.1 nM, PKCβ (human):5.3 nM (ki), PKCβII (human):7.6 nM, PKCθ (human):25.6 nM, PKCα (human):10.4 nM (ki), PKCα (human):2.3 nM |
| molecular weight | 500.61 |
| Molecular formula | C25H37FN8O2 |
| CAS | 1046787-18-1 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/mL (49.94 mM) |
| References | 1. Michael Niesman, et al. Treatment of autoimmune disease. WO2015179847A1. |