Bisindolylmaleimide XI (hydrochloride) (Ro 32-0432) 是一种有效的、选择性的、具有口服活性的 PKC 抑制剂，对 PKCα、PKCβI、PKCβII、PKCγ 和 PKCε 的 IC50 分别为 9 nM、28 nM、31 nM、37 nM 和 108 nM ， 分别。
| Cas No. | 145333-02-4 |
| 别名 | Ro 32-0432; Ro 31-8830 hydrochloride |
| 化学名 | 3-[8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione, monohydrochloride |
| Canonical SMILES | O=C(NC1=O)C(C2=CNC3=C2C=CC=C3)=C1C4=C5N(CCC(CN(C)C)C5)C6=CC=CC=C64.Cl |
| 分子式 | C28H28N4O2.HCl |
| 分子量 | 489 |
| 溶解度 | DMSO: Soluble,Methanol: Soluble |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Bisindolylmaleimide XI (BIM XI) is a selective, cell-permeable protein kinase C (PKC) inhibitor that displays 10-fold greater selectivity for PKCα (IC50 = 9 nM) and 4-fold greater selectivity for PKCβI (IC50 = 28 nM) over Ca2+-independent PKCε (IC50 = 108 nM). Inhibition of PKCα by BIM XI and other similar PKC inhibitors has been associated with enhanced cardiac contractility and protection from heart failure. BIM XI prevents T-cell activation and proliferation (with IC50s ranging from 30-150 nM) associated with chronic inflammatory responses in vivo. |
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