For research use only. Not for therapeutic Use.
Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (K<sub>i</sub> = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. <span class=/itemid/>81590</span>). It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC<sub>50</sub> = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC<sub>50</sub> = 170 nM). It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT<sub>3</sub> with a K<sub>i</sub> value of 61 nM.
| Catalog Number | M039904 |
| CAS Number | 176504-36-2 |
| Synonyms | BIM I;GF109203X;Gö 6850 |
| Molecular Formula | C25H25ClN4O2 |
| Purity | ≥95% |
| Target | TGF-beta/Smad |
| Storage | -20°C |
| IUPAC Name | 3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione;hydrochloride |
| InChI | InChI=1S/C25H24N4O2.ClH/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20;/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31);1H |
| InChIKey | XRAMWNCMYJHGGH-UHFFFAOYSA-N |
| SMILES | CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54.Cl |
