For research use only. Not for therapeutic Use.
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
Go 6983 inhibits PKCμ with IC50 of 20 μM, and the pther PKC isoenzymes can be suppressed by Go 6983 with IC50 values from 7 to 60 nM[1]. Go 6983 (100 nM) significantly reduces PMN adherence to the endothelium and infiltration into the myocardium compared with I/R + PMN hearts, and significantly inhibits superoxide release from PMNs by 90 +/- 2% in rat hearts[2]. Go 6983 (200 nM) has a reduced cardioprotective effect compared with the cardioprotective Go 6983 concentrations (50 and 100 nM) despite inhibiting PMN superoxide release by 99%[3].
Catalog Number | I001260 |
CAS Number | 133053-19-7 |
Synonyms | 3-[1-[3-(dimethylamino)propyl]-5-methoxyindol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione |
Molecular Formula | C26H26N4O3 |
Purity | ≥95% |
InChI | InChI=1S/C26H26N4O3/c1-29(2)11-6-12-30-15-20(18-13-16(33-3)9-10-22(18)30)24-23(25(31)28-26(24)32)19-14-27-21-8-5-4-7-17(19)21/h4-5,7-10,13-15,27H,6,11-12H2,1-3H3,(H,28,31,32) |
InChIKey | LLJJDLHGZUOMQP-UHFFFAOYSA-N |
SMILES | CN(C)CCCN1C=C(C2=C1C=CC(=C2)OC)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54 |
Reference | [1]. Gschwendt M, et al. Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett, 1996, 392(2), 77-80. [2]. Peterman EE, et al. G0 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion. J Cardiovasc Pharmacol, 2004, 43(5), 645-656. [3]. Young LH, et al. G0 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury. Cardiovasc Drug Rev, 2005, 23(3), 255-272. |