Go 6983

Cas：133053-19-7

Product Information：

GO6983 is a potent protein kinase C (PKC) inhibitor. GO6893 displays cardioprotective properties; reduces polymorphonuclear leukocyte adherence and infiltration following myocardial ischemia/reperfusion injury.

Chemical Formula: C26H26N4O3

Exact Mass: 442.20049

Molecular Weight: 442.51

Elemental Analysis: C, 70.57; H, 5.92; N, 12.66; O, 10.85

Synonym:

Go6983

Chemical Name:

3-(1-(3-(dimethylamino)propyl)-5-methoxy-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione

InChi Key: 

LLJJDLHGZUOMQP-UHFFFAOYSA-N

InChi Code: 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)

Smiles Code:

O=C(C(C1=CN(CCCN(C)C)C2=C1C=C(OC)C=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O

Technical Data：

Appearance: Solid powder

Purity: >98%

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

In Vitro：

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. 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. 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%.

References：

1. Dai B, Zhang J, Liu M, Lu J, Zhang Y, Xu Y, Miao J, Yin Y. The role of Ca(2+) mediated signaling pathways on the effect of taurine against Streptococcus uberis infection. Vet Microbiol. 2016 Aug 30;192:26-33. doi: 10.1016/j.vetmic.2016.06.008. PubMed PMID: 27527761.

2. Olianas MC, Dedoni S, Onali P. Protection from interferon-β-induced neuronal apoptosis through stimulation of muscarinic acetylcholine receptors coupled to ERK1/2 activation. Br J Pharmacol. 2016 Oct;173(19):2910-28. doi: 10.1111/bph.13570. PubMed PMID: 27474091.

3. Hu SY, Tong GJ, Meng Y, Hao S, Li W, Xu FL, He YH, Chen JT, Yang DH. [Parathyroid hormone inhibits the apoptosis of osteoblast MC-3T3E1 cells through a non-PLC-dependent protein kinase C pathway]. Nan Fang Yi Ke Da Xue Xue Bao. 2016 Jun;36(6):785-9. Chinese. PubMed PMID: 27320879.

4. 4.Meng Z, Bischof J, Ianes C, Henne-Bruns D, Xu P, Knippschild U. CK1δ kinase activity is modulated by protein kinase C α (PKCα)-mediated site-specific phosphorylation. Amino Acids. 2016 May;48(5):1185-97. doi: 10.1007/s00726-015-2154-3. PubMed PMID: 26803658.

Products are for research use only. Not for human use.