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PKC&ROCK

GO6983 (133053-19-7)

Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ withIC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.

Not Intended for Therapeutic Use. For research use only.

CAS: 133053-19-7 Category

GO6983 (133053-19-7) Description:

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

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%.

GO6983 (133053-19-7) Specifications:

Product Name GO6983
Synonym Go6983 Go-6983; Go 6983; GO6983; GO 6983; GO-6983
Chemical Name 3-(1-(3-(dimethylamino)propyl)-5-methoxy-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 133053-19-7
Molecular Formula C26H26N4O3
Molecular Weight 442.51
Monoisotopic Mass 442.20049 g/mol
MDL number MFCD04040031
InChIKey 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
SMILES O=C(C(C1=CN(CCCN(C)C)C2=C1C=C(OC)C=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O
Form Powder
Color red
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life >5 years if stored properly
Handling Protect from air and light
Application A potent protein kinase C (PKC) inhibitor

 


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RIDADR NONH for all modes of transport

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]. 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.

[5]. Jian Y, Chen C, Li B, Tian X. Delocalized Claudin-1 promotes metastasis of human osteosarcoma cells. Biochem Biophys Res Commun. 2015 Oct 23;466(3):356-61. doi: 10.1016/j.bbrc.2015.09.028. PubMed PMID: 26361141.

1 review for GO6983 (133053-19-7)

  1. Cofttek

    Never had such good experience before,The GO6983 (133053-19-7) is high purity,also customer service is pretty nice !gotta try!!

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