Go6893 --- PKC Inhibitor

Go6983 is a potent 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. It is inactive to PKCμ. Go6983 displays cardioprotective properties. It can reduce polymorphonuclear leukocyte adherence and infiltration following myocardial ischemia/reperfusion injury. It can also optimize naïve human pluripotent stem cell growth and viability following naïve cell derivation from primed ESCs and iPSCs using naïve human stem cell medium (NHSM). It is used in a chemical cocktail of seven small molecules to directly convert human fibroblasts into neuronal cells bypassing a neural progenitor stage.

Product information

CAS Number: 133053-19-7

Molecular Weight: 442.51

Formula: C26H26N4O3

Synonym:

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

Smiles: CN(C)CCCN1C=C(C2=C(C3=CNC4=CC=CC=C34)C(=O)NC2=O)C2=CC(=CC=C12)OC

InChiKey: LLJJDLHGZUOMQP-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Go6983 was used at 1-5 µM final concentration in vitro and in cellular assays.

In Vivo:

Go6983 was dosed by IV injection to mice bearing B16BL6 tumors at 22 μg per mouse.

References:

1. Gschwendt M, et al. Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. (1996) FEBS Lett. 392(2):77-80.
2. Peterman EE, et al. Gö 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion. (2004) J Cardiovasc Pharmacol. 43(5):645-56.
3. Young LH, et al. Gö 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury. (2005) Cardiovasc Drug Rev. 23(3):255-72.
4. Hu W, et al. Direct Conversion of Normal and Alzheimer's Disease Human Fibroblasts into Neuronal Cells by Small Molecules. (2015) Cell Stem Cell. 17(2):204-12.

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

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