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Go 6983

Catalog No. T6313 CAS 133053-19-7

Synonyms: Goe 6983

Go 6983 is a pan-PKC inhibitor targeting PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, exhibiting IC50 values of 7 nM, 7 nM, 6 nM, 10 nM, and 60 nM, respectively.

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Go 6983, CAS 133053-19-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 76.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 258.00
50 mg	In stock	$ 408.00
100 mg	In stock	$ 593.00
1 mL * 10 mM (in DMSO)	In stock	$ 80.00

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Purity: 99.04%

Purity: 98.84%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Go 6983 is a pan-PKC inhibitor targeting PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, exhibiting IC50 values of 7 nM, 7 nM, 6 nM, 10 nM, and 60 nM, respectively.
Targets&IC50	PKCα:7 nM, PKCδ:10 nM, PKCγ:6 nM, PKCζ:60 nM, PKCβ:7 nM
In vitro	A 22.0 μg intravenous (i.v.) dose of Go6983 significantly inhibits 51.2% of tumor metastasis in the B16BL6 lung tumor model in mice.
In vivo	Go 6983 is a subtype-specific PKC inhibitor that targets the ATP binding site. It inhibits ΔPfPKB activity with an IC50 of 1 μM. When 1 μM Go 6983 is used in conjunction with 390 nM Ro-31-8425, it slightly inhibits Angiotensin II-induced PLD2 activity in PGSMCs. Treatment with Go 6983 (5 μM) results in significantly fewer cycles in the next generation compared to control cultures, and this treatment leads to a nearly 60% reduction in new ring formation in cultures of the malaria parasite. At a concentration of 300 μM, Go6983 decreases PKCμ autophosphorylation by 20% in NIH3T3 cells transfected with PKCμ. In scenarios involving cardiac reperfusion, treatment with Go6983 (100 nM) alongside PMNs restores left ventricular developed pressure and the rate of left ventricular pressure development to 89% and 74% of baseline values, respectively, significantly higher than treatment with PMNs alone. Compared to cardiac ischemia-reperfusion (I/R) + PMN, 100 nM Go6983 significantly inhibits PMN adhesion to endothelial cells and myocardial infiltration and reduces superoxide release by PMNs by 90%. Go6983 reduces myocardial contractile dysfunction after I/R in the presence of PMNs, likely due to reduced superoxide production. It notably inhibits superoxide release from leukocytes in patients previously sensitized to tree pollen antigens. Furthermore, Go6983 inhibits Ca(2+) accumulation in human vascular tissue cells, indicating its mechanism for vascular relaxation properties.
Kinase Assay	Phosphorylation reactions are carried out in a total volume of 100 μL, containing buffer C (50 mM Tris-HCl, pH 7.5, 10 mM β-mercaptoethanol), 4 mM MgCl2, 10 μg PS, 100 nM TPA, 5 μL of a Sf158 cell extract as a source of recombinant PKCμ or of Sf9 cell extracts as a source of other recombinant PKC isoenzymes, 10 μg of syntide 2 as substrate, and 35 μM ATP containing 1 μCi [γ-32P]ATP. In some experiments, PS and TPA are omitted or various inhibitors at concentrations indicated in the text are added. After incubation for 10 min at 30°C, the reaction is terminated by transferring 50 μL of the assay mixture onto a 20 mm square piece of phosphocellulose paper, which is washed 3 times in deionized water and twice in acetone. The radioactivity on each paper is determined by liquid scintillation counting.

Synonyms	Goe 6983
Molecular Weight	442.51
Formula	C26H26N4O3
CAS No.	133053-19-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.1 mg/mL (50 mM)

References and Literature

1. Gschwendt M, et al. FEBS Lett, 1996, 392(2), 77-80. 2. Peterman EE, et al. J Cardiovasc Pharmacol, 2004, 43(5), 645-656. 3. Young LH, et al. Cardiovasc Drug Rev, 2005, 23(3), 255-272. 4. Andresen BT, et al. Hypertension, 2001, 37(2 Part 2), 635-639. 5. Kumar A, et al. J Biol Chem, 2004, 279(23), 24255-24264. 6. Zhang Y, Wang Z, Cao J, et al. Physiological crosstalk between the Mel1a and Mel1c pathways modulates melatonin-mediated, monochromatic light combination-induced bursa B-lymphocyte proliferation in chickens[J]. 2020 8. Zhang Y, Wang Z, Cao J, et al. A Green and Blue Monochromatic Light Combination Therapy Reduces Oxidative Stress and Enhances B-Lymphocyte Proliferation through Promoting Melatonin Secretion[J]. Oxidative Medicine and Cellular Longevity. 2021, 2021. 9. Fan Y L, Li B, Zhao H P, et al. A function of fascin1 in the colony formation of mouse embryonic stem cells[J]. STEM CELLS. 2020.

Citations

1. Fan Y L, Li B, Zhao H P, et al. A function of fascin1 in the colony formation of mouse embryonic stem cells. Stem Cells. 2020, 38(9): 1078-1090 2. Zhang Y, Wang Z, Cao J, et al. A Green and Blue Monochromatic Light Combination Therapy Reduces Oxidative Stress and Enhances B-Lymphocyte Proliferation through Promoting Melatonin Secretion. Oxidative Medicine and Cellular Longevity. 2021, 2021. 3. Ning S, Wang Z, Cao J, et al. Mel1c Mediated Monochromatic Light-Stimulated IGF-I Synthesis through the Intracellular Gαq/PKC/ERK Signaling Pathway. International journal of molecular sciences. 2019, 20(7): 1682. 4. Wang D, Wang Y, Di X, et al.Cortical tension drug screen links mitotic spindle integrity to Rho pathway.Current Biology.2023

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library TGF-beta/Smad Compound Library Bioactive Compounds Library Max Anti-Cardiovascular Disease Compound Library Bioactive Compound Library Cytoskeletal Signaling Pathway Compound Library Anti-Aging Compound Library Reprogramming Compound Library Bioactive Lipid Compound Library

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Keywords

Go 6983 133053-19-7 Chromatin/Epigenetic Cytoskeletal Signaling PKC G? 6983 Go6983 inhibit Go-6983 Inhibitor Goe6983 Goe-6983 Protein kinase C Goe 6983 inhibitor

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