Go 6983 (Synonyms: Goe 6983;Go6983;Go-6983)

Name: Go 6983
Brand: GlpBio
SKU: GC16907
Availability: InStock
Rating: 5 (10 reviews)

Catalog No.GC16907

Go 6983 (GÖ 6983) est l'un des composés inhibiteurs de PKC du groupe bisindolylmaleimide. Go 6983 (GÖ 6983) a été capable de différencier entre la PKC mu et les autres isoenzymes de PKC.

Products are for research use only. Not for human use. We do not sell to patients.

Go 6983 Chemical Structure

Cas No.: 133053-19-7

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10mM (in 1mL DMSO)	83,00 $US	En stock
5mg	76,00 $US	En stock
10mg	138,00 $US	En stock
50mg	414,00 $US	En stock
100mg	640,00 $US	En stock

Tel：(909) 407-4943 Email: sales@glpbio.com

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Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

GlpBio Products Cited In Reputable Papers

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Description Protocol Chemical Properties Product Documents

Product Documents

Quality Control & SDS

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Purity: >98.00%

Protocol

Kinase experiment [1]:
Preparation Method	Phosphorylation reactions were carried out in a total volume of 100 μl, containing buffer C, 4 mM MgCl2, 10 μg PS, 100 nM TPA, 5 ul of a Sf158 cell extract as a source of recombinant PKCu or of Sf9 cell extracts as a source of other recombinant PKC isoenzymes, 10 ug of syntide 2 as substrate, and 35 μM ATP containing 1 μCi [y-32P] ATP. In some experiments PS and TPA were omitted or various inhibitors(including Go 6983 (Gö 6983)) at concentrations were added. After incubation for 10 min at 30°C, the reaction was terminated by transferring 50 ul of the assay mixture onto a 20 mm square piece of phosphocellulose paper (Whatman p81), which was washed 3 times in deionized water and twice in acetone.
Reaction Conditions	10^-1-10⁶nM Go 6983 (Gö 6983) for 10 min at 30°C
Applications	Go 6983 (Gö 6983) is a pan-PKC inhibitor that acts on PKCα, PKCβ, PKCγ and PKCδ with IC50 values of 7 nM, 7 nM, 6 nM and 10 nM, respectively. Go 6983 (Gö 6983) has a weak effect on PKCζ and inhibits the activity of PKCμ.
Cell experiment [2]:
Cell lines	MDA-MB-231 cells
Preparation Method	MDA-MB-231 cells were seeded in 96-well plates and incubated overnight. Next, various concentrations of Go 6983 (Gö 6983) (0, 0.625, 1.25, 2.5, 5, 10, 20, or 40 μM) were added to the cells to incubate for 24, 48 and 72 h. PMS (100 μL) and MTS (2 mL) were thoroughly mixed, and the resulting solution was added to each well of the 96-well plate. Finally, the optical density (OD) at 490 nm of each well was measured by using an enzyme-linked immunosorbent assay (ELISA) plate reader.
Reaction Conditions	Go 6983 (Gö 6983) (0, 0.625, 1.25, 2.5, 5, 10, 20, or 40 μM) for 24, 48 and 72 h
Applications	The IC50 of Go 6983 (Gö 6983) at 24, 48, and 72 h were 58.64, 22.07, and 12.93 μM, respectively.At the concentrations used in our experiments, Go 6983 (Gö 6983) has no toxic effects on MDA-MB-231 cells. Go 6983 (Gö 6983) inhibits invasion and migration of MDA-MB-231 cells.
Animal experiment [3]:
Animal models	Nude mice
Preparation Method	Twenty-four nude mice were divided randomly into the following four groups: Sham group, vehicle group, low dose group, and high dose group. MDA-MB-231 cells or PBS were injected into the humeral metaphysis of each mouse. After 14 days, the mice in the vehicle and sham groups were injected intraperitoneally with 100 μL of PBS, and high- and low-dose groups were injected intraperitoneally daily with 5 or 2.5 mg/kg Go 6983 (Gö 6983), respectively. All mice were sacrificed 28 days later, and tumor growth and bone destruction were observed by X-ray and microCT. The tumor tissues were examined histologically, and the long diameter, short diameter, and volume of the tumor were measured.
Dosage form	5 or 2.5 mg/kg Go 6983 (Gö 6983) for 28days
Applications	Go 6983 (Gö 6983) can inhibit breast cancer osteolysis in vivo.
References: [1]. Gschwendt M, Dieterich S,et,al.Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett. 1996 Aug 26;392(2):77-80. doi: 10.1016/0014-5793(96)00785-5. PMID: 8772178. [2]. Luan Z, Li J, et,al. GÖ6983 attenuates breast cancer-induced osteolysis by the apoptotic pathway. Cell Biol Int. 2020 Mar;44(3):838-847. doi: 10.1002/cbin.11281. Epub 2019 Dec 26. PMID: 31814221.

Go 6983 (GÖ 6983) is one of the bisindolylmaleimide group of PKC inhibitor compounds, Go 6983 (GÖ 6983) was able to differentiate between PKC mu and other PKC isoenzymes. Go 6983 (GÖ 6983) is a pan-PKC inhibitor that acts on PKCα, PKCβ, PKCγ and PKCδ with IC50 values of 7 nM, 7 nM, 6 nM and 10 nM, respectively. Go 6983 (GÖ 6983) has a weak effect on PKCζ and inhibits the activity of PKCµ^[3,4].

Go 6983 (GÖ 6983) inhibits invasion and migration of MDA-MB-231 cells. Go 6983 (GÖ 6983) activates the mitochondrial apoptosis pathway in MDA-MB-231 cell. Go 6983 (GÖ 6983) inhibits the Src pathway in MDA-MB-231 cells and inhibits phosphorylation of PKC^[2]. Platelet aggregation induced by epi was potentiated by RO 31-8220 (RO) or Go 6983 (GÖ 6983) ^[1]. Go 6983 (GÖ 6983) may exert cardioprotection by en- hancing endothelial NO release, which has been found to be cardioprotective in the setting of MI/R^[6].

Tumor volume, long diameter, and short diameter were all lower in the mice injected with Go 6983 (GÖ 6983) than in those of the vehicle control group (Figures 1B D). The volume of tumors in the high dose group was approximately one-third of those in the vehicle group, indicating that Go 6983 (GÖ 6983) suppresses the growth and bone metastasis of breast cancer^[2]. Go 6983 (GÖ 6983) (100 nM) significantly reduced PMN adherence to the endothelium and infiltration into the myocardium compared with I/R + PMN hearts, and significantly inhibited superoxide release from PMNs. In the presence of PMNs, Go 6983 (GÖ 6983) attenuated post-I/R cardiac contractile dysfunction, which may be related in part to decreased superoxide production^[5]. Go 6983 (GÖ 6983) was able to attenuate urotensin II-induced contraction in rat aorta, in this case, through inhibition of Ca 2+/calmodulin/MLC kinase^[7].

References:
[1]. Kim SY, Kim S, et,al. PKC inhibitors RO 31-8220 and GÖ 6983 enhance epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation. BMB Rep. 2011 Feb;44(2):140-5. doi: 10.5483/BMBRep.2011.44.2.140. PMID: 21345315.
[2]. Luan Z, Li J, et,al. GÖ6983 attenuates breast cancer-induced osteolysis by the apoptotic pathway. Cell Biol Int. 2020 Mar;44(3):838-847. doi: 10.1002/cbin.11281. Epub 2019 Dec 26. PMID: 31814221.
[3]. Gschwendt M, Dieterich S, et,al. Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett. 1996 Aug 26;392(2):77-80. doi: 10.1016/0014-5793(96)00785-5. PMID: 8772178.
[4]. Gschwendt M, Kittstein W, et,al. Differential effects of suramin on protein kinase C isoenzymes. A novel tool for discriminating protein kinase C activities. FEBS Lett. 1998 Jan 9;421(2):165-8. doi: 10.1016/s0014-5793(97)01530-5. PMID: 9468299.
[5]. Peterman EE, Taormina P 2nd, et,al. GÖ 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion. J Cardiovasc Pharmacol. 2004 May;43(5):645-56. doi: 10.1097/00005344-200405000-00006. PMID: 15071351.
[6]. Omiyi D, Brue RJ, et,al. Protein kinase C betaII peptide inhibitor exerts cardioprotective effects in rat cardiac ischemia/reperfusion injury. J Pharmacol Exp Ther. 2005 Aug;314(2):542-51. doi: 10.1124/jpet.104.082131. Epub 2005 May 5. PMID: 15878997.
[7]. Tasaki K, Hori M, et,al. Mechanism of human urotensin II-induced contraction in rat aorta. J Pharmacol Sci. 2004 Apr;94(4):376-83. doi: 10.1254/jphs.94.376. PMID: 15107577.

Cas No.	133053-19-7	SDF
Synonymes	Goe 6983;Go6983;Go-6983
Chemical Name	3-[1-[3-(dimethylamino)propyl]-5-methoxyindol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
Canonical SMILES	CN(C)CCCN1C=C(C2=C1C=CC(=C2)OC)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54
Formula	C₂₆H₂₆N₄O₃	M.Wt	442.51
Solubility	≥ 22.15mg/mL in DMSO	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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		1 mg	5 mg	10 mg
	1 mM	2.2598 mL	11.2992 mL	22.5984 mL
	5 mM	0.452 mL	2.2598 mL	4.5197 mL
	10 mM	0.226 mL	1.1299 mL	2.2598 mL

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 10 reference(s) in Google Scholar.)

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Go 6983 (Synonyms: Goe 6983;Go6983;Go-6983)

Avis des clients

GlpBio Citations

Bioactive Compounds Premium Provider

GlpBio Products Cited In Reputable Papers

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

Molarity Calculator

Dilution Calculator

In vivo Formulation Calculator (Clear solution)

Avis

Go 6983 (Synonyms: Goe 6983;Go6983;Go-6983)

Avis des clients

GlpBio Citations

Bioactive Compounds Premium Provider

GlpBio Products Cited In Reputable Papers

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

Molarity Calculator

Dilution Calculator

In vivo Formulation Calculator (Clear solution)

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