Go 6983

製品コードS2911 バッチS291103

印刷

化学情報

Synonyms

GOE 6983, Gö 6983

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₂₆N₄O₃

分子量

442.51

CAS No.

133053-19-7

Solubility (25°C)*

体外

DMSO

89 mg/mL (201.12 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Go 6983 (GOE 6983, Gö 6983) is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.
in vitro	Go 6983 (300 μM) suppresses PKCμ auto-phosphorylation by 20% reduction in NIH3T3 transfected with PKCμ. ^[1] In hearts reperfused with PMNs and this compound (100 nM), left ventricular developed pressure (LVDP) and the rate of LVDP recoveres to 89% and 74% of baseline values, respectively, significantly higher than PMNs alone. This chemical (100 nM) significantly reduces PMNs adherence to the endothelium and infiltration into the myocardium compared with Ischemia followed by reperfusion (I/R)+ PMN hearts, and significantly inhibits superoxide release from PMNs by 90%. It attenuates post-I/R cardiac contractile dysfunction in the presence of PMNs, which may be related in part to decreased superoxide production. ^[2] This inhibitor significantly inhibits antigen-induced superoxide release from leukocytes of patients previously sensitized to tree pollen. It inhibited intracellular Ca(2+) accumulation in human vascular tissue, suggesting a mechanism for its vasodilator properties. ^[3] This compound (1 μM) combined with Ro-31-8425 (390 nM) slightly inhibits Angiotensin II–induced PLD2 activity in PGSMCs. ^[4] It is isoform-specific PKC inhibitor that target the ATP binding site. It inhibits ΔPfPKB activity with an IC50 of 1 μM. In this chemical (5 μM)-treated cells, the number of rings in the following cycle is markedly less compared with the control cultures. This treatment (5 μM) results in an almost 60% decrease in formation of new rings in P. falciparum cultures. ^[5]
in vivo	Go6983 (22.0 μg/mouse, i.v.) strongly inhibits tumor metastasis by 51.2 % in a mouse pulmonary B16BL6 tumor model. ^[6]

製品説明

Go 6983 (GOE 6983, Gö 6983) is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.

in vitro

Go 6983 (300 μM) suppresses PKCμ auto-phosphorylation by 20% reduction in NIH3T3 transfected with PKCμ. ^[1]

In hearts reperfused with PMNs and this compound (100 nM), left ventricular developed pressure (LVDP) and the rate of LVDP recoveres to 89% and 74% of baseline values, respectively, significantly higher than PMNs alone. This chemical (100 nM) significantly reduces PMNs adherence to the endothelium and infiltration into the myocardium compared with Ischemia followed by reperfusion (I/R)+ PMN hearts, and significantly inhibits superoxide release from PMNs by 90%. It attenuates post-I/R cardiac contractile dysfunction in the presence of PMNs, which may be related in part to decreased superoxide production. ^[2]

This inhibitor significantly inhibits antigen-induced superoxide release from leukocytes of patients previously sensitized to tree pollen. It inhibited intracellular Ca(2+) accumulation in human vascular tissue, suggesting a mechanism for its vasodilator properties. ^[3]

This compound (1 μM) combined with Ro-31-8425 (390 nM) slightly inhibits Angiotensin II–induced PLD2 activity in PGSMCs. ^[4]

It is isoform-specific PKC inhibitor that target the ATP binding site. It inhibits ΔPfPKB activity with an IC50 of 1 μM. In this chemical (5 μM)-treated cells, the number of rings in the following cycle is markedly less compared with the control cultures. This treatment (5 μM) results in an almost 60% decrease in formation of new rings in P. falciparum cultures. ^[5]

in vivo

Go6983 (22.0 μg/mouse, i.v.) strongly inhibits tumor metastasis by 51.2 % in a mouse pulmonary B16BL6 tumor model. ^[6]

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	Phosphorylation reactions are carried out in a total volume of 100 μL, containing buffer C (50 mM Tris-HC1, 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℃, 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.
細胞アッセイ	細胞株	Cell-free assays
	濃度	IC50 of 7, 7, 6 and 10 nM for PKCα, PKCβ, PKCγ and PKCδ, respectively.
	反応時間
	実験の流れ
動物実験	動物モデル	Mice bearing B16BL6 tumors
	投薬量	22 μg/mouse
	投与方法	i.v.

参考

https://pubmed.ncbi.nlm.nih.gov/8772178/
https://pubmed.ncbi.nlm.nih.gov/15071351/
https://pubmed.ncbi.nlm.nih.gov/16252018/

https://pubmed.ncbi.nlm.nih.gov/11230348/
https://pubmed.ncbi.nlm.nih.gov/15024016/
https://pubmed.ncbi.nlm.nih.gov/19259669/

+ 展开

カスタマーフィードバック

: Data from [Data independently produced by , , Amino Acids, 2016, 48(5):1185-97]

: Data from [Data independently produced by , , Cellular Signalling, 2014, 26(11): 2436-2445]

: Data from [Data independently produced by , , PLoS One, 2015, 10(4): e0122179 ]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Derivation of embryonic stem cells across avian species [ Nat Biotechnol, 2025, 10.1038/s41587-025-02833-3]	PubMed: 41028831
IDH status dictates oHSV mediated metabolic reprogramming affecting anti-tumor immunity [ Nat Commun, 2025, 16(1):3874]	PubMed: 40274791
METTL3-dependent m6A RNA methylation regulates transposable elements and represses human naïve pluripotency through transposable element-derived enhancers [ Nucleic Acids Res, 2025, 53(8)gkaf349]	PubMed: 40298111
Reciprocal regulation of MMP-28 and EGFR is required for sustaining proliferative signaling in PDAC [ J Exp Clin Cancer Res, 2025, 44(1):68]	PubMed: 39994761
Caragana jubata ethanol extract ameliorates the symptoms of STZ-HFD-induced T2DM mice by PKC/GLUT4 pathway [ J Ethnopharmacol, 2025, 339:119171]	PubMed: 39613004
Interaction and regulatory expression of Polycomb and NuRD complexes in mouse embryonic stem cell under PKC inhibition [ Sci Rep, 2025, 15(1):27204]	PubMed: 40715296
Regulation of PKCi-mediated pluripotency and gene expression by polycomb complex 1 in mouse embryonic stem cells [ Am J Transl Res, 2025, 17(6):4455-4469]	PubMed: 40672580
PTPN22-CD45 dual phosphatase retrograde feedback enhances TCR signaling and autoimmunity [ Sci Adv, 2025, 11(36):eadw2568]	PubMed: 40911684
Experimental study on small molecule combinations inducing reprogramming of rat fibroblasts into functional neurons [ Zhejiang Da Xue Xue Bao Yi Xue Ban, 2024, 53(4):498-508]	PubMed: 39183062
High-throughput chemogenetic drug screening reveals PKC-RhoA/PKN as a targetable signaling vulnerability in GNAQ-driven uveal melanoma [ Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244]	PubMed: 37858338

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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