Home TGF-beta/Smad PKC inhibitor Go 6983

연구용

Go 6983 PKC inhibitor

제품 번호S2911

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; this compound is less potent to PKCζ and inactive to PKCμ.
Go 6983 PKC inhibitor Chemical Structure

화학 구조

분자량: 442.51

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품질 관리 (Quality Control)

배치: 순도: 99.79%
99.79

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
PC12 Function assay 0.5 μM GO6983 blocked the effect of PMA on the activation of Akt and MAPK induced by IGF-1 10788447
PC-3 Function assay 1 μM 2 h Gö6983 abrogates the TPA-induced RGFR transactivation response 15897236
HCT116 Function assay 2 μM 8 h attenuated PMA-induced FLIP mRNA expression 16052516
HT29 Function assay 2 μM 8 h attenuated PMA-induced FLIP mRNA expression 16052516
KM20 Function assay 2 μM 8 h attenuated PMA-induced FLIP mRNA expression 16052516
KM12C Function assay 2 μM 8 h attenuated PMA-induced FLIP mRNA expression 16052516
Caco-2 Function assay 2 μM 8 h completely attenuated PMA-induced FLIP mRNA expression 16052516
A549 Function assay 10 μM 1 h markedly inhibited ATPγS-stimulated NADPH oxidase activity and H2O2 and/or ROS generation 23326583
HeLa Function assay 2 μM 48 h suppressed the effect of PMA on apicularen A-induced cytotoxicity 24447339
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
HEK293 Function assay Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in human HEK293 cells transfected with rabbit L-type calcium channel subunits, IC50 = 20 μM. ChEMBL
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 442.51 화학식

C26H26N4O3

 보관 (수령일로부터)
CAS 번호 133053-19-7 SDF 다운로드 원액 보관

동의어 GOE 6983, Gö 6983 Smiles CN(C)CCCN1C=C(C2=C1C=CC(=C2)OC)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

용해도 (Solubility)

In vitro
배치:

DMSO : 89 mg/mL (201.12 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
PKCγ
(Cell-free assay)
6 nM
PKCα
(Cell-free assay)
7 nM
PKCβ
(Cell-free assay)
7 nM
PKCδ
(Cell-free assay)
10 nM
PKCζ
(Cell-free assay)
60 nM
시험관 내(In vitro)

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

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.

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.

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

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.

키나아제 분석
Binding assay
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.
생체 내(In vivo)

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

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/11230348/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15024016/
  • [6] https://pubmed.ncbi.nlm.nih.gov/19259669/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot PKCη / PKCα / PKCδ / PKCε
S2911-WB1
22892130