연구용

GSK650394 SGK 억제제

제품 번호S7209

GSK650394는 혈청 및 글루코코르티코이드 조절 키나아제-1(SGK1)과 SGK2에 대해 각각 62 nM 및 103 nM의 IC50을 갖는 SGK1 및 SGK2 억제제입니다.

화학 구조

분자량: 382.45

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품질 관리

배치: 순도: 99.92%

99.92

관련 타겟	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
기타 SGK 억제제	EMD638683 PROTAC SGK3 degrader-1

세포 배양, 처리 및 작업 농도

세포주	분석 유형	활성 설명
human M-1 cells	Function assay	Inhibition of SGK1-mediated epithelial sodium channel activity in human M-1 cells assessed as short circuit current by whole cell electrophysiological transepithelial experiment, IC50=0.58 μM
human MV-4-11 cell	Growth inhibition assay	Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.1649 μM
human Daoy cell	Growth inhibition assay	Inhibition of human Daoy cell growth in a cell viability assay, IC50=0.51532 μM
human BFTC-905 cell	Growth inhibition assay	Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=0.78455 μM
human KM12 cell	Growth inhibition assay	Inhibition of human KM12 cell growth in a cell viability assay, IC50=0.85069 μM
human GDM-1 cell	Growth inhibition assay	Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.87937 μM
human RT-112 cell	Growth inhibition assay	Inhibition of human RT-112 cell growth in a cell viability assay, IC50=1.02782 μM
human MONO-MAC-6 cell	Growth inhibition assay	Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=1.18097 μM
human HUTU-80 cell	Growth inhibition assay	Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.30172 μM
human HGC-27 cell	Growth inhibition assay	Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=1.30821 μM
human LCLC-97TM1 cell	Growth inhibition assay	Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=1.36768 μM
human LXF-289 cell	Growth inhibition assay	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.40152 μM
human HLE cell	Growth inhibition assay	Inhibition of human HLE cell growth in a cell viability assay, IC50=1.42683 μM
human RKO cell	Growth inhibition assay	Inhibition of human RKO cell growth in a cell viability assay, IC50=1.57869 μM
human SNG-M cell	Growth inhibition assay	Inhibition of human SNG-M cell growth in a cell viability assay, IC50=1.79853 μM
human MCF7 cell	Growth inhibition assay	Inhibition of human MCF7 cell growth in a cell viability assay, IC50=1.8178 μM
human A431 cell	Growth inhibition assay	Inhibition of human A431 cell growth in a cell viability assay, IC50=1.85902 μM
human BC-3 cell	Growth inhibition assay	Inhibition of human BC-3 cell growth in a cell viability assay, IC50=1.87094 μM
human A427 cell	Growth inhibition assay	Inhibition of human A427 cell growth in a cell viability assay, IC50=1.87611 μM
human SW620 cell	Growth inhibition assay	Inhibition of human SW620 cell growth in a cell viability assay, IC50=1.92816 μM
human HOS cell	Growth inhibition assay	Inhibition of human HOS cell growth in a cell viability assay, IC50=1.97312 μM
human MFH-ino cell	Growth inhibition assay	Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=1.98658 μM
human TE-12 cell	Growth inhibition assay	Inhibition of human TE-12 cell growth in a cell viability assay, IC50=1.99128 μM
human KU812 cell	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=2.1871 μM
human NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=2.19053 μM
human BC-1 cell	Growth inhibition assay	Inhibition of human BC-1 cell growth in a cell viability assay, IC50=2.51651 μM
human TE-15 cell	Growth inhibition assay	Inhibition of human TE-15 cell growth in a cell viability assay, IC50=2.59181 μM
human T84 cell	Growth inhibition assay	Inhibition of human T84 cell growth in a cell viability assay, IC50=2.60446 μM
human SW1710 cell	Growth inhibition assay	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=2.70082 μM
human CAL-12T cell	Growth inhibition assay	Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=2.71158 μM
human NKM-1 cell	Growth inhibition assay	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=2.76731 μM
human OCUB-M cell	Growth inhibition assay	Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=2.78861 μM
human 786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=2.94825 μM
human EW-13 cell	Growth inhibition assay	Inhibition of human EW-13 cell growth in a cell viability assay, IC50=3.01558 μM
human 5637 cell	Growth inhibition assay	Inhibition of human 5637 cell growth in a cell viability assay, IC50=3.20669 μM
human PA-1 cell	Growth inhibition assay	Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.33083 μM
human NCI-H2122 cell	Growth inhibition assay	Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=3.333 μM
human NCI-H460 cell	Growth inhibition assay	Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=3.4041 μM
human CHL-1 cell	Growth inhibition assay	Inhibition of human CHL-1 cell growth in a cell viability assay, IC50=3.49665 μM
human MOLT-16 cell	Growth inhibition assay	Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=3.51555 μM
human HCT-15 cell	Growth inhibition assay	Inhibition of human HCT-15 cell growth in a cell viability assay, IC50=3.62842 μM
human G-361 cell	Growth inhibition assay	Inhibition of human G-361 cell growth in a cell viability assay, IC50=3.71745 μM
human SK-LU-1 cell	Growth inhibition assay	Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=3.97014 μM
human ES4 cell	Growth inhibition assay	Inhibition of human ES4 cell growth in a cell viability assay, IC50=4.06069 μM
human TE-8 cell	Growth inhibition assay	Inhibition of human TE-8 cell growth in a cell viability assay, IC50=4.11582 μM
human IGR-1 cell	Growth inhibition assay	Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=4.233 μM
human SW954 cell	Growth inhibition assay	Inhibition of human SW954 cell growth in a cell viability assay, IC50=4.46124 μM
human A375 cell	Growth inhibition assay	Inhibition of human A375 cell growth in a cell viability assay, IC50=5.25492 μM
human CAL-27 cell	Growth inhibition assay	Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=5.33221 μM
human CAL-51 cell	Growth inhibition assay	Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=5.35583 μM
human SK-LMS-1 cell	Growth inhibition assay	Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=5.38255 μM
human HT-1080 cell	Growth inhibition assay	Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=5.49347 μM
human NCI-H1299 cell	Growth inhibition assay	Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=5.98557 μM
human HT-29 cell	Growth inhibition assay	Inhibition of human HT-29 cell growth in a cell viability assay, IC50=7.26843 μM
human A388 cell	Growth inhibition assay	Inhibition of human A388 cell growth in a cell viability assay, IC50=7.59965 μM
human SK-MEL-30 cell	Growth inhibition assay	Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=7.97215 μM
human CMK cell	Growth inhibition assay	Inhibition of human CMK cell growth in a cell viability assay, IC50=8.25377 μM
human HuP-T4 cell	Growth inhibition assay	Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50=8.50234 μM
human SF126 cell	Growth inhibition assay	Inhibition of human SF126 cell growth in a cell viability assay, IC50=8.80208 μM
human MKN1 cell	Growth inhibition assay	Inhibition of human MKN1 cell growth in a cell viability assay, IC50=9.18565 μM
human LoVo cell	Growth inhibition assay	Inhibition of human LoVo cell growth in a cell viability assay, IC50=9.91292 μM
human HEL cell	Growth inhibition assay	Inhibition of human HEL cell growth in a cell viability assay, IC50=10.68 μM
human SW872 cell	Growth inhibition assay	Inhibition of human SW872 cell growth in a cell viability assay, IC50=13.6896 μM
human SW982 cell	Growth inhibition assay	Inhibition of human SW982 cell growth in a cell viability assay, IC50=13.7916 μM
human HuH-7 cell	Growth inhibition assay	Inhibition of human HuH-7 cell growth in a cell viability assay, IC50=18.2783 μM
human DU-145 cell	Growth inhibition assay	Inhibition of human DU-145 cell growth in a cell viability assay, IC50=20.4955 μM
human MC116 cell	Growth inhibition assay	Inhibition of human MC116 cell growth in a cell viability assay, IC50=21.2676 μM
human H4 cell	Growth inhibition assay	Inhibition of human H4 cell growth in a cell viability assay, IC50=21.4244 μM
human SK-MEL-3 cell	Growth inhibition assay	Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=30.0228 μM
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	382.45	화학식	C₂₅H₂₂N₂O₂	보관 (수령일로부터)	3년-20°C분말
CAS 번호	890842-28-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O

용해도

In vitro
배치:

DMSO : 76 mg/mL (198.71 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 76 mg/mL (198.71 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 76 mg/mL (198.71 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 76 mg/mL (198.71 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:
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.
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	0.500mg/ml (1.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	3.800mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 76 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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.
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.

생체 내 제형 계산기 (투명한 용액)

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

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

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

Targets/IC₅₀/Ki	SGK1 (Cell-free assay) 62 nM SGK2 (Cell-free assay) 103 nM
시험관 내(In vitro)	GSK650394는 SCC 분석에서 IC50 0.6 μM로 SGK1 매개 상피 수송을 억제합니다. LNCaP 세포에서 이 화합물은 안드로겐 매개 Nedd4-2 인산화 증강 및 안드로겐 매개 세포 성장을 억제합니다.이 화합물은 코르티솔 유발 신경 발생 감소, 헤지호그 신호 전달 변화, GR 핵 전좌를 상쇄합니다. [2] 인플루엔자 vRNP의 A549 세포 내 세포질 수출을 저해하여 인플루엔자 바이러스 복제를 억제합니다.
키나아제 분석	신틸레이션 근접 분석법(SPA)
키나아제 분석	SGK1 S422D (60–431 aa; 최종 농도 0.275 μg/mL) 또는 SGK2 (최종 농도 0.875 μg/mL)는 50 mM Tris (pH 7.5), 0.1 mM EGTA, 0.1 mM EDTA, 10 mM MgCl₂, 0.1% β-메르캅토에탄올, 1 mg/mL BSA 및 ATP(최종 농도 0.15 mM)로 구성된 완충액에서 30°C에서 30분간 배양됩니다. SGK2는 SGK1과 정확히 동일한 방법으로 준비되나, 전체 길이 단백질에 해당합니다. 반응 완충액에 최종 농도 75 μM의 비오틴화 CROSStide 펩타이드와 2×10⁶ cpm에 해당하는 γ³²P-ATP를 함유한 용액을 준비한다. 96-웰 플레이트에서 활성화된 효소 혼합물 25 μL에 이 화합물 5 μL를 첨가한다. 여기에 CROSStide 혼합물 20μL를 첨가하고 실온에서 1시간 동안 배양합니다. 다음으로, 0.1M EDTA, pH 8.0 PBS 용액에 현탁된 스트렙타비딘 코팅 SPA 비드(25mg/mL 슬러리) 50μL를 첨가합니다. 플레이트를 밀봉한 뒤 2000 rpm에서 8분간 원심 분리하고, Packard TopCount NXT 섬광 계수기로 웰당 30초 동안 측정하여 신호를 검출합니다. 이 화합물에 의한 SGK1 및 SGK2 활성 억제의 IC50 값은 GraphPad Prism 3 소프트웨어를 사용하여 계산됩니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/18794135/ [2] https://pubmed.ncbi.nlm.nih.gov/23650397/ [3] https://pubmed.ncbi.nlm.nih.gov/23487453/

적용 분야

방법	바이오마커	PMID
Western blot	p-SGK2 / SGK2 p-SGK1 / SGK1 c-Jun / NRF2 p21 / LC3 / p62 / PARP / Cleaved PARP	26392083
Immunofluorescence	LC3	29017179
Growth inhibition assay	Cell viability	29017179

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