연구용
SB216763 GSK-3 inhibitor
제품 번호: S1075
화학 구조
분자량: 371.22
바로가기
품질 관리 (Quality Control)
배치:
순도:
99.98%
99.98
세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| HEK293 | Function assay | Glycogen synthase activity of HEK293 cells, inhibition of GSK3-beta, EC50=0.2μM | 12941331 | |||
| HEK293 | Function assay | Effective concentration of compound against glycogen synthase kinase-3 in HEK293 cells, EC50=0.2μM | 15149684 | |||
| MIAPaCa2 | Growth inhibition assay | 72 hrs | Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay, IC50=25μM | 19338355 | ||
| ST14A | Function assay | 6 hrs | Inhibition of GSK-3-beta-mediated Wnt signaling in human ST14A cells assessed as increase in accumulation of beta-casein around nucleus after 6 hrs by microscopic analysis | 20708937 | ||
| neural precursor cells | Function assay | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 17417631 | |||
| ReNcell VM | Antiproliferative assay | 3 uM | 72 hrs | Antiproliferative activity against human ReNcell VM cells assessed as reduction of cell proliferation at 3 uM after 72 hrs | 20708937 | |
| HepG2 | Function assay | 34 uM | 12 hrs | Increase in glucose incorporation in human HepG2 cells at 34 uM after 12 hrs by glucose assay | 25467150 | |
| 3T3L1 | Function assay | 34 uM | 12 hrs | Increase in glucose incorporation in mouse 3T3L1 cells at 34 uM after 12 hrs by glucose assay | 25467150 | |
| HepG2 | Function assay | 34 uM | 12 hrs | Inhibition of GSK3beta in human HepG2 cells assessed as decrease in ratio of phosphorylated GS/GS at 34 uM after 12 hrs by Western blot analysis | 25467150 | |
| Sf9 | Function assay | 30 min | Inhibition of GSK3beta (unknown origin) expressed in Sf9 cells using GS1 as substrate and [gamma32]ATP after 30 min by scinitllation counting, IC50=0.03388μM | SANGER | ||
| human HDLM-2 cell | Growth inhibition assay | Inhibition of human HDLM-2 cell growth in a cell viability assay, IC50=0.20984 μM | SANGER | |||
| human NCI-H1770 cell | Growth inhibition assay | Inhibition of human NCI-H1770 cell growth in a cell viability assay. IC50=0.29392 μM | SANGER | |||
| human HOP-62 cell | Growth inhibition assay | Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.85256 μM | SANGER | |||
| human JAR cell | Growth inhibition assay | Inhibition of human JAR cell growth in a cell viability assay, IC50=1.21044 μM | SANGER | |||
| human K5 cell | Growth inhibition assay | Inhibition of human K5 cell growth in a cell viability, IC50=1.53698 μM | SANGER | |||
| human MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=2.69685 μM | SANGER | |||
| human BT-549 cell | Growth inhibition assay | Inhibition of human BT-549 cell growth in a cell viability assay, IC50=5.29376 μM | SANGER | |||
| human LB2241-RCC cell | Growth inhibition assay | Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=6.42874 μM | SANGER | |||
| human GAMG cell | Growth inhibition assay | Inhibition of human GAMG cell growth in a cell viability assay, IC50=6.65409 μM | SANGER | |||
| human HMV-II cell | Growth inhibition assay | Inhibition of human HMV-II cell growth in a cell viability assay, IC50=7.67607 μM | SANGER | |||
| human RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=8.24141 μM | SANGER | |||
| human NCI-H1993 cell | Growth inhibition assay | Inhibition of human NCI-H1993 cell growth in a cell viability assay, IC50=8.36534 μM | SANGER | |||
| human IST-SL1 cell | Growth inhibition assay | Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=9.0204 μM | SANGER | |||
| human SK-OV-3 cell | Growth inhibition assay | Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=9.1002 μM | SANGER | |||
| human ESS-1 cell | Growth inhibition assay | Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=9.59872 μM | SANGER | |||
| human G-361 cell | Growth inhibition assay | Inhibition of human G-361 cell growth in a cell viability assay, IC50=10.1798 μM | SANGER | |||
| human ALL-PO cell | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=10.3477 μM | SANGER | |||
| human NB5 cell | Growth inhibition assay | Inhibition of human NB5 cell growth in a cell viability assay, IC50=11.2157 μM | SANGER | |||
| human DU-145 cell | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=11.6535 μM | SANGER | |||
| human NMC-G1 cell | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=11.7264 μM | SANGER | |||
| human RPMI-7951 cell | Growth inhibition assay | Inhibition of human RPMI-7951 cell growth in a cell viability assay. IC50=11.7864 μM | SANGER | |||
| human NCI-H2009 cell | Growth inhibition assay | Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=13.2427 μM | SANGER | |||
| human LoVo cell | Growth inhibition assay | Inhibition of human LoVo cell growth in a cell viability assay, IC50=13.3771 μM | SANGER | |||
| human A2058 cell | Growth inhibition assay | Inhibition of human A2058 cell growth in a cell viability assay, IC50=13.469 μM | SANGER | |||
| human D-566MG cell | Growth inhibition assay | Inhibition of human D-566MG cell growth in a cell viability assay, IC50=13.9481 μM | SANGER | |||
| human QIMR-WIL cell | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=15.6394 μM | SANGER | |||
| human S-117 cell | Growth inhibition assay | Inhibition of human S-117 cell growth in a cell viability assay, IC50=16.4022 μM | SANGER | |||
| human YH-13 cell | Growth inhibition assay | Inhibition of human YH-13 cell growth in a cell viability assay, IC50=16.6865 μM | SANGER | |||
| human IGROV-1 cell | Growth inhibition assay | Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=17.2001 μM | SANGER | |||
| human BHT-101 cell | Growth inhibition assay | Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=17.6099 μM | SANGER | |||
| human MKN45 cell | Growth inhibition assay | Inhibition of human MKN45 cell growth in a cell viability assay, IC50=18.4128 μM | SANGER | |||
| human A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50=19.4549 μM | SANGER | |||
| human U-266 cell | Growth inhibition assay | Inhibition of human U-266 cell growth in a cell viability assay, IC50=20.8797 μM | SANGER | |||
| human BFTC-905 cell | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=21.1879 μM | SANGER | |||
| human BxPC-3 cell | Growth inhibition assay | Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=21.3554 μM | SANGER | |||
| human NCI-SNU-1 cell | Growth inhibition assay | Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50=21.5558 μM | SANGER | |||
| human SF539 cell | Growth inhibition assay | Inhibition of human SF539 cell growth in a cell viability assay, IC50=22.0198 μM | SANGER | |||
| human VA-ES-BJ cell | Growth inhibition assay | Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=22.5763 μM | SANGER | |||
| human HuO-3N1 cell | Growth inhibition assay | Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=22.6151 μM | SANGER | |||
| human EM-2 cell | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay, IC50=22.6689 μM | SANGER | |||
| human T98G cell | Growth inhibition assay | Inhibition of human T98G cell growth in a cell viability assay, IC50=23.3009 μM | SANGER | |||
| human SW1783 cell | Growth inhibition assay | Inhibition of human SW1783 cell growth in a cell viability assay, IC50=23.5243 μM | SANGER | |||
| human NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=23.8512 μM | SANGER | |||
| human KOSC-2 cell | Growth inhibition assay | Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=24.1292 μM | SANGER | |||
| human SW48 cell | Growth inhibition assay | Inhibition of human SW48 cell growth in a cell viability assay, IC50=24.6067 μM | SANGER | |||
| human NCI-H28 cell | Growth inhibition assay | Inhibition of human NCI-H28 cell growth in a cell viability assay, IC50=25.2104 μM | SANGER | |||
| human 5637 cell | Growth inhibition assay | Inhibition of human 5637 cell growth in a cell viability assay, IC50=25.8111 μM | SANGER | |||
| human NB69 cell | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50=26.1764 μM | SANGER | |||
| human HT-29 cell | Growth inhibition assay | Inhibition of human HT-29 cell growth in a cell viability assay, IC50=27.1752 μM | SANGER | |||
| human PFSK-1 cell | Growth inhibition assay | Inhibition of human PFSK-1 cell growth in a cell viability assay, IC50=27.593 μM | SANGER | |||
| human UACC-257 cell | Growth inhibition assay | Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=27.743 μM | SANGER | |||
| human D-423MG cell | Growth inhibition assay | Inhibition of human D-423MG cell growth in a cell viability assay, IC50=27.9106 μM | SANGER | |||
| human NH-12 cell | Growth inhibition assay | Inhibition of human NH-12 cell growth in a cell viability assay, IC50=28.4059 μM | SANGER | |||
| human DEL cell | Growth inhibition assay | Inhibition of human DEL cell growth in a cell viability assay, IC50=29.0474 μM | SANGER | |||
| human LS-513 cell | Growth inhibition assay | Inhibition of human LS-513 cell growth in a cell viability assay, IC50=30.1334 μM | SANGER | |||
| human NBsusSR cell | Growth inhibition assay | Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=30.5678 μM | SANGER | |||
| human BV-173 cell | Growth inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay, IC50=30.7649 μM | SANGER | |||
| human A101D cell | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50=30.9784 μM | SANGER | |||
| human LU-134-A cell | Growth inhibition assay | Inhibition of human LU-134-A cell growth in a cell viability assay, IC50=31.0238 μM | SANGER | |||
| human ES3 cell | Growth inhibition assay | Inhibition of human ES3 cell growth in a cell viability assay, IC50=31.3376 μM | SANGER | |||
| human NY cell | Growth inhibition assay | Inhibition of human NY cell growth in a cell viability assay, IC50=32.2965 μM | SANGER | |||
| human NCI-H1975 cell | Growth inhibition assay | Inhibition of human NCI-H1975 cell growth in a cell viability assay, IC50=32.3582 μM | SANGER | |||
| human A704 cell | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay, IC50=34.2059 μM | SANGER | |||
| human SK-MEL-24 cell | Growth inhibition assay | Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=34.2523 μM | SANGER | |||
| human SW1088 cell | Growth inhibition assay | Inhibition of human SW1088 cell growth in a cell viability assay, IC50=34.3452 μM | SANGER | |||
| human SK-MEL-1 cell | Growth inhibition assay | Inhibition of human SK-MEL-1 cell growth in a cell viability, IC50=34.714 μM | SANGER | |||
| human MOLT-4 cell | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=36.1467 μM | SANGER | |||
| human T47D cell | Growth inhibition assay | Inhibition of human T47D cell growth in a cell viability assay, IC50=37.1647 μM | SANGER | |||
| human SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=37.3608 μM | SANGER | |||
| human MKN7 cell | Growth inhibition assay | Inhibition of human MKN7 cell growth in a cell viability assay, IC50=38.0909 μM | SANGER | |||
| human CAL-72 cell | Growth inhibition assay | Inhibition of human CAL-72 cell growth in a cell viability assay, IC50=38.1178 μM | SANGER | |||
| human AGS cell | Growth inhibition assay | Inhibition of human AGS cell growth in a cell viability assay, IC50=38.2039 μM | SANGER | |||
| human BE-13 cell | Growth inhibition assay | Inhibition of human BE-13 cell growth in a cell viability assay, IC50=38.7783 μM | SANGER | |||
| human Calu-6 cell | Growth inhibition assay | Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=39.6964 μM | SANGER | |||
| human CAL-27 cell | Growth inhibition assay | Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=44.0054 μM | SANGER | |||
| human BB49-HNC cell | Growth inhibition assay | Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=44.0278 μM | SANGER | |||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)
| 분자량 | 371.22 | 화학식 | C19H12N2O2Cl2 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 280744-09-4 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | N/A | Smiles | CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl | ||
용해도 (Solubility)
|
In vitro |
DMSO
: 23 mg/mL
(61.95 mM)
Water : Insoluble Ethanol : Insoluble |
몰농도 계산기
희석 계산기
분자량 계산기
|
In vivo |
|||||
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 |
GSK-3α
(Cell-free assay) 34.3 nM
GSK-3β
(Cell-free assay) ~34.3 nM
|
|---|---|
| 시험관 내(In vitro) |
SB216763은 10 μM에서 96%의 억제율로 GSK-3β에 대해 유사한 효능을 나타내는 동시에, PKBα 및 PDK1을 포함한 다른 24개 단백질 키나아제에 대해서는 10 μM 초과의 IC50 값으로 최소한의 활성만을 보입니다. 이 화합물은 인간 간세포에서 3.6 μM의 EC50으로 글리코겐 합성을 자극하며, HEK293 세포에서 5 μM 농도에서 최대 2.5배 유도되는 β-catenin-LEF/TCF 조절 리포터 유전자의 용량 의존적 전사를 유도합니다. 이 화합물은 LY-294002 또는 칼륨 결핍에 의해 유도된 소뇌 과립 뉴런의 세포 사멸을 농도 의존적으로 보호하며, 3 μM에서 최대 신경 보호 효과를 나타내는데, 이는 염화리튬이 10 mM 농도를 필요로 하는 것과 대조적입니다. 이 화학물질은 3 μM 농도에서 NGF 존재 여부와 관계없이 LY-294002에 의해 유도된 닭 배근 신경절 감각 뉴런의 사멸을 완전히 방지합니다. 5 μM 처리 시 소뇌 과립 뉴런 내 뉴런 특이적 미세소관 관련 단백질 tau 또는 HEK293 세포 내 재조합 tau의 GSK-3 의존적 인산화를 현저히 억제하며, Wnt 매개 GSK-3 억제 효과를 모방하여 두 세포 모두에서 세포질 내 β-catenin 수치를 증가시킵니다. BXPC-3, MIA-PaCa2, PANC1, ASPC1 및 CFPAC를 포함한 췌장암 세포주에서 이 화합물을 25-50 μM 농도로 처리하면 용량 의존적으로 세포 생존력이 감소하며, GSK-3β의 특이적 하향 조절로 인해 72시간 후 세포 사멸이 50%까지 유의미하게 증가하지만, HMEC 또는 WI38 세포주에는 영향을 미치지 않습니다.
|
| 키나아제 분석 |
GSK-3 활성 분석
|
|
GSK-3 키나아제 활성은 1 nM 인간 GSK-3α, 50 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM Mg-아세트산, 7.5 mM β-머캅토에탄올, 5% (w/v) 글리세롤, 0.01% (w/v) Tween-20, 10% (v/v) DMSO 및 28 μM GS-2 펩타이드 기질의 최종 농도를 포함하는 반응 혼합물에서 다양한 농도의 SB 216763 존재 하에 측정됩니다. GS-2 펩타이드 서열은 GSK-3에 의해 인산화되는 글리코겐 합성효소의 영역에 해당합니다. 분석은 0.34 μCi [33P]γ-ATP를 첨가하여 시작됩니다. 총 ATP 농도는 10 μM입니다. 실온에서 30분간 배양한 후, 21 mM ATP를 포함하는 2.5% (v/v) H3PO4를 분석 부피의 1/3만큼 첨가하여 분석을 중단합니다. 샘플을 P30 인산셀룰로오스 매트에 점적하고 0.5% (v/v) H3PO4로 6회 세척합니다. 필터 매트는 Wallac betaplate 섬광 유체(scintillation fluid)가 포함된 샘플 백에 밀봉됩니다. 기질 펩타이드로의 33P 혼입은 Wallac microbeta 섬광 계수기(scintillation counter)에서 매트를 계수하여 결정됩니다.
|
|
| 생체 내(In vivo) |
SB216763을 20 mg/kg 용량으로 투여하면 bleomycin(BLM)으로 유도된 마우스 폐 염증 및 섬유화 모델에서 대식세포에 의한 염증성 사이토카인인 MCP-1 및 TNF-α의 생성을 유의하게 차단함으로써 폐 염증과 그에 따른 섬유화를 유의하게 예방하고, BLM을 투여한 마우스의 생존율을 유의하게 개선합니다. 이 화합물 처리는 폐포 상피 세포 손상을 억제함으로써 BLM으로 유도된 폐포염을 유의하게 감소시킵니다.
|
참조 |
|
적용 분야 (Applications)
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | c-Myb pGSK-3β / GSK-3β / E2F1 / β-catenin |
|
21795403 |
| Growth inhibition assay | Cell viability |
|
24779365 |
제품은 연구용으로만 사용됩니다. 인체에는 사용하지 마십시오. 환자에게 판매하지 않습니다.
©Copyright 2013 Selleck Chemicals. All Rights Reserved.