연구용

PD 98059 MEK 억제제

제품 번호S1177

PD98059는 세포 없는 분석에서 IC50이 2 μM인 비-ATP 경쟁적 MEK 억제제로, MEK-1 매개 MAPK 활성화를 특이적으로 억제합니다. ERK1 또는 ERK2를 직접 억제하지 않습니다. PD98059는 아릴 탄화수소 수용체(AHR)의 리간드이며 AHR 길항제로 기능합니다.
PD 98059 MEK 억제제 Chemical Structure

화학 구조

분자량: 267.28

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품질 관리

배치: 순도: 99.92%
99.92

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
TE4 Function Assay 50 μM 48 h DMSO upregulates the expression of HLA class I 24244023
MKN7 Function Assay 50 μM 48 h DMSO increases expression of HLA-A02 or HLA-A24 molecules 24244023
OE19 Function Assay 50 μM 48 h DMSO increases expression of HLA-A02 or HLA-A24 molecules 24244023
NCI-N87  Function Assay 50 μM 48 h DMSO increases expression of HLA-A02 or HLA-A24 molecules 24244023
KATOIII  Function Assay 50 μM 48 h DMSO increases expression of HLA-A02 or HLA-A24 molecules 24244023
NUGC3 Function Assay 50 μM 48 h DMSO increases expression of HLA-A02 or HLA-A24 molecules 24244023
NUGC2 Function Assay 50 μM 48 h DMSO increases expression of HLA-A02 or HLA-A24 molecules 24244023
SGC-7901  Apoptosis Assay 20 μM 24 h inhibits CP-mediated apoptosis 24241351
MG-63 Function Assay 20 μM 0.5 h blocks the CH-induced phosphorylated ELK1 protein expression 24239640
ARPE-19 Function Assay 20 μM 0.5 h inhibits Apelin-induced phosphorylation of Erk and Akt 24227918
CRL-2302 Function Assay 20 μM 0.5 h inhibits Apelin-induced phosphorylation of Erk and Akt 24227918
MCF-7 Apoptosis Assay 20 μM 1 h increases caspase-9 enzyme activity 24216289
MCF-7 Function Assay 20 μM 1 h abolishes expression of phosphorylated ERK co-treatment with conjugate 24216289
7402 Apoptosis Assay 30 μM 5 d decreases cell proliferation 24211253
HT-29 Function Assay 20 μM 48 h reduces the BNIP3 expression pre-treated with 5-aza-dC 24211581
DLD-1  Function Assay 20 μM 48 h reduces the BNIP3 expression pre-treated with 5-aza-dC 24211581
7721 Apoptosis Assay 30 μM 5 d decreases cell proliferation 24211253
SGC7901  Apoptosis Assay 50 μM 24/48/72 h DMSO induces apoptosis combined with JAK2 shRNA 24178240
SMMC7721 Function Assay 25/50 μM 24 h suppresses the expression of p-Akt or p-ERK1/2  24168056
MCF-7 Growth Inhibition Assay 10 μM 48h DMSO reverses BNF-induced cell cycle arrest 24163404
Caco-2 Function Assay 50 μM 48h DMSO enhances the mRNA levels of SCNN1A,FXYD3, LCT, LOX, HIF3A, ZG16, PDE6A and LGALS16 genes co-treated with Dex 24161695
HAECs Function Assay 10 μM 1 h  attenuates TNF-α-stimulated ICAM-1 and VCAM-1 expression 24134657
Ca9-22 Function Assay 3 μM 1 h abolishes the ability of HbR to induce IL-8 production 24126532
Ca9-22 Function Assay 3 μM 1/2 h reduces HbR-induced ATF-2 phosphorylation 24126532
AGS Function Assay 10 μM  0.5 h inhibits the upregulation of the IL-8 gene 24106166
Caco-2  Apoptosis Assay 10 μM 24 h decreases cell apoptosis induced by 5-FU 24095863
A549 Function Assay 50 μM 2 h blocks ERK phosphorylation mediated by 1,2-NQ 24067727
HPMC Function Assay 10 μM 48 h reverses the changes in cell morphology induced by HGPDS 24042838
HCT-8 Apoptosis Assay 10 μM 24 h decreases cell apoptosis induced by 5-FU 24095863
HPMC Apoptosis Assay 10 μM 24 h reverses decrease in cell viability induced by HGPDS 24042838
MGC803  Apoptosis Assay 20 μM 1 h inhibits apoptosis induced by IFN-α and 5′-DFUR 24027750
SGC7901 Apoptosis Assay 20 μM 1 h inhibits apoptosis induced by IFN-α and 5′-DFUR 24027750
G292  Apoptosis Assay 30 μM 2 h restores capsaicin-induced cell death 24012930
COLO205 Apoptosis Assay 10/20/40 μM 24 h induces DNA ladder formation 24019108
BxPC-3 Function Assay 10 μM  6 h increase miR-143 expression 23973710
HPAF-II Function Assay 10 μM  6 h increase miR-143 expression 23973710
HepG2 Function Assay 40 μM 6/12 h inhibits the increase of p-ERK1 and p-c-Jun protein expression by PL 23942851
HL-60 Apoptosis Assay 50 μM 1 h rescues BA145 mediated apoptosis 23948751
LNCaP  Function Assay 10 μM  1 h decreases the EGF upregulated p-YB-1 23838318
HUVECs Function Assay 25 μM 1 h increase NF-κB p65 nuclear translocation 23901008
HL60  Function Assay 20 μM 72 h DMSO inhibits -induced CD11b expression 23825585
NB4  Function Assay 10 μM  72 h DMSO inhibits -induced CD11b expression 23825585
EPOR/CR3 Function Assay 50 μM 3 h reduces EPO and/or IL-3-induced the tyrosine phosphorylation  23820731
HUASMCs Function Assay 10 μM  24 h inhibits Ang II-induced ERK1/2 phosphorylation level 23816468
HUASMCs Function Assay 10 μM  24 h diminishes Ang II-caused SOCS3 mRNA and protein expression  23816468
SGC7901 Function Assay 10 μM  24 h inhibits the expression of phosphorylated ERK1/2 23792588
MKN45 Growth Inhibition Assay 10 μM  24/48/72 h inhibits cell growth co-treated with DAPT 23792588
SGC7901 Growth Inhibition Assay 10 μM  24/48/72 h inhibits cell growth co-treated with DAPT 23792588
MKN45 Function Assay 10 μM  24 h inhibits the expression of phosphorylated ERK1/2 23792588
SGC7901 Apoptosis Assay 10 μM  24 h increases the DAPT-induced cell apoptosis 23792588
MKN45 Apoptosis Assay 10 μM  24 h increases the DAPT-induced cell apoptosis 23792588
BxPC-3 cells Growth Inhibition Assay 20 μM 0.5 h inhibits VEGF-A-regulated HUVEC growth and tube formation induced by PAR-2 AP 23764046
NB4  Apoptosis Assay 10/20/60 μM 1.5 h DMSO decreases cell viability co-treated 23735541
HepG2  Function Assay 20 μM 24 h inhibits the HO-1 protein expression co-treated 23707609
HUVECs Apoptosis Assay 2/4 μM 24/48 h induces cell death 23707520
KG-1  Apoptosis Assay 20 μM 12 h enhances cell apoptosis induced by S1 23706691
AML 1# Apoptosis Assay 20 μM 12 h enhances cell apoptosis induced by S1 23706691
A2780  Function Assay 20 μM 1 h blocks DTCD-induced DR5 expression 23696862
KYSE30 Function Assay 50 μM 48 h DMSO upregulates the expression of HLA class I 24244023
TE5 Function Assay 50 μM 48 h DMSO upregulates the expression of HLA class I 24244023
TE1 Function Assay 50 μM 48 h DMSO upregulates the expression of HLA class I 24244023
TE3 Function Assay 50 μM 48 h DMSO upregulates the expression of HLA class I 24244023
KYSE30 Function Assay 20/50/100 μM 48 h DMSO inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner 24244023
TE1 Function Assay 20/50/100 μM 48 h DMSO inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner 24244023
TE4 Function Assay 20/50/100 μM 48 h DMSO inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner 24244023
HT29 Function Assay 10 μM 2 h inhibits of JAK2, ERK1/2 and STAT3 phosphorylation 24265293
HepG2 Apoptosis Assay 20 μM 24 h inhibits ERK1/2 phosphorylation and enhances VB1-induced apoptosis 24247909
HepG2 Function Assay 20 μM 2 h enhances VB1-induced FOXO3a transcriptional activity 24247909
MC-3 Apoptosis Assay 10 μM 24 h potentiated MESC-induced apoptosis in cells 24270523
Raji  Function Assay 10 μM 1 h blocks hsBAFF induced Erk1/2 phosphorylation 24269630
Raji  Growth Inhibition Assay 10 μM 1 h inhibits the basal or hsBAFF-stimulated cell proliferation and viability 24269630
A549 Function Assay 30 μM 0.5 h DMSO inhibits thrombin-induced C/EBPβ Thr235 phosphorylation 24277696
HCSMCs Growth Inhibition Assay 10 μM 24 h blocks FABP4-induced HCASMC proliferation 24312381
PANC-1 Function Assay 20 μM 48 h inhibits the expression of Δ6D in response to the PPARδ agonist  24294133
A549 Function Assay 30 μM 0.5 h DMSO inhibits the thrombin-induced IL-8/CXCL8-Luc activity 24277696
SW480 Function Assay 10 μM 20 h DMSO suppresses the CRT activity 24324366
HEK 293 Function Assay 10 μM 5 h DMSO inhibits Wnt-induced β-catenin/TCF4 activity and nuclear β-catenin accumulation 24324366
HEK 293 Function Assay 10 μM 5 h DMSO suppresses the CRT activity 24324366
HL-60  Function Assay 10/20 μM 1 h inhibits the N. chinensisextract induced differentiation into granulocytes 24357020
HL-60 Function Assay 2 µM 16 h DMSO inhibits the association of pS621 Raf-1 and NFATc3, and the RA-induced phosphorylation of nuclear NFATc3 24330068
HeLa Function Assay 50 μM 0.5 h blocks TRX-1 nuclear migration and TXNIP down-regulation 24376827
HUVECs Function Assay 10 μM 1 h inhibits the HDL reduced COX-2 expression and PGI-2 release 24385109
MCF-7 Function Assay 10 μM 10/30 min reduces the UTP-dependent ERK phosphorylation 24390819
HGC-27 Apoptosis Assay 1 µM 1 h suppresses RAD001 plus MK-2206-induced cell viability loss 24416349
PC3  Apoptosis Assay 50 μM 0.5 h inhibits MHY-449-induced apoptosis  24424889
HPAEpiCs  Function Assay 30 μM 1 h inhibits TNF-α stimulated p42/p44 MAPK phosphorylation 24441870
BeWo Function Assay 10 μM 2 h inhibits ERK1/2 24433846
A498 Apoptosis Assay 50 μM 24 h potentiates the pro-apoptotic effects of NC 24508476
NHBE Function Assay 2/20 μM 2 h attenuates IL-33 stimulated CXCL8/IL-8 secretion 24479526
A375 Cell Invasion Assay 10–20 µM 24 h reduces melanoma cell invasion 24466036
HBMEC Function Assay 10 μM 1 h blocks VEGF-induced EphA2 expression 24458982
HCT-15 Function Assay 1 h attenuates PGE2-induced phosphorylation of Erk  25431425
HCT-15 Apoptosis Assay 1 h abolishes the protective effects of PGE2 against curcumin-induced apoptosis 25431425
786-O Apoptosis Assay 50 μM 24 h potentiates the pro-apoptotic effects of NC 24508476
HepG2  Growth Inhibition Assay 20 μM 24 h suppresses TGF-β1-induced cell proliferation and invasion 25560488
SW480 Function Assay 20 μM 1 h reduces the expression of ATF3 protein 25447816
MDA-MB-231 Function Assay 25 μM 2-3 h decreases p-ERK1/2 and S100A4 expression 25555875
HepG2  Function Assay 10 μM 5 h blocks phosphorylated MAPKs induced by exogenous TGF-β1 25560488
MCF-7  Function Assay 10 μM 1 h inhibits IL-18-enhanced cell migration 25727011
H1355 Function Assay 25 μM 1 h blunts the B[a]P-induced increase in phospho-Chk1 and phospho-ERK expression 25769181
PC12 Function assay Inhibition of nerve growth factor-mediated MAP kinase activity in human PC12 cells, IC50 = 2 μM. 18077363
HT-29 Antiproliferative assay 5 days Antiproliferative activity against human HT-29 cells after 5 days by WST1 assay, IC50 = 4 μM. 25078316
IEC6 Function assay 5 mins Inhibition of MEK1/2 in rat IEC6 cells assessed as reduction in ERK1/2 loop phosphorylation dosed 30 mins before to stimulation with 10% serum for 5 mins by immunoblotting method, IC50 = 4.2 μM. 25078316
NG 108-15 Function assay Concentration required to abolish MAPK activity in mouse neuroblastoma and rat glioma hybrid NG 108-15 cells, Activity = 10 μM. 15537354
PC12 Function assay 10 uM 5 hrs Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with JNK inhibitor SP600125 for 1 hr before compound addition by Western blot analysis 21345685
PC12 Function assay 10 uM 5 hrs Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with MEK2 inhibitor U0126 for 1 hr before compound addition by Western blot analysis 21345685
PC12 Function assay 10 uM 5 hrs Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with MEK1 inhibitor PD98059 for 1 hr before compound addition by Western blot analysis 21345685
HeLa Function assay 20 uM 3 hrs Inhibition of ERK1/2 phosphorylation in human HeLa cells at 20 uM after 3 hrs by Western blotting analysis 23570615
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MDA-MB-231 Function assay 50 uM Downregulation of MMP2 in human MDA-MB-231 cells at 50 uM by Western blot analysis 22926226
MDA-MB-231 Function assay 50 uM Downregulation of MMP9 in human MDA-MB-231 cells at 50 uM by Western blot analysis 22926226
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 267.28 화학식

C16H13NO3

보관 (수령일로부터)
CAS 번호 167869-21-8 SDF 다운로드 원액 보관

동의어 N/A Smiles COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2

용해도

In vitro
배치:

DMSO : 46 mg/mL (172.1 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

특징
Does not inhibit c-Raf phosphorylated MEK1.
Targets/IC50/Ki
AhR
(Cell-free assay)
1 μM
MEK1
(Cell-free assay)
2 μM
시험관 내(In vitro)

PD98059는 세린 잔기 218 및 222를 글루타메이트로 돌연변이시켜 생성된 기저 MEK1 또는 부분적으로 활성화된 MEK(MEK-2E)를 IC50 2 μM으로 억제합니다. 이 화합물은 MAPK 상동체 JNK 및 P38을 억제하지 않습니다. Raf 키나아제, cAMP 의존성 키나아제, 단백질 키나아제 C, v-Src, 표피 성장 인자(EGF) 수용체 키나아제, 인슐린 수용체 키나아제, PDGF 수용체 키나아제 및 포스파티딜이노시톨 3-키나아제를 포함한 여러 다른 키나아제 활성을 억제하지 않으므로 MEK에 대해 고도로 선택적입니다. 이 억제제는 PDGF 자극 MAPK 활성화 및 3T3 세포로의 티미딘 통합을 각각 약 10 μM 및 약 7 μM의 IC50로 억제합니다. Raf 또는 MEK 키나아제에 의한 MEK1 활성화를 4 μM의 IC50로 강력하게 억제하고, Raf에 의한 MEK2 활성화를 50 μM의 IC50로 약하게 억제합니다. 이 화학 물질은 KB 및 PC12 세포에서 스트레스 및 인터루킨-1 자극 키나아제 캐스케이드에 참여하는 MEK 상동체 MKK4 및 RK 키나아제의 활성화와 Swiss 3T3 세포에서 인슐린 또는 표피 성장 인자에 의한 p70 S6 키나아제의 활성화를 억제하지 않습니다. 세포 생존력을 변경하지 않고 신경 성장 인자(NGF) 유도 PC12 세포 분화를 완전히 차단합니다. 이 화합물은 RANKL을 포함하는 배양액에서 RAW264.7 세포의 증식을 용량 의존적으로 억제하여 TRAP 양성 세포의 명백한 감소를 초래합니다.

키나아제 분석
시험관 내 MEK 억제 활성
미엘린 기본 단백질(MBP)로의 32P 통합은 44-kDa MAPK(GST-MAPK) 또는 45-kDa MEK(GST-MEK1)를 함유하는 글루타티온 S-트랜스퍼라제(GST) 융합 단백질의 존재 하에 분석됩니다. 분석은 50 μL의 50 mM Tris, pH 7.4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP에 10 μg의 GST-MEK1, 0.5 μg의 GST-MAPK 및 40 μg의 MBP를 포함하여 수행됩니다. 30°C에서 15분 동안 인큐베이션한 후, Laemmli SDS 샘플 버퍼를 첨가하여 반응을 중단합니다. 인산화된 MBP는 SDS/10% PAGE로 분리됩니다.
생체 내(In vivo)

국소 뇌 허혈 30분 전 마우스에 PD98059를 처리하면 손상으로부터 보호하여 경색 부피가 감소합니다. 이 화합물로 30분 전 전처리한 후 3시간 동안 시간당 세룰레인 주사와 함께 처리하면 췌장 습중량 및 조직학을 기반으로 세룰레인 유발 급성 췌장염이 유의하게 개선됩니다. 카라기난 1시간 후 마우스에 이 화학 물질(10 mg/kg)을 투여하면 측정된 모든 염증 매개변수가 감소합니다.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/12237315/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10536014/
  • [6] https://pubmed.ncbi.nlm.nih.gov/12370536/
  • [7] https://pubmed.ncbi.nlm.nih.gov/20074457/
  • [8] https://pubmed.ncbi.nlm.nih.gov/11254111/
  • [9] https://pubmed.ncbi.nlm.nih.gov/17161815/
  • [10] https://pubmed.ncbi.nlm.nih.gov/14506750/
  • [11] https://pubmed.ncbi.nlm.nih.gov/14506750/
  • [12] https://pubmed.ncbi.nlm.nih.gov/9495809/

적용 분야

방법 바이오마커 이미지 PMID
Western blot c-Jun / α-tubulin / p-ERK / ERK / p-AKT / AKT p-JNK / JNK / Cyclin D1 p-HER2 / HER2 MMP9 / XIAP / VEGF
S1177-WB1
17482134

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자주 묻는 질문

질문 1:
How to formulate this inhibitor for i.p. injection?

답변:
You can prepare the stock of this compound by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.