연구용
제품 번호S1177
| 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 | ||||||
| 분자량 | 267.28 | 화학식 | C16H13NO3 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 167869-21-8 | SDF 다운로드 | 원액 보관 |
|
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| 동의어 | N/A | Smiles | COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2 | ||
|
In vitro |
DMSO
: 46 mg/mL
(172.1 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
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.
| 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.
|
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| 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 |
|
| 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 |
|
17482134 |
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.