Home MAPK p38 MAPK 억제제 SB202190

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SB202190 p38 MAPK 억제제

제품 번호S1077

SB202190은 세포 유리 분석에서 IC50이 50 nM/100 nM인 p38α/β를 표적으로 하는 강력한 p38 MAPK 억제제로, 때때로 생체 내 SAPK2a/p38의 잠재적 역할을 조사하기 위해 SB 203580 대신 사용됩니다. 이 화합물은 autophagy 및 헴 옥시게나제-1 유도를 통해 내피세포 apoptosis를 억제합니다. 에라스틴 의존성 ferroptosis를 유의하게 억제합니다.
SB202190 p38 MAPK 억제제 Chemical Structure

화학 구조

분자량: 331.34

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품질 관리

배치: 순도: 99.99%
99.99

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
HCT-116 Function Assay 25 μM 30 min DMSO  attenuates the mRNA and protein expression of hBD-2 in responsive to DA 26223251
MDA-MB-231 Function Assay 2 μM 24 h lessenes CCL2 induction by TNFα 26100848
rBMSCs Function Assay 10 μM 2.5 h depresses the phosphorylation of ERK and p38 26053266
MG63 Function Assay 10/20/30 μM 24 h significantly decreases the level of phosphorylated p38 induced by CdCl2 in a concentration -dependent manner 25998312
MG63 Apoptosis Assay 10/20/30 μM 24 h significantly decreased the apoptosis rate of MG63 induced by CdCl2 25998312
HTSMCs Function Assay 0.1/1/10 μM 1 h inhibited CORM-2-induced HO-1 protein levels and mRNA expression 25921464
MIA PaCa-2 Function Assay 20 μM 24 h reduced lactate accumulation in combination with both 2-DG and D-allose  25888489
MIA PaCa-2 Function Assay 20 μM 24 h results in a modest inhibition of HIF-1α protein accumulation 25888489
BxPC-3 Function Assay 20 μM 24 h results in a modest inhibition of HIF-1α protein accumulation 25888489
AsPC-1 Function Assay 20 μM 24 h results in a modest inhibition of HIF-1α protein accumulation 25888489
MIA PaCa-2 Function Assay 20 μM 24 h enhances cleavage of PARP when combined with glucose analogs 25888489
MIA PaCa-2 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
BxPC-3 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
AsPC-1 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
HEY Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
OVCAR-3 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
SK-OV-3 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
MH7A  Growth Inhibition Assay 24 h reinforces the inhibitory effects of XAN 25862966
MH7A  Apoptosis Assay 25 μM 24 h reverses cell cycle arrest induced by XAN and caused apoptosis of cells via activation of JNK 25862966
SCC25 Function Assay 20 μM 24 h increases autophagy level 25834400
HaCaT  Function Assay 5 µM 24 h inhibits IFN-γ-induced CCL22 production levels 25834353
HaCaT  Function Assay 5 µM 24 h inhibits IFN-α-induced CCL22 production levels 25834353
HPAEpiCs  Function Assay 1/3/10 μM 1 h reduces S1P-induced ICAM-1 protein and mRNA expression and promoter activity 25734900
HPAEpiCs Function Assay 1/3/10 μM 1 h inhibits S1P-stimulated Akt phosphorylation   25734900
HPAEpiCs Function Assay 1/3/10 μM 1 h inhibits S1P time-dependently stimulated c-Jun phosphorylation 25734900
K562 Function Assay 10 μM 1 h DMSO inhibits quinacrine-induced p38 MAPK phosphorylation 25684043
PANC-1 Function Assay 10 μM 1 h enhances the autophagic effect  25632222
BxPC-3 Function Assay 10 μM 1 h enhances the autophagic effect  25632222
K562  Function Assay 0.25-1 μM 24 h suppresses resveratrol-induced H2AX phosphorylation 25619392
THP-1 Function Assay 5 µM 2 h significantly attenuates secretion of IL-1α induced by 27OHChol plus FSL-1  25598661
WB Function Assay 20 μM  30 min decreases the LPS- or LTA-induced IL-6 and TNF-α production 25530682
RAW 264.7 Function Assay 10 μM 30 min induces characteristic vacuolation of OCs  25461399
RAW 264.7 Function Assay 10 μM 30 min attenuates the effects of OPG on osteoclast retraction 25461399
HaCaT  Function Assay 40 μM 3-24 h DMSO reduces the accumulation of ZO-1 25435485
H9c2 Function Assay 50 μM  12 h reduces LDH release and MMP loss 25245818
HSCs Apoptosis Assay 25 μM 24 h significantly attenuates TG-induced activated HSCs apoptosis 24961950
THP-1 Growth Inhibition Assay 72 h DMSO IC50=4.7μM 24815087
MDDCs Growth Inhibition Assay 72 h DMSO IC502.7μM 24815087
MDDCs Function Assay 0-15 μM 48 h DMSO suppresses IFN-α and IP-10 production  24815087
MDDCs Function Assay 0-15 μM 48 h DMSO inhibits MIP-1a, MIP-1b and RANTES production 24815087
MDDCs Function Assay 10 μM 3.5 h DMSO blocks EBOV GP, but not VSV G mediated entry into human MDDCs 24815087
macrophages Function Assay 1 μM 4.5 h completely inhibits MT-III-induced activation of NF-κB 24808633
PDL  Function Assay 20 μM  30 min DMSO significantly inhibits the tensile force-mediated BMP-2 expression 24561081
AGS Function Assay 5 μM 30 min suppresses 1-induced caspase-8 and caspase-3 activation 24547878
H520 Function Assay 10 µM 1 h DMSO decreases the pemetrexed-induced MSH2 mRNA and protein levels 24530475
H1703 Function Assay 10 µM 1 h DMSO decreases the pemetrexed-induced MSH2 mRNA and protein levels 24530475
H520 Function Assay 10 µM 12 h DMSO inhibits pemetrexed-elicited MSH2 protein stability 24530475
H1703 Function Assay 10 µM 12 h DMSO inhibits pemetrexed-elicited MSH2 protein stability 24530475
H520 Function Assay 10 µM 6 h DMSO significantly increases the levels of ubiquitin-conjugated MSH2 in pemetrexed-treated cell line 24530475
H1703 Function Assay 10 µM 6 h DMSO significantly increases the levels of ubiquitin-conjugated MSH2 in pemetrexed-treated cell line 24530475
MC3T3-E1 Function Assay 0.3/3/30 μM 1 h attenuates TNF-α-induced MMP-9 expression in a concentration-dependent manner  24502696
MC3T3-E1 Function Assay 30 μM 1 h attenuates TNF-α-stimulated p38 MAPK phosphorylation 24502696
HUVECs  Function Assay 10 µM 1 h inhibits TNF-α-induced CXCL1 production 24487964
AGS  Function Assay 10 µM 30 min inhibits IL-1β-induced activation of p38 24479681
MKN-45 Function Assay 10 µM 30 min inhibits IL-1β-induced activation of p38 24479681
AGS  Function Assay 10 µM 30 min attenuates IL-1β-induced GA cell migration and invasion 24479681
MKN-45 Function Assay 10 µM 30 min attenuates IL-1β-induced GA cell migration and invasion 24479681
AGS  Function Assay 10 µM 30 min significantly decreases Il-1β-induced MMP2 and MMP9 mRNA expression 24479681
MKN-45 Function Assay 10 µM 30 min significantly decreases Il-1β-induced MMP2 and MMP9 mRNA expression 24479681
DCs Function Assay 20 μM 1 h decreases IL-12 production 24434636
HUVEC  Function Assay 20 μm  5 h DMSO reduces cytokine expression levels in a concentration-dependent manner 24189062
A 549 Function Assay 50 μM 1 h decreases the level of IL-8  24179688
H520  Function Assay 5/10 μM 1 h DMSO decreases MSH2 protein as well as mRNA levels in gefitinib-exposed cell 24138903
H1703  Function Assay 5/10 μM 1 h DMSO decreases MSH2 protein as well as mRNA levels in gefitinib-exposed cell 24138903
H520  Function Assay 10 µM 12 h DMSO decreases MSH2 mRNA and protein stability in gefitinib-treated NSCLC cells 24138903
H1703  Function Assay 10 µM 12 h DMSO decreases MSH2 mRNA and protein stability in gefitinib-treated NSCLC cells 24138903
MCF-7  Growth Inhibition Assay 10 μM 24 h inhibits the CR108-induced cell death 24128853
HPAEpiCs Function Assay 0.1/1/10 μM 1 h inhibits TNF-α-induced cPLA2 protein and mRNA expression 24069158
podocytes Function Assay 10 μM 1 h inhibits TGFβ1-induced activation of p38MAPK and Erk1/2  24036212
MCF-7 Function Assay 10 μM 1 h DMSO reduces the WA-induced phosphorylated p38 MAPK 24019090
MCF-7 Function Assay 10 μM 24 h DMSO increases the WA-induced apoptosis 24019090
HAPI Function Assay 10/20/40 μM 1 h inhibits TCDD-induced p38/JNK MAPK phosphorylation 23969120
HAPI Function Assay 20 μM  1 h DMSO attenuates TCDD-induced activation of iNOS and production 23969120
HepG2 Function Assay 350 nM 24 h inhibits the deguelin-induced activation of p38MAPK 23933198
AGS  Function Assay 10 μM 30 min inhibits caspase-3 activation and inhibition of ERK 23850994
HepG2 Growth Inhibition Assay 0-50 μM 48 h inhibits the proliferation in a dose dependent manner 23807508
BEL7404 Growth Inhibition Assay 0-50 μM 48 h inhibits the proliferation in a dose dependent manner 23807508
HL7702 Growth Inhibition Assay 0-50 μM 48 h inhibits the proliferation in a dose dependent manner 23807508
HepG2 Function Assay 0-50 μM 24 h inhibits the phosphorylation of p38 downstream proteins MAPKAPK2, ATF2, MSK1 and HSP27 in a dose-dependent manner 23807508
BEAS-2B Growth Inhibition Assay 10 μM 30 min reverses the decrease of cell viability induced by HCI 23784034
BEAS-2B Cytotoxity Assay 10 μM 30 min inhibited the increase in LDH and IL-8 expression 23784034
BEAS-2B Function Assay 10 μM 30 min decreases the levels of caspase-3, Bad and fas 23784034
H9c2  Function Assay 0.01/0.1/1 μM 1 h attenuates TNF-α-induced MMP-9 expression, mRNA levels, and promoter activity 23774252
H9c2  Function Assay 1 μM 1 h reduces TNF-α directly stimulated p38 MAPK phosphorylation 23774252
U937 Function Assay 10 μM  1 h abrogates the caffeine effect on MKP-1 and PP2Acα mRNA transcriptional levels 23707387
U937 Function Assay 10 μM  1 h abrogates caffeine-induced MKP-1 down-regulation and PP2Acα up-regulation 23707387
U937 Function Assay 10 μM  1 h suppresses c-Jun and CREB phosphorylation in caffeine-treated cells  23707387
A549 Function Assay 0.3/3/30 μM 1 h significantly attenuates ATPγS-mediated COX-2 protein and mRNA expression and promoter activity  23680674
A549 Function Assay 10 μM  0-30 min inhibits ATPγS induced p42/p44 MAPK and p38 MAPK phosphorylation 23680674
A549 Function Assay 10 μM  1 h inhibits ATPγS induced NF-κB p65 subunit phosphorylation and NF-κB promoter activity 23680674
A549 Function Assay 10 μM  1 h reduces ATPγS-stimulated cPLA2 phosphorylation  23680674
A549 Function Assay 10 μM  1 h reduces ATPγS-enhanced enzymatic activity of cPLA2  23680674
PC12 Function Assay 10/20/40 μM 1 h inhibits JNK and p38 23584357
HK-2 Apoptosis Assay 20 μM 24 h inhibits ERK and p38MAPK 23543151
H9c2 Function Assay 1 μM 1 h reduces TNF-α-induced MMP-9 mRNA levels and promoter activity 23353699
H9c2 Function Assay 1 μM 1 h reduces TNF-α-enhanced AP-1 promoter activity 23353699
H1650  Function Assay 10 μM  1 h DMSO decreases both protein and mRNA levels of ERCC1 in paclitaxel-exposed cells 23228696
H1703 Function Assay 10 μM  1 h DMSO decreases both protein and mRNA levels of ERCC1 in paclitaxel-exposed cells 23228696
H1650  Growth Inhibition Assay 10 μM  1 h DMSO enhances paclitaxel-induced cytotoxicity 23228696
H1703 Growth Inhibition Assay 10 μM  1 h DMSO enhances paclitaxel-induced cytotoxicity 23228696
medulloblastoma cells Antiproliferative assay Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay, EC50 = 3.006 μM. 17417631
neural precursor cells Antiproliferative assay Antiproliferative activity against mouse neural precursor cells by MTT assay, EC50 = 8.063 μM. 17417631
RAW264.7 Antiinflammatory assay 10 mins Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 10 mins prior to LPS-challenge measured after 18 hrs by Griess method, IC50 = 16 μM. 22831798
BL21(DE3) Function assay 60 mins Inhibition of recombinant human N-terminal His6-tagged BRD4 expressed in Escherichia coli BL21(DE3) cells using biotinylated histone H4 peptide as substrate after 60 mins by AlphaScreen assay, IC50 = 3.4 μM. 28195723
RAW264.7 Function assay Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein mediated cytotoxicity in mouse RAW264.7 cells assessed as cell viability 17485504
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 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
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 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
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) 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
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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
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
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 331.34 화학식

C20H14N3OF

 보관 (수령일로부터)
CAS 번호 152121-30-7 SDF 다운로드 원액 보관

동의어 FHPI Smiles C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)O

용해도

In vitro
배치:

DMSO : 66 mg/mL (199.19 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 22 mg/mL

Water : 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

Targets/IC50/Ki
Ferroptosis
p38α
(Cell-free assay)
50 nM
p38β
(Cell-free assay)
100 nM
시험관 내(In vitro)

SB 202190은 기저 및 항-Fas 항체 유도 MAPKAPK 2 활성을 용량 의존적으로 유의하게 억제합니다. 이 화합물 자체만으로 CPP32 유사 카스파제 활성화를 통해 Jurkat 및 HeLa 세포에서 세포 사멸을 유도하기에 충분하며, 이는 bcl-2 발현에 의해 차단될 수 있습니다. 이의 apoptosis는 p38β에 의해 약화되지만 p38α에 의해 증강됩니다. 이 화학 물질은 HaCaT 세포에서 UVB 유도 COX-2 단백질 발현을 강력히 억제하고, UVB 유도 cox-2 mRNA를 현저히 억제합니다. 이 억제제 처리로 신장 세뇨관 세포(정상 쥐 신장-52E)에서 알부민 유도 전염증성(monocyte chemoattractant protein-1) 및 형질전환 성장 인자(TGF)-beta1 유도 섬유화 촉진(procollagen-Ialpha1) 유전자 발현이 50% 이상 억제됩니다. A549 세포에서 용량 및 시간 의존적으로 JNK 인산화를 유도하고, ATF-2 전사 인자의 인산화를 유도하며, AP-1 DNA 결합을 증가시킵니다. 이 물질은 THP-1 및 MV4-11 세포의 성장을 촉진합니다. c-Raf 및 ERK의 인산화를 증가시키며, 이는 Ras-Raf-MEK-mitogen-activated protein kinase (MAPK) 경로 활성화가 이 화합물에 의해 유도되는 백혈병 세포 성장에 관여함을 시사합니다.

키나아제 분석
시험관 내 키나아제 분석
p38α 및 p38β는 0.1 mM EGTA를 포함하는 25 mM Tris-HCl, pH 7.5에서 기질로 미엘린 기본 단백질(0.33 mg/mL)을 사용하여 분석됩니다. 분석은 [γ-33P]ATP를 사용하여 50 μL 배양액에서 30 °C에서 10분 동안 수동으로 수행하거나, Biomek 2000 실험실 자동화 워크스테이션을 사용하여 96웰 형식으로 25 μL 배양액에서 상온에서 40분 동안 수행됩니다. ATP 및 마그네슘 아세테이트 농도는 각각 0.1 mM 및 10 mM입니다. 모든 분석은 MgATP로 시작됩니다. 수동 분석은 인산셀룰로스 종이에 배양액을 스팟팅한 다음 50 mM 인산에 담가 종료됩니다. 로봇 분석은 P30 필터 매트에 알리코트를 스팟팅하기 전에 5 μL의 0.5 M 인산을 추가하여 종료됩니다. 모든 종이는 ATP를 제거하기 위해 50 mM 인산에서 4번 세척하고, 아세톤(수동 배양) 또는 메탄올(로봇 배양)에서 한 번 세척한 다음 건조시키고 방사능을 측정합니다.
생체 내(In vivo)

SB202190 투여를 통한 p38 억제는 수동 전달 마우스 모델에서 PV IgG 유도 수포 형성을 억제합니다. 패혈증의 내독소 모델에서, 이 화합물로 치료하면 대조군에 비해 통계적으로 유의미한 생존 이점을 제공합니다.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/16807361/
  • [5] https://pubmed.ncbi.nlm.nih.gov/16908851/
  • [6] https://pubmed.ncbi.nlm.nih.gov/18222647/
  • [7] https://pubmed.ncbi.nlm.nih.gov/18995898/
  • [8] https://pubmed.ncbi.nlm.nih.gov/19027920/
  • [9] https://pubmed.ncbi.nlm.nih.gov/21159664/
  • [10] https://pubmed.ncbi.nlm.nih.gov/22053010/
  • [11] https://pubmed.ncbi.nlm.nih.gov/22053010/

적용 분야

방법 바이오마커 이미지 PMID
Western blot pJNK1 / pJNK2 / JNK1 / JNK2 mTOR / p-S6K / S6K / p-S6 / p-AKT / p-MK2
S1077-WB2
18222647
Immunofluorescence p-p38 / MMP9
S1077-IF1
24479681
Growth inhibition assay Cell viability
S1077-viability1
26844273

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