ホームページ MAPK p38 MAPK inhibitor - Mitophagy activator Adezmapimod (SB203580) For research use only.

Adezmapimod (SB203580)

別名：RWJ 64809, PB 203580

Adezmapimod (SB203580, RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.

Adezmapimod (SB203580)化学構造

CAS No. 152121-47-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫なし(納期7~10日)
JPY 145500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Adezmapimod (SB203580)関連製品

シグナル伝達経路

p38 MAPK Signaling Pathways

p38 MAPKシグナル伝達経路

p38 MAPK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
RAW 264.7 Cytotoxic Assay 12.5 μM 12h Blocks lethal toxin-mediated cytotoxicity 17485504
PC12 Kinase Assay 10 μM 15 min Inhibits p38 MAP kinase with IC50 of 0.6 μM 7750577
HCA2 Function Assay 2.5 μM Inhibits p38 mediated MK2 activation 17964780
PC12 Function Assay 10 μM Activates Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction 21345685
hESCs Growth Inhibition Assay 5 μM Induces cardiomyogenic activity assessed as cell growth 23602399
RAW264.7 Function Assay 10 μM Induces antiinflammatory activity by inhibiting IL-1β release 23791078
RAW264.7 Function Assay 10 μM Induces antiinflammatory activity by inhibiting iNOS release 23791078
RAW264.7 Function Assay 10 μM Induces antiinflammatory activity by inhibiting NO release 23791078
RAW264.7 Function Assay 10 μM Inhibits LPS-induced p38 MAPK phosphorylation 24016057
IEC-18 Function Assay 10 μM Inhibits LPS-induced p38 MAPK phosphorylation 23758110
whole blood cell Function assay 0.01 to 100 uM Inhibition of p38-related IL1-beta release by whole blood cells at 10 e-4 to 10 e-8 M, IC50 = 0.35 μM. 12852754
whole blood cell Function assay 0.01 to 100 uM Inhibition of p38-related TNF-alpha release by whole blood cells at 10 e-4 to 10 e-8 M, IC50 = 0.94 μM. 12852754
WS Function assay 2.5 uM Inhibition of anisomycin-induced P38-alpha activation in human human TERT-immortalised WS cells assessed as HSP27 phosphorylation at 2.5 uM 17659871
SW1353 Function Assay 1 h Inhibits IL-6 production with IC50 of 0.05 μM 11140741
PBMC Function Assay 15 min Inhibits the release of interleukin-1-beta with IC50 of 0.037 μM 12361396
Sf9 Function assay 30 mins Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells assessed as reduction in autophosphorylation pre-incubated for 30 mins followed by incubation with ATP for 2 hrs by ADP-Glo assay, IC50 = 0.01 μM. 26455654
BMDC Antiinflammatory assay 1 hr Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-6 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA, IC50 = 3.5 μM. 24047259
BMDC Antiinflammatory assay 1 hr Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-12 p40 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA, IC50 = 5 μM. 24047259
BMDC Antiinflammatory assay 1 hr Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA, IC50 = 7.5 μM. 24047259
macrophage-like cell Antiinflammatory assay 30 mins Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA, IC50 = 8.6 μM. 23811089
U937 Function Assay Inhibits JAK-mediated interferon-gamma/anisomycin-induced Stat1 phosphorylation 18157122
Hela Function Assay Inhibits Tat-induced HIV1 LTR transactivation in human HeLa cells with IC50 of 0.1 μM 18926711
THP-1 Function Assay Inhibits LPS-induced TNFalpha production with IC50 of 0.16 μM 18325768
U937 Function Assay Inhibits JAK-mediated interferon-gamma/anisomycin-induced p38 phosphorylation 18157122
sf21 Function assay Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells SPR analysis, Kd = 0.0217 μM. 28834431
PBMC Function assay Inhibition of TNF-alpha production by lipopolysaccharide-stimulated human peripheral blood mononuclear cells, IC50 = 0.025 μM. 9873730
PBMC Function assay Inhibition of LPS-stimulated TH+NF-alphs production by human peripheral blood mononuclear cells (PBMCs), IC50 = 0.025 μM. 9784093
PBMC Function assay Inhibition of p38 MAP kinase related TNF-alpha release from peripheral blood mononuclear cells (PBMC), IC50 = 0.037 μM. 12061876
PBMC Function assay Inhibition of LPS-induced IL1-beta production in human peripheral blood mononuclear cells(PBMCs), IC50 = 0.048 μM. 9784093
SW1353 Function assay Compound was evaluated for its ability to inhibit IL-6 production in SW1353 cells treated with cytokines IL-1 and TNF, IC50 = 0.05 μM. 10999467
SW1353 Function assay Inhibition of TNF and IL-1 induced IL-6 production in human chondro-sarcoma SW 1353 cells, IC50 = 0.05 μM. 10999468
THP1 Function assay Inhibition of LPS-stimulated IL1 production in human THP1 cells, IC50 = 0.05 μM. 18077363
THP1 Function assay Inhibition of LPS-stimulated TNFalpha production in human THP1 cells, IC50 = 0.05 μM. 18077363
THP1 Function assay Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells, EC50 = 0.06 μM. 12086485
THP1 Function assay Inhibition of tumor necrosis factor alpha release by THP-1 cells, IC50 = 0.07 μM. 15658855
monocytic cell Function assay Inhibitory activity against TNF-alpha production using lipopolysaccharide stimulated human monocytic cells, IC50 = 0.072 μM. 12729637
THP1 Function assay Inhibitory activity against LPS-stimulated TNF-alpha production in human monocytic cells (THP-1), IC50 = 0.072 μM. 15139749
THP-1 Function assay Inhibitory activity against lipopolysaccharide stimulated TNF-alpha production in THP-1 cells (human monocytic cells), IC50 = 0.072 μM. 15837310
THP1 Function assay Inhibition of LPS-stimulated TNFalpha production in THP1 cells, IC50 = 0.072 μM. 16750367
PBMC Function assay Inhibition of staphylococcal enterotoxin B(SEB) stimulated tumor necrosis factor alpha (TNF-alpha) production by human peripheral blood mononuclear cells(PBMCs), IC50 = 0.16 μM. 9784093
PBMC Function assay Concentration required to inhibit lipopolysaccharide induced TNF-alpha release was determined in human peripheral blood mononuclear cells, IC50 = 0.19 μM. 15454231
Sf9 Function assay Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells by fluorescent polarization assay, IC50 = 0.2 μM. 26455654
HEK293F Function assay Inhibition of sodium arsenate activated N-terminal GST-tagged Brugia malayi MPK1 expressed in HEK293F cells using FAM-p38tide as substrate by IMAP assay, IC50 = 0.22 μM. 29541362
HEK-293 Function assay Inhibition of RIP2K in MDP-stimulated HEK-293 cells over-expressing NOD2 assessed as IL8 secretion, IC50 = 0.25 μM. 27109867
PBMC Function assay Inhibition of p38 MAP kinase related TNF-alpha release from peripheral blood mononuclear cells (PBMC), IC50 = 0.59 μM. 12061876
PBMC Function assay Inhibition of the release of tumor necrosis factor alpha from peripheral blood mononuclear cells, IC50 = 0.59 μM. 12361396
PBMC Function assay Inhibitory activity against TNF-alpha release in PBM cells, IC50 = 0.59 μM. 12852754
HEK-293 Function assay Inhibition of RIP2K in Pam2CSK4-stimulated HEK-293 cells over-expressing TLR2 assessed as IL8 secretion, IC50 = 6.31 μM. 27109867
WS Function assay Inhibition of MK2 mediated HSP27 phosphorylation in immortalised WS cells assessed as reduction in F-actin stress fibres 17964780
WS Function assay Inhibition of p38 mediated MK2 activation in WS cells 17964780
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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
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生物活性

製品説明 Adezmapimod (SB203580, RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.
特性 First reported p38 inhibitor.
Targets
p38 MAPK [1]
(THP-1 cells)		 PKB [1]
(THP-1 cells)
0.3 μM-0.5 μM 3 μM-5 μM
In Vitro
In vitro

SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. [1] SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. [2] SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells. [3]
Kinase Assay Cellular receptor kinase phosphorylation assay
4 μg of sheep anti-PKBα is immobilized on 25 μL of protein G-Sepharose overnight (or 1.5 hours) and washed in Buffer A (50 mm Tris, pH 7.5, 1 mm EDTA, 1 mm EGTA, 0.5 mm Na3VO4, 0.1% β-mercaptoethanol, 1% Triton X-100, 50 mm sodium fluoride, 5 mm sodium pyrophosphate, 0.1 mm phenylmethylsulfonyl fluoride, 1 μg/mL pepstatin, leupeptin, and 1 μm microcystin). The immobilized anti-PKB is then incubated with 0.5 ml of lysate (from 5 × 106 cells) for 1.5 hours and washed three times in 0.5 mL of Buffer A supplemented with 0.5 m NaCl, two times in 0.5 mL of Buffer B (50 mm Tris-HCl, pH 7.5, 0.03% (w/v) Brij-35, 0.1 mm EGTA, and 0.1% β-mercaptoethanol), and twice with 100 μl of assay dilution buffer; 5× assay dilution buffer is 100 mm MOPS, pH 7.2, 125 mm β-glycerophosphate, 25 mm EGTA, 5 mm sodium orthovanadate, 5 mm DTT. To the PKB enzyme immune complex is added 10 μL of assay dilution buffer, 40 μm protein kinase A inhibitor peptide, 100 μm PKB-specific substrate peptide, and 10 μCi of [γ-32P]ATP, all made up in assay dilution buffer. The reaction is incubated for 20 minutes at room temperature with shaking, then samples are pulse spun, and 40 μL of reaction volume are removed into another tube to which is added 20 μL of 40% trichloroacetic acid to stop the reaction. This is mixed and incubated for 5 minutes at room temperature, and 40 μL is transferred onto P81 phosphocellulose paper and allowed to bind for 30 seconds. The P81 piece is washed three times in 0.75% phosphoric acid then in acetone at room temperature. γ-32P incorporation is then measured by scintillation counting.
細胞実験 細胞株 CT6 cell , BA/F3 F7 cell
濃度 0–30 μM
反応時間 1 hour
実験の流れ

CT6 cell and BA/F3 F7 cell are rested by washing three times in RPMI and culturing overnight in RPMI, 5% fetal calf serum in the absence of growth factor, antibiotics, or β-mercaptoethanol supplements. 2–5 × 106 rested CT6 cells are resuspended in 2 mL of RPMI, 5% fetal calf serum and preincubated with SB203580 or vehicle control as indicated in figure legends. Cells are then stimulated with 20 ng/ml recombinant human IL-2 for 5 minutes at 37  °C and pelleted in a minifuge for 30 seconds, medium is aspirated, and the pellet is lysed in the appropriate buffer. BA/F3 cells stably expressing deletion mutants of IL-2 receptor β chain are maintained in glutamine containing RPMI further supplemented with 5% fetal calf serum and 0.2 μg/mL G418. The cells are then washed extensively, rested overnight, and washed again before activating with IL-2; such cell preparations are >90% T cells. Cellular proliferation assays are performed by measurement of [3H]thymidine incorporation.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot phospho-p38 / p38 p-ASK1 / ASK1 / P-JNK / p-MKK4 / p-ERK phospho-MK2(T334) / phospho-HSP27(S82) / phospho-Akt(T308) / phospho-Akt(S473) 25747578
Immunofluorescence dsRNA / hnRNP A1 25747578
Growth inhibition assay Cell viability 23001390
In Vivo
In Vivo

SB203580 protects pig myocardium against ischemic injury in an in vivo model. [4]SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE). [5]
動物実験 動物モデル Systemic lupus erythematosus (SLE) are established in female MRL/lpr mice and female C57BL/6 mice
投与量 0.1 M/day
投与経路 Orally administered

化学情報

分子量 377.43 化学式

C21H16FN3OS
CAS No. 152121-47-6 SDF Download Adezmapimod (SB203580) SDFをダウンロードする
Smiles CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F
保管 3 years-20°C （in the dark）powder

In vitro
Batch:

DMSO : 38 mg/mL ( (100.68 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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