SP600125

別名:Nsc75890

SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.

SP600125化学構造

CAS No. 129-56-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 16300 国内在庫あり
JPY 12000 国内在庫あり
JPY 23100 国内在庫あり
JPY 33300 国内在庫あり
JPY 144600 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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製品安全説明書

現在のバッチを見る: 純度: 99.94%
99.94

SP600125と併用されることが多い化合物

Adezmapimod (SB203580)


SP600125 inhibits autophagy and activates apoptosis whereas, Adezmapimod induces mitophagy and autophagy.

PD98059


SP600125 and PD98059 are two kinases that possess pro-survival activities in TQ-induced cell death.

El-Najjar N, et al. Apoptosis. 2010 Feb;15(2):183-95.

SCH772984


SP600125 and SCH772984 significantly increase apoptosis of both PMN-MDSCs and M-MDSCs in vitro.

Yu J, et al. Front Oncol. 2021 Mar 18;11:647312.

LY294002


SP600125 and LY294002 suppress cell growth of SNU-216 and NCI-N87 cells.

Choi Y, et al. World J Gastroenterol. 2016 Nov 7; 22(41): 9141–9153.

Bentamapimod (AS602801)


SP600125 and Bentamapimod are pan-JNK inhibitors that cause a robust reduction in cell viability in a panel of GBM stem cells (GSCs) cultures.

MacLeod G, et al. Cell Rep. 2019 Apr 16;27(3):971-986.e9.

SP600125関連製品

シグナル伝達経路

JNK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
PC12 Function Assay 10 μM 5 h Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with SB203580 21345685
PC12 Function Assay 10 μM 5 h Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with SP600125 21345685
PC12 Function Assay 10 μM 5 h Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with U0126 21345685
PC12 Function Assay 10 μM 5 h Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with PD98059 21345685
A549 Function Assay 20 μM 1 h Inhibition of TPA-induced MMP-2 and u-PA expression 20492175
HaCaT Function Assay 20 μM 24 h Blocks the phosphorylation of c-Jun protein 19812349
HaCaT Function Assay 20 μM 4 h Blocks the TNF-α-induced CYP4F11 transcription 19812349
PC3 Function Assay 20 μM 1 h Decreases the MMP2 and MMP9 expression 19633975
RAW264.7 Function Assay 10 μM 12 h Antiinflammatory activity assessed as inhibition of LPS-induced NO production with IC50 of 17μM 19497418
BV-2 Function Assay 2 μM 1 h Inhibits the increase of sBAFF release in Gmix-treated BV-2 cells 19406831
Hep3B Function Assay 10 μM 1 h Blocks autophagy and upregulation of Beclin 1 expression induced by ceramide 19060920
LoVo Function Assay 1 μM 1 h Inhibition of PGE2-induced expression of uPA and MMP-9 significantly 21859479
LoVo Function Assay 1 μM 1 h BlocksPGE2-induced cell migration significantly 21859479
THP-1 Function Assay 90 nM 30 min Inhibition of tissue factor expression 22940059
PC3 Function Assay 25 μM 24 h Inhibition of AP-1 and p21 luciferase activity induced by S179D PRL 23162652
SH-SY5Y Function Assay 10 μM 1 h Neuroprotective activity assessed as reduction of anisomycin-induced cell death 23498914
SH-SY5Y Kinase Assay 10 μM 1 h Inhibition of JNK3 assessed as blockade of anisomycin-induced c-jun phosphorylation at ser73 23498914
RAW264.7 Function Assay 10 μM 24 h Antiinflammatory activity assessed as inhibition of IL-1beta release 23791078
RAW264.7 Function Assay 10 μM 24 h Antiinflammatory activity assessed as inhibition of LPS-induced iNOS expression 23791078
RAW264.7 Function Assay 10 μM 2 h Antiinflammatory activity assessed as inhibition of LPS-induced NO production 23791078
A549 Growth Inhibition Assay 20 μM 72 h Rapid and potent inhibition of cell proliferation 23912840
BMMC Function assay 1 to 20 uM 7 days Inhibition of RANKL/M-CSF-stimulated osteoclastogenesis in ICR mouse BMMC assessed as reduction in TRAP positive multinucleated cells at 1 to 20 uM incubated for 7 days by light microscopy 25397676
Plasmodium falciparum GB4 Antibacterial Assay 72 h Antiplasmodial activity with IC50 of 12.5893μM 19734910
Plasmodium falciparum 3D7 Antibacterial Assay 72 h Antiplasmodial activity with IC50 of 12.5893 μM 19734910
Plasmodium falciparum 7G8 Antibacterial Assay 72 h Antiplasmodial activity with IC50 of 10 μM 19734910
Plasmodium falciparum W2 Antibacterial Assay 72 h Antiplasmodial activity with IC50 of 7.94328 μM 19734910
Plasmodium falciparum HB3 Antibacterial Assay 72 h Antiplasmodial activity with IC50 of 7.94328 μM 19734910
B16-F10 Function Assay 1 h Inhibition of TNF-alpha-induced c-JUN phosphorylation 21815634
RAW264.7 Antiinflammatory assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production relative to control, IC50 = 17 μM. 22831798
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
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
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
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生物活性

製品説明 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Targets
serine/threonine kinase [1] JNK1 [1]
(Cell-free assay)
JNK2 [1]
(Cell-free assay)
Aurora A [4]
(Cell-free assay)
TrkA [4]
(Cell-free assay)
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40 nM 40 nM 60 nM 70 nM
In Vitro
In vitro

SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. In Jurkat T cells, SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM. In CD4+ cells, such as Th0 cells isolated from either human cord or peripheral blood, SP600125 blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-γ, and TNF-α, with IC50 of 5 μM to 12 μM. [1] However, later studies reveal that SP600125 also suppresses aryl hydrocarbon receptor (AhR) [2], Mps1 [3], and a panel of other serine/threonine kinases, including Aurora kinase A, FLT3, MELK, and TRKA [4]. In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation. [5] In HCT116 cells, SP600125 (20 μM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of SP600125 is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1. [6]

Kinase Assay In Vitro Kinase Assays
The potency of SP600125 towards kinases, including MPS1, JNK, and Aurora kinase A, is determined based on the specific measurement of radioactive phosphotransfer to the substrate. For each enzyme, the absolute Km values for ATP and the specific substrate are initially determined and each assay is then run at optimized [ATP] (2·αKm) and [substrate] (5·Km) concentrations. MPS1 activity is measured using 5 nM of MPS1 recombinant protein in 50 mM HEPES pH 7.5, 2.5 mM MgCl2, 1 mM MnCl2, 1 mM DTT, 3 μM NaVO3, 2 mM β-glycerophosphate, 0.2 mg/mL BSA, 200 μM P38-βtide substrate-peptide (KRQADEEMTGYVATRWYRAE), and 8 μM ATP with 1.5 nM 33P-γ-ATP. Ten serial 1:3 dilutions (from 30 μM to 1.5 nM) of SP600125 are tested and IC50 determined.
細胞実験 細胞株 HCT116, A2780, and U2OS cells
濃度 0–5 μM
反応時間 72 hours
実験の流れ

Cells are seeded in 384 well-plates. One day after seeding, the cells are treated with SP600125 for 72 hours and the plates are then processed using a CellTiter-Glo assay. Inhibitory activity is evaluated comparing treated versus control data and IC50 value of proliferation is calculated.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-JNK p-IGF1R / IGF1R / p-Akt / Akt / p-ERK / ERK p-Src / Src p-c-Jun / c-Jun / pJNK / JNK Survivin / Bcl-2 / PARP p-FADD / FADD / p-c-Jun / c-Jun 25226534
Immunofluorescence AIF / Endo G E-cadherin / β-catenin α-catenin / Actin 21738692
Growth inhibition assay Cell viability (U-87 MG) Cell viability (A549) 27176481
In Vivo
In Vivo

In mice, SP600125 (15 mg/kg or 30 mg/kg) significantly inhibits lipopolysaccharide (LPS)-induced TNF-α expression and anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes. [1]

動物実験 動物モデル Mouse LPS/TNF model (female CD-1)
投与量 15 or 30 mg/kg
投与経路 Administered via intravenous injection or orally

化学情報

分子量 220.23 化学式

C14H8N2O

CAS No. 129-56-6 SDF Download SP600125 SDFをダウンロードする
Smiles C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O
保管

In vitro
Batch:

DMSO : 44 mg/mL ( (199.79 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

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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Handling Instructions

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よくある質問(FAQ)

質問1:
how to reconstitute the inhibitor for in vivo studies?

回答
S1460 can be dissolved in 5% DMSO/corn oil at 5 mg/ml as a clear solution for injection. The inhibitor dissolved in vehicle 30% PEG400/0.5% Tween80/5%Propylene glycol, at 30mg/ml is a suspension and can be used for oral administration.

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