SP600125

別名：Nsc75890

製品コード：S1460 純度：99.94%

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 A，FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.

CAS No. 129-56-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫なし(納期7~10日)
10mg	JPY 22000	国内在庫あり
50mg	JPY 37000	国内在庫あり
100mg	JPY 55500	国内在庫あり
1g	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] よく尋ねられる質問

文献中Selleckの製品使用例（1012）

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

関連ターゲット	JNK1 JNK2 JNK3	もっと見る
関連製品	JNK-IN-8 Anisomycin JNK Inhibitor IX Tanzisertib(CC-930) JNK Inhibitor VIII Bentamapimod (AS602801) BI-78D3 SP 600125, negative control DTP3 CC-401 Hydrochloride Polyphyllin I	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library MAPK Inhibitor Library Cell Cycle compound library TGF-beta/Smad compound library Anti-alzheimer Disease Compound Library	もっと見る

シグナル伝達経路

JNK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

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)	もっとクリックする
	40 nM	40 nM	60 nM	70 nM	もっとクリックする

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
Kinase Assay	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 K_m values for ATP and the specific substrate are initially determined and each assay is then run at optimized [ATP] (2·αK_m) and [substrate] (5·K_m) 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

参考
[1] Bennett BL, et al. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686. [2] Joiakim A, et al. Drug Metab Dispos, 2003, 31(11), 1279-1282. [3] Schmidt M, et al. EMBO Rep, 2005, 6(9), 866-872. [4] Colombo R, et al. Cancer Res, 2010, 70(24), 10255-64. [5] Vaishnav D, et al. Biochem Biophys Res Commun, 2003, 307(4), 855-860. [6] Kim JA, et al. Oncogene, 2010, 29(11), 1702-1716. + 展開

参考

+ 展開

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

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
	Clear solution	5% DMSO 1 95% Corn oil	0.3mg/ml (1.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.0mg/ml (9.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	10%DMSO 1 90%Corn oil	6.0mg/ml (27.24mM)	Taking the 1 mL working solution as an example, add 100 μL of 60 mg/ml clear DMSO stock solution to 900 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.2mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 44 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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。

技術サポート

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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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):