SP600125 | NSC 75890;Pyrazolanthrone;1PMV | 蒽[1,9-cd]吡唑-6(2H)-酮 | JNK

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1,9-吡唑并蒽酮 /SP600125 98%

货号：A155219 同义名： 蒽[1,9-cd]吡唑-6(2H)-酮 / NSC 75890;Pyrazolanthrone

SP600125 是一种选择性的 JNK 抑制剂，对 JNK1、JNK2 和 JNK3 具有高亲和力，IC50 值分别为 40 nM、50 nM 和 90 nM。SP600125 具有抗炎和抗肿瘤作用，可用于 JNK 信号通路相关疾病的研究。

SP600125 化学结构
CAS号：129-56-6

SP600125 3D分子结构
CAS号：129-56-6

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SP600125 纯度/质量文件产品仅供科研

货号：A155219 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

JNK 亚型比较

产品名称	JNK ↓ ↑	JNK1 ↓ ↑	JNK2 ↓ ↑	JNK3 ↓ ↑	其他靶点	纯度
Mulberroside A	✔					99%+
Loureirin B	✔				Calcium Channel,Potassium Channel	99%+
Ginsenoside Re	✔				NF-κB	98%
(+)-(3R,8S)-Falcarindiol	✔				STAT,ERK	99%+
trans-Zeatin	✔				ERK,p38 MAPK	95+%
Urolithin B	✔				ERK,NF-κB	95%
Cucurbitacin IIb	✔				NF-κB	98+%
Astragaloside IV	✔				mTOR,NF-κB,Akt	98%
NDMC101	✔					99%+
DB07268		++++ JNK1, IC50: 9 nM				99%+
SP600125	+ MKK4, IC50: 0.4 μM	+++ JNK1, IC50: 40 nM	+++ JNK2, IC50: 40 nM	+++ JNK3, IC50: 90 nM		98%
JNK-IN-7		++++ JNK1, IC50: 1.5 nM	++++ JNK2, IC50: 2 nM	++++ JNK3, IC50: 0.7 nM		98+%
JNK-IN-8		++++ JNK1, IC50: 4.7 nM	+++ JNK2, IC50: 18.7 nM	++++ JNK3, IC50: 1 nM		99%+
3,3',5-Triiodo-L-thyronine		++ JNK1, Kd: 240 nM	++ JNK2, Kd: 290 nM	+++ JNK3, Kd: 66 nM		98%
IQ-1S free acid		+ JNK1, IC50: 390 nM	++ JNK2, IC50: 360 nM	+++ JNK3, IC50: 87 nM		98%
BI-78D3	++ JNK, IC50: 280 nM	++ JNK, IC50: 280 nM	++ JNK, IC50: 280 nM	++ JNK, IC50: 280 nM		99%+
Bentamapimod		+++ JNK1, IC50: 80 nM	+++ JNK2, IC50: 90 nM	++ JNK3, IC50: 230 nM		98%
Resveratrol		+ JNK1, IC50: 50 μM				98%
Indirubin-3′-oxime		✔				99%+
SU3327	+ JNK, IC50: 0.7 μM	+ JNK, IC50: 0.7 μM	+ JNK, IC50: 0.7 μM	+ JNK, IC50: 0.7 μM		99%+
JNK Inhibitor VIII		++++ JNK1, Ki: 2 nM JNK1, IC50: 45 nM	++++ JNK2, IC50: 160 nM JNK2, Ki: 4 nM	+++ JNK3, Ki: 52 nM		98%
Doramapimod			✔			99%+
RPI-1			✔			97%
TCS JNK 5a			++ JNK2, pIC50: 6.5	++ JNK3, pIC50: 6.7		98%
SP 600125, negative control			+ JNK2, IC50: 18 μM	+ JNK3, IC50: 24 μM		97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

SP600125 生物活性

靶点	JNK1 JNK1, IC50:40 nM JNK MKK4, IC50:0.4 μM JNK2 JNK2, IC50:40 nM JNK3 JNK3, IC50:90 nM
描述	c-Jun N-terminal kinase (JNK) is a serine threonine protein kinase that belongs to the mitogen-activated protein kinase family. SP-600125 is an anthrapyrazolone inhibitor of JNK with IC50 values of 40, 40, and 90nM for JNK1, JNK2, and JNK3, respectively. SP-600125 also exhibits inhibitory activity against p56Lck, MMK3, MMK4, MMK6, MM7, PKB/AKT, and PKCα with IC50 values of 4.3, 1.5, 0.4, 1.0, 5.1, 1.0, and 1.5μM, respectively. SP-600125 inhibited JNK2 in an ATP-competitive manner with a K_i value of 0.19±0.06μM. It inhibited the phosphorylation of c-Jun in Jurkat T cells with an IC50 value of 5-10μM. In cells stimulated with PMA and phytohemagglutinin, SP-600125 inhibited both IL-2 and IFN-γ expression in a dose-dependent manner with IC50 values of 6 and 7μM, respectively. The incubation of Th1 cells with SP-600125 for 5 days potently inhibited the expression of IFN-γ, TNF-α, and IL-10 (IC50 = 7-12μM), but only weakly blocked the production of IL-1β and IL-6 (IC50 > 30μM). In primary human peripheral blood mononuclear cells stimulated with LPS (100 ng/ml) for 4 h, treatment with SP-600125 dose-dependently inhibited the mRNA expression of COX-2 and TNF-α with IC50 values of 5 and 10μM. In CD-1 mice induced with LPS, intravenous administration of SP-600125 significantly decreased the serum level of TNF-α at doses of 15 and 30mg/kg, while oral administration of 30mg/kg SP-600125 significantly inhibited TNF-α expression compared to the vehicle-treated group^[2].
作用机制	SP-600125 is a small-molecule, ATP-competitive inhibitor of JNK^[1].

SP600125 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A549	20 μM	Growth Inhibition Assay	72 h	Rapid and potent inhibition of cell proliferation	23912840
A549	20 μM	Function Assay	1 h	Inhibition of TPA-induced MMP-2 and u-PA expression	20492175
B16-F10		Function Assay	1 h	Inhibition of TNF-alpha-induced c-JUN phosphorylation	21815634
BV-2	2 μM	Function Assay	1 h	Inhibits the increase of sBAFF release in Gmix-treated BV-2 cells	19406831

SP600125 参考文献

[1]Bennett BL, Sasaki DT, Murray BW, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A. 2001;98(24):13681-13686. doi:10.1073/pnas.251194298

SP600125 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

4.54mL

0.91mL

0.45mL

22.70mL

4.54mL

2.27mL

45.41mL

9.08mL

4.54mL

SP600125 技术信息

CAS号	129-56-6
分子式	C₁₄H₈N₂O
分子量	220.226

别名	蒽[1,9-cd]吡唑-6(2H)-酮 ;NSC 75890;Pyrazolanthrone;1PMV
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 12 mg/mL(54.49 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 3 mg/mL clear

PO 0.5% CMC-Na 42 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

A549	20 μM	Growth Inhibition Assay	72 h	Rapid and potent inhibition of cell proliferation	23912840
A549	20 μM	Function Assay	1 h	Inhibition of TPA-induced MMP-2 and u-PA expression	20492175
B16-F10		Function Assay	1 h	Inhibition of TNF-alpha-induced c-JUN phosphorylation	21815634
BV-2	2 μM	Function Assay	1 h	Inhibits the increase of sBAFF release in Gmix-treated BV-2 cells	19406831
HaCaT	20 μM	Function Assay	4 h	Blocks the TNF-α-induced CYP4F11 transcription	19812349
HaCaT	20 μM	Function Assay	24 h	Blocks the phosphorylation of c-Jun protein	19812349
Hep3B	10 μM	Function Assay	1 h	Blocks autophagy and upregulation of Beclin 1 expression induced by ceramide	19060920
LoVo	1 μM	Function Assay	1 h	Inhibition of PGE2-induced expression of uPA and MMP-9 significantly	21859479
LoVo	1 μM	Function Assay	1 h	BlocksPGE2-induced cell migration significantly	21859479
PC12	10 μM	Function Assay	5 h	Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with PD98059	21345685
PC12	10 μM	Function Assay	5 h	Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with U0126	21345685
PC12	10 μM	Function Assay	5 h	Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with SP600125	21345685
PC12	10 μM	Function Assay	5 h	Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with SB203580	21345685
PC3	25 μM	Function Assay	24 h	Inhibition of AP-1 and p21 luciferase activity induced by S179D PRL	23162652
PC3	20 μM	Function Assay	1 h	Decreases the MMP2 and MMP9 expression	19633975
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 GB4		Antibacterial Assay	72 h	Antiplasmodial activity with IC50 of 12.5893μM	19734910
Plasmodium falciparum HB3		Antibacterial Assay	72 h	Antiplasmodial activity with IC50 of 7.94328 μM	19734910
Plasmodium falciparum W2		Antibacterial Assay	72 h	Antiplasmodial activity with IC50 of 7.94328 μM	19734910
RAW264.7	10 μM	Function Assay	12 h	Antiinflammatory activity assessed as inhibition of LPS-induced NO production with IC50 of 17μM	19497418
RAW264.7	10 μM	Function Assay	24 h	Antiinflammatory activity assessed as inhibition of IL-1beta release	23791078
RAW264.7	10 μM	Function Assay	24 h	Antiinflammatory activity assessed as inhibition of LPS-induced iNOS expression	23791078
RAW264.7	10 μM	Function Assay	2 h	Antiinflammatory activity assessed as inhibition of LPS-induced NO production	23791078
SH-SY5Y	10 μM	Function Assay	1 h	Neuroprotective activity assessed as reduction of anisomycin-induced cell death	23498914
SH-SY5Y	10 μM	Kinase Assay	1 h	Inhibition of JNK3 assessed as blockade of anisomycin-induced c-jun phosphorylation at ser73	23498914
THP-1	90 nM	Function Assay	30 min	Inhibition of tissue factor expression	22940059

1,9-吡唑并蒽酮 /SP600125 98%

SP600125 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

SP600125 质控信息

SP600125 生物活性

SP600125 细胞研究

SP600125 参考文献

SP600125 实验方案

SP600125 技术信息

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JNK1	JNK1, IC50:40 nM
JNK	MKK4, IC50:0.4 μM
JNK2	JNK2, IC50:40 nM
JNK3	JNK3, IC50:90 nM

1,9-吡唑并蒽酮 /SP600125 98%

SP600125 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

SP600125 质控信息

SP600125 生物活性

SP600125 细胞研究

SP600125 参考文献

SP600125 实验方案

SP600125 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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SP600125 纯度/质量文件产品仅供科研