|1,9-吡唑并蒽酮|CsnPharm

CAS No.: 129-56-6

1,9-吡唑并蒽酮 Catalog No. CSN12230

Synonyms: Nsc75890;1PMV;Pyrazolanthrone

SP-600125 is a competitive and reversible JNK inhibitor with IC50 values of 40 nM, 40 nM and 90 nM for JNK1, 2 and 3.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Aurora Kinase A

IC50:60nM FLT3

IC50:90nM JNK1

IC50:40nM JNK2

IC50:40nM JNK3

IC50:90nM 更多
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].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.5407 mL
- 22.7035 mL
- 45.4071 mL
- 5 mM
- 0.9081 mL
- 4.5407 mL
- 9.0814 mL
- 10 mM
- 0.4541 mL
- 2.2704 mL
- 4.5407 mL

技术信息

CAS号

129-56-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H8N2O

运输

蓝冰

分子量

220.23

别名

Nsc75890;1PMV;Pyrazolanthrone

溶解度

DMSO	13.64 mg/mL (61.9 mM) warming
Water	insoluble

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

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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

靶点	Description	IC50
Aurora Kinase A		IC50:60nM
FLT3		IC50:90nM
JNK1		IC50:40nM
JNK2		IC50:40nM
JNK3		IC50:90nM
MEK3		IC50:1.5μM
MEK4		IC50:0.4μM
MEK6		IC50:1μM
PKCα		IC50:1.5μM
Trk Receptor A		IC50:70nM

1,9-吡唑并蒽酮 Catalog No. CSN12230

靶点选择性

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