SP 600125.|129-56-6|-陌孚医药/Medlife

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SP 600125.

目录号: PC11760 纯度: ≥98%

CAS No. :129-56-6

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PC11760-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥700.00	请登录

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中文名称

SP 600125.

中文别名

吡唑蒽酮;炭疽[1,9-cd]吡唑-6(2H)-酮;1,9-吡唑并蒽酮;Anthra[1,9-cd]pyrazol-6(2H)-one 炭疽[1,9-cd]吡唑-6(2H)-酮;蒽并[1,9-cd]吡唑-6（2H）-酮;二苯并[cd,g]吲唑-6(2H)-酮;蒽并吡唑酮;蒽[1,9-CD]吡唑-6(2H)-酮

英文名称

SP 600125

英文别名

Dibenzo[cd,g]indazol-6(2H)-one;Anthra[1,9-cd]pyrazol-6(2H)-one;SP600125;1 9-PYRAZOLEANTHRONE;1,9-Pyrazoloanthrone;2H-Dibenzo[CD,G]Indazol-6-One;SP600125 (NSC 75890,Pyrazolanthrone);SP-600125;JNKII;Nsc75890;c.i.70300;pyrazolanthrone;ANTHRAPYRAZOLONE;JNK INHIBITOR II;SP 600125;SP600125 >99%;InSolution™SP 600125, >=98%

Cas No.

129-56-6

分子式

C₁₄H₈N₂O

分子量

220.23

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC₅₀s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.

性状

Solid

IC50 & Target[1][2]

JNK1

40 nM (IC₅₀)

JNK2

40 nM (IC₅₀)

JNK3

90 nM (IC₅₀)

Autophagy

体外研究(In Vitro)

SP600125 is an ATP-competitive inhibitor of JNK2 with a K_i value of 0.19±0.06 μM. SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM in Jurkat T cells. 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.
In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Administration of SP600125 at 15 or 30 mg/kg i.v. significantly inhibits TNF-α serum levels, whereas oral administration dose-dependently blocks TNF-α expression with significant inhibition observed at 30 mg/kg per os.
SP600125 attenuates LPS-induced ALI in rats in vivo. The expression levels of TNF-α and IL-6 in the BALF in rats in the SP600125 group are significantly decreased.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Bennett BL, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686. [Information]

[2]. Vaishnav D, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochem Biophys Res Commun, 2003, 307(4), 855-860. [Information]

[3]. Kim JA, et al. SP600125 suppresses Cdk1 and induces endoreplication directly from G2 phase, independent of JNK inhibition. Oncogene, 2010, 29(11), 1702-1716. [Information]

[4]. Zheng Y, et al. JNK inhibitor SP600125 protects against lipopolysaccharide-induced acute lung injury via upregulation ofclaudin-4. Exp Ther Med. 2014 Jul;8(1):153-158. [Information]

[5]. Zhang H, et al. SP600125 Suppresses Keap1 Expression and Results in NRF2-mediated Prevention of Diabetic Nephropathy. J Mol Endocrinol. J Mol Endocrinol. 2018 Feb;60(2):145-157. [Information]

[6]. Yatsushige H, et al. Role of c-Jun N-terminal kinase in cerebral vasospasm after experimental subarachnoid hemorrhage. Stroke. 2005 Jul;36(7):1538-43. [Information]

溶解度数据

体外研究:

DMSO : 12.5 mg/mL (56.76 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 1% CMC-Na/saline water
Solubility: 3.33 mg/mL (15.12 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (9.44 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (9.44 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： corn oil
Solubility: 1 mg/mL (4.54 mM); Suspended solution; Need ultrasonic and warming and heat to 80°C

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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