化合物 Pyrazolanthrone|T3109

SP600125
129-56-6

￥449 10mg 起订

￥712 50mg 起订

￥996 100mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Pyrazolanthrone

英文名称：: SP600125

CAS号：: 129-56-6

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.58%

产品类别：: 抑制剂

货号：: T3109

Product Introduction

Bioactivity

名称	SP600125
描述	SP600125 (JNK Inhibitor II) is a JNK inhibitor that inhibits JNK1, JNK2, and JNK3 (IC50=40/40/90 nM) with oral potency, reversibility, and ATP-competitive properties. SP600125 inhibits autophagy and induces apoptosis.
细胞实验	Multiarray plate screening of mRNA was performed by High Throughput Genomics. In brief, cell lysates were prepared by using a single-step proprietary lysis buffer. Lysates were incubated with a 16-gene capture array manufactured into each well of a 96-well plate. Detection was by luminescence and was performed by HTG. SDs for triplicate samples were typically 3–8% for samples with high levels of gene expression and 15–25% for samples with very low (near-threshold) levels of cytokine gene expression [1].
动物实验	Mouse LPS/TNF assay was performed as follows: Female CD-1 mice (8–10 weeks of age) were dosed i.v. or per os with SP600125 in PPCES vehicle (30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline), final volume of 5 ml/kg, 15 min before i.v. injection with LPS in saline (0.5 mg/kg; Escherichia coli 055:B5). At 90 min, a terminal bleed was obtained from the abdominal vena cava, and the serum was recovered. Samples were analyzed for mouse TNF-α by using an ELISA. The in-life phase of the thymocyte apoptosis assay was performed in female C57BL/6 mice. SP600125 was administered at 0, 12, 24, and 36 h, 15 mg/kg s.c. in PPCES vehicle. Anti-CD3 (50 μg) i.p. (clone 145-2C11) was administered as a single dose immediately after SP600125 at time 0. After 48 h, mice were killed, and the thymus was dissected for thymocyte isolation. Treated and untreated mice thymuses were excised and immediately placed in complete medium (RPMI medium 1640 with 10% FBS, penicillin/streptomycin, and l-glutamine) on ice. Each thymus was then pressed between the frosted ends of 2 microscope slides to form a single cell suspension and collected through a 30 μm nylon mesh. Cells were stained for cell surface CD4 and CD8 and apoptosis and measured by flow cytometry [1].
体外活性	方法：小鼠肺癌细胞 LLC 和小鼠肿瘤细胞 4T1 用 SP600125 (3-10 μM) 处理 72 h，使用 MTT assay 检测细胞活力。结果：SP600125 剂量依赖性抑制 LLC 和 4T1 细胞生长，IC50 为 8.14 μM 和 7.37 μM。[1] 方法：Jurkat T 细胞用 SP600125 (1-50 μM) 预处理 10 min，随后用 PMA (50 ng/mL)、anti-CD3 (0.5 μg/mL) 和 anti-CD28 (2 μg/mL) 刺激 30 min，使用 Western Blot 方法检测靶点蛋白表达水平。结果：SP600125 以 5-10 μM 的 IC50 阻断 c-Jun 的磷酸化。在 50 μM 的浓度下，SP600125 不阻断 ERK 的磷酸化，也不抑制 IκBα 的降解。在 50 μM 时观察到磷酸-p38 和 ATF2 的部分抑制，但在 25 μM 时没有观察到。[2]
体内活性	方法：为检测体内对 TNF-α 的抑制活性，将 SP600125 (7.5-30 mg/kg，30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline) 静脉注射或口服给药给 CD-1 小鼠，15 min 后注射 LPS 诱导的 TNF-α 表达。结果：静脉注射 15 或 30 mg/kg SP600125 可显著抑制 TNF-α 血清水平，而口服给药剂量依赖性阻断 TNF-α 表达，每次口服 30 mg/kg 可观察到显著抑制作用。[2] 方法：为检测体内抗肿瘤活性，将 SP600125 (5 mg/kg) 和 C-2 (10 mg/kg) 腹腔注射给携带膀胱癌肿瘤 BIU87 的 nude 小鼠，每天一次，持续二十一天。结果：C-2 治疗抑制了肿瘤的生长，C-2/SP600125 组肿瘤显著低于用载体或 C-2 单独治疗的小鼠。[3]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Methanol : 1.25 mg/mL (5.68 mM), Sonication is recommended. DMSO : 50 mg/mL (227.04 mM) Ethanol : 1.1 mg/mL (5 mM)), Heating is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.2 mg/mL (9.99 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
关键字	ATP-competitive \| JNK \| inhibit \| Inhibitor \| Apoptosis \| SP-600125 \| Ferroptosis \| phosphorylation \| SP 600125 \| Autophagy \| SP600125 \| reversible
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Pyrazolanthrone|||Nsc75890|||JNK Inhibitor II|||1PMV|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子