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SP600125

SP600125

产品编号 T3109   CAS 129-56-6
别名: 1PMV, JNK Inhibitor II, Nsc75890, Pyrazolanthrone

SP600125 (JNK Inhibitor II) 是一种 JNK 抑制剂,抑制 JNK1、JNK2 和 JNK3 (IC50=40/40/90 nM),具有口服有效性、可逆性和 ATP 竞争性。SP600125 可以抑制自噬,诱导凋亡

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SP600125 Chemical Structure
SP600125, CAS 129-56-6
规格 价格/CNY 货期 数量
10 mg ¥ 449 现货
50 mg ¥ 712 现货
100 mg ¥ 996 现货
200 mg ¥ 1,885 现货
500 mg ¥ 3,997 现货
1 mL * 10 mM (in DMSO) ¥ 321 现货
产品目录号及名称: SP600125 (T3109)
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纯度: 99.58%
纯度: 99.58%
纯度: 97.63%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 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.
靶点活性 JNK3:90 nM (cell free), JNK1:40 nM (cell free), JNK2:40 nM (cell free)
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]
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].
别名 1PMV, JNK Inhibitor II, Nsc75890, Pyrazolanthrone
分子量 220.23
分子式 C14H8N2O
CAS No. 129-56-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 22 mg/mL (100 mM)

Ethanol: 1.1 mg/mL (5 mM)), with gentle warming

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 4.5407 mL 22.7035 mL 45.4071 mL 113.5177 mL
5 mM 0.9081 mL 4.5407 mL 9.0814 mL 22.7035 mL
DMSO 10 mM 0.4541 mL 2.2704 mL 4.5407 mL 11.3518 mL
20 mM 0.227 mL 1.1352 mL 2.2704 mL 5.6759 mL
50 mM 0.0908 mL 0.4541 mL 0.9081 mL 2.2704 mL
100 mM 0.0454 mL 0.227 mL 0.4541 mL 1.1352 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Li CH, et al. Enhancement of radiosensitivity by inhibition of c-Jun N-terminal kinase activity in a Lewis lung carcinoma‑bearing subcutaneous tumor mouse model. Oncol Rep. 2016 Dec;36(6):3397-3404. 2. Bennett BL, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A. 2001 Nov 20;98(24):13681-6. 3. Yu H, et al. SP600125 enhances C-2-induced cell death by the switch from autophagy to apoptosis in bladder cancer cells. J Exp Clin Cancer Res. 2019 Nov 4;38(1):448. 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. 5. Zheng Y, Wang Y, Zhang X, et al. C19, a C-terminal peptide of CKLF1, decreases inflammation and proliferation of dermal capillaries in psoriasis[J]. Scientific Reports. 2017, 7(1): 1-11. 6. Qiu Y, Sun Y, Xu D, et al. Screening of FDA-approved drugs identifies sutent as a modulator of UCP1 expression in brown adipose tissue[J]. EBioMedicine. 2018, 37: 344-355. 7. Liu J, Lv L, Gong J, et al. Overexpression of F-box only protein 31 predicts poor prognosis and deregulates p38α- and JNK-mediated apoptosis in esophageal squamous cell carcinoma [J]. International journal of cancer. 2018 Jan 1;142(1):145-155. 8. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma[J]. Theranostics. 2020, 10(14): 6530. 9. Dong L, Gong J, Wang Y, et al. Chiral geometry regulates stem cell fate and activity[J]. Biomaterials. 2019: 119456. 10. Yujie Deng, et al. Reciprocal inhibition of YAP/TAZ and NF-κB regulates osteoarthritic cartilage degradation [J]. Nature communications. 2018 Nov 1;9(1):4564.

文献引用

1. Qiu C, Shen X, Lu H, et al.Combination therapy with HSP90 inhibitors and piperlongumine promotes ROS-mediated ER stress in colon cancer cells.Cell Death Discovery.2023, 9(1): 375. 2. Zou X, Zeng M, Zheng Y, et al.Comparative Study of Hydroxytyrosol Acetate and Hydroxytyrosol in Activating Phase II Enzymes.Antioxidants.2023, 12(10): 1834. 3. Shen S, Huang Z, Lin L, et al.Tussilagone attenuates atherosclerosis through inhibiting MAPKs-mediated inflammation in macrophages.International Immunopharmacology.2023, 119: 110066. 4. Li M, Wang Z, Fu S, et al.Taurine reduction of injury from neutrophil infiltration ameliorates Streptococcus uberis-induced mastitis.International Immunopharmacology.2023, 124: 111028. 5. Yu Y, Wu T, Zhang X, et al.Regorafenib activates oxidative stress by inhibiting SELENOS and potentiates oxaliplatin-induced cell death in colon cancer cells.European Journal of Pharmacology.2023: 175986. 6. Wang D, Wang H, Yan Y, et al.Coating 3D-printed bioceramics with histatin promotes adhesion and osteogenesis of stem cells.Tissue Engineering.2023 (ja). 7. Yang N, Zou C, Luo W, et al. Sclareol attenuates angiotensin II‐induced cardiac remodeling and inflammation via inhibiting MAPK signaling. Phytotherapy Research. 2022 8. Wen Y, Peng D, Li C, et al. A new polysaccharide isolated from Morchella importuna fruiting bodies and its immunoregulatory mechanism. International Journal of Biological Macromolecules. 2019, 137: 8-19. 9. Bai G, Chen B, Xiao X, et al. Geniposide inhibits cell proliferation and migration in human oral squamous carcinoma cells via AMPK and JNK signaling pathways. Experimental and Therapeutic Medicine. 2022, 24(6): 1-10. 10. Ciou H H, Lee T H, Wang H C, et al. Repurposing gestrinone for tumor suppressor through P21 reduction regulated by JNK in gynecological cancer. Translational Research. 2021
11. Wang M, Sun J, Yu T, et al. Diacerein protects liver against APAP-induced injury via targeting JNK and inhibiting JNK-mediated oxidative stress and apoptosis. Biomedicine & Pharmacotherapy. 2022, 149: 112917 12. Zhang T, Xu C, Zheng P, et al. Glaucocalyxin B Attenuates Ovarian Cancer Cell Growth and Cisplatin Resistance In Vitro via Activating Oxidative Stress. Oxidative Medicine and Cellular Longevity. 2022 13. Chen X, Lin J, Hu T, et al. Galectin‐3 exacerbates ox‐LDL‐mediated endothelial injury by inducing inflammation via integrin β1‐RhoA‐JNK signaling activation. Journal of Cellular Physiology. 2019 Jul;234(7):10990-11000 14. Qiu Y, Sun Y, Xu D, et al. Screening of FDA-approved drugs identifies sutent as a modulator of UCP1 expression in brown adipose tissue. EBioMedicine. 2018, 37: 344-355. 15. Wang Y, Zeng Y, Zhu L, et al. Polysaccharides from Lentinus edodes inhibits lymphangiogenesis via the toll-like receptor 4/JNK pathway of cancer-associated fibroblasts. Frontiers in Oncology. 2021: 3419. 16. Zhu Y, Xiao Y, Kong D, et al. Down-Regulation of miR-378d Increased Rab10 Expression to Help Clearance of Mycobacterium tuberculosis in Macrophages. Frontiers in cellular and infection microbiology. 2020, 10: 108. 17. Chang Y H, Chiang C Y, Fu E, et al. Staphylococcus aureus enhances gelatinase activities in monocytic U937 cells and in human gingival fibroblasts. Journal of Dental Sciences. 2022 18. Zheng Y, Wang Y, Zhang X, et al. C19, a C-terminal peptide of CKLF1, decreases inflammation and proliferation of dermal capillaries in psoriasis. Scientific Reports. 2017, 7(1): 1-11 19. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma. Theranostics. 2020, 10(14): 6530. 20. Hu H, Jiang H, Zhang K, et al. Memantine nitrate MN-08 suppresses NLRP3 inflammasome activation to protect against sepsis-induced acute lung injury in mice. Biomedicine & Pharmacotherapy. 2022, 156: 113804 21. Deng Y, Lu J, Li W, et al. Reciprocal inhibition of YAP/TAZ and NF-κB regulates osteoarthritic cartilage degradation. Nature Communications. 2018, 9(1): 1-14 22. Bai G, Wang H, Cui N. mTOR pathway mediates endoplasmic reticulum stress-induced CD4+ T cell apoptosis in septic mice. Apoptosis. 2022: 1-11 23. Shen S, Wu G, Luo W, et al. Leonurine attenuates angiotensin II-induced cardiac injury and dysfunction via inhibiting MAPK and NF-κB pathway. Phytomedicine. 2022: 154519. 24. Zhang P, Zhang J, Quan H, et al. Effects of butein on human osteosarcoma cell proliferation, apoptosis, and autophagy through oxidative stress. Human & Experimental Toxicology. 2022, 41: 09603271221074346. 25. Xu C, Zhao W, Huang X, et al. TORC2/3-mediated DUSP1 upregulation is essential for human decidualization. Reproduction. 2021, 1(aop). 26. Liu J, Lv L, Gong J, et al. Overexpression of F-box only protein 31 predicts poor prognosis and deregulates p38α- and JNK-mediated apoptosis in esophageal squamous cell carcinoma. International Journal of Cancer. 2018, 142(1): 145-155 27. Hu Q, Du H, Ma G, et al. Purification, identification and functional characterization of an immunomodulatory protein from Pleurotus eryngii. Food & Function. 2018, 9(7): 3764-3775 28. Dong L, Gong J, Wang Y, et al. Chiral geometry regulates stem cell fate and activity. Biomaterials. 2019: 119456. 29. Wu F, Shao R, Zheng P, et al. Isoalantolactone Enhances the Antitumor Activity of Doxorubicin by Inducing Reactive Oxygen Species and DNA Damage. Frontiers in Oncology. 2022: 81. 30. Pak M E, Park Y J, Yang H J, et al. Samhwangsasim-tang attenuates neuronal apoptosis and cognitive decline through BDNF-mediated activation of tyrosin kinase B and p76-neurotrophin receptors. Phytomedicine. 2022: 153997. 31. Cui S, Suo N, Yang Y, et al.The aminosteroid U73122 promotes oligodendrocytes generation and myelin formation.Acta Pharmacologica Sinica.2023: 1-12. 32. Ouyang P, Tao Y, Wei W, et al.Spring Viremia of Carp Virus Infection Induces Carp IL-10 Expression, Both In Vitro and In Vivo.Microorganisms.2023, 11(11): 2812. 33. Zhang L, Wang J, Xu T, et al.Bicyclol alleviates obesity-induced renal injury by inhibiting JNK and NF-κB-mediated inflammation.International Immunopharmacology.2024, 129: 111609.
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NADPH tetrasodium salt CIL56 Fluvastatin sodium Artemisinin Ciclopirox Dopamine hydrochloride L-Glutathione reduced Erastin

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抗癌活性化合物库 神经退行性疾病化合物库 HIF-1化合物库 表型筛选靶点鉴定库 抗前列腺癌化合物库 成骨分子库 神经再生化合物库 内质网应激化合物库 已知活性化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

SP600125 129-56-6 Apoptosis Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic MAPK Tyrosine Kinase/Adaptors Ferroptosis Trk receptor Aurora Kinase JNK ATP-competitive inhibit 1PMV JNK Inhibitor II Inhibitor Nsc75890 Pyrazolanthrone SP-600125 phosphorylation SP 600125 reversible inhibitor

 

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