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SP600125

产品编号 T3109 CAS 129-56-6

别名: JNK Inhibitor II, 1PMV, Nsc75890, Pyrazolanthrone

SP600125 是一种口服有效的，可逆的，ATP 竞争性的 JNK 抑制剂，抑制 JNK1，JNK2和 JNK3的 IC50分别为 40，40，90 nM。它是一种有效的铁死亡抑制剂，可抑制自噬，诱导凋亡。

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SP600125, CAS 129-56-6

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	SP600125 is a JNK1/2/3 inhibitor (IC50: 40/40/90 nM) and 10-fold higher selectivity than MKK4, 25-fold higher selectivity than MKK3, MKK6, PKCα, and PKB.
靶点活性	JNK3:90 nM (cell free), JNK1:40 nM (cell free), JNK2:40 nM (cell free)
体外活性	In cells, SP600125 dose-dependently inhibited the phosphorylation of c-Jun ( IC50s: 5–10 μM), the expression of inflammatory genes COX-2, IL-2, IFN-gamma, TNF-alpha, and prevented the activation and differentiation of primary human CD4 cell cultures [1]. Fas agonistic antibody CH11-induced autophagy was blocked by SP600125, and the CH11-induced apoptosis was increased by SP600125 [2]. In synchronized cells, SP600125 prevents the entry of cells into mitosis and leads to endoreplication of DNA from G2 phase. The inhibitory effect of SP600125 on mitotic entry predominantly occurs upstream of Aurora A kinase and Polo-like kinase 1, resulting in a failure to remove the inhibitory phosphorylation of Cdk1 [3].
体内活性	In control animals, CD4+ CD8+ thymocytes represented just less than 40% of total thymocytes. Forty-eight hours after exposure to CD3 Ab in vivo, the percentage of CD4+ CD8 + cells had declined to 10%. Mice receiving SP600125 showed almost complete resistance to CD3 Ab-mediated apoptosis with CD4+ CD8+ numbers the same as control animals [1]. Pulmonary edema, the expression of inflammatory cytokines and pathological alterations were found to be significantly attenuated in LPS-induced ALI following treatment with SP600125 in vivo [4].
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	JNK Inhibitor II, 1PMV, 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 2 years

溶解度

DMSO: 22 mg/mL (100 mM)

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

( < 1 mg/mL refers to the product slightly soluble or insoluble )

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. 2. Zhang Y, et al. Fas-mediated autophagy requires JNK activation in HeLa cells. Biochem Biophys Res Commun. 2008 Dec 26;377(4):1205-10. 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. 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

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

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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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质量

配液浓度

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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 JNK Aurora Kinase ATP-competitive SP 600125 inhibit Inhibitor JNK Inhibitor II 1PMV SP-600125 Nsc75890 Pyrazolanthrone phosphorylation reversible inhibitor

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SP600125

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溶解度

参考文献

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剂量换算

体内实验配液计算器

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