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SP600125

Catalog No. T3109   CAS 129-56-6
Synonyms: ATP-competitive, JNK, SP 600125, inhibit, Inhibitor, Apoptosis, JNK Inhibitor II, 1PMV, Ferroptosis, SP-600125, Nsc75890, Pyrazolanthrone, phosphorylation, Autophagy, SP600125, reversible

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
SP600125, CAS 129-56-6
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 JNK3:90 nM (cell free), JNK1:40 nM (cell free), JNK2:40 nM (cell free)
In vitro 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].
In vivo 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].
Cell Research 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].
Animal Research 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].
Synonyms ATP-competitive, JNK, SP 600125, inhibit, Inhibitor, Apoptosis, JNK Inhibitor II, 1PMV, Ferroptosis, SP-600125, Nsc75890, Pyrazolanthrone, phosphorylation, Autophagy, SP600125, reversible
Molecular Weight 220.231
Formula C14H8N2O
CAS No. 129-56-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

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 )

Citations

References and Literature
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. 1. 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. 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. 2. 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 3. Dong L, Gong J, Wang Y, et al. Chiral geometry regulates stem cell fate and activity. Biomaterials. 2019: 119456. 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. 4. 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 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. 5. 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. 6. 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 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. 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. International Journal of Cancer. 2018, 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. 8. 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 9. 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. 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. 10. 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. 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. Yang N, Zou C, Luo W, et al. Sclareol attenuates angiotensin II‐induced cardiac remodeling and inflammation via inhibiting MAPK signaling. Phytotherapy Research. 2022 13. 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. 14. 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. 15. Bai G, Wang H, Cui N. mTOR pathway mediates endoplasmic reticulum stress-induced CD4+ T cell apoptosis in septic mice. Apoptosis. 2022: 1-11 16. 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 17. 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. 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. 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 20. 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. 21. Xu C, Zhao W, Huang X, et al. TORC2/3-mediated DUSP1 upregulation is essential for human decidualization. Reproduction. 2021, 1(aop). 22. 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. 23. 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. 24. 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

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Endoplasmic Reticulum Stress Compound Library Preclinical Compound Library Autophagy Compound Library Anti-Lung Cancer Compound Library HIF-1 Signaling Pathway Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Neural Regeneration Compound Library Immunology/Inflammation Compound Library

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