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SP600125

Catalog No. T3109 CAS 129-56-6

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

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SP600125, CAS 129-56-6

Pack Size	Availability	Price/USD
10 mg	In stock	$ 41.00
50 mg	In stock	$ 48.00
100 mg	In stock	$ 74.00
200 mg	In stock	$ 93.00
500 mg	In stock	$ 150.00

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Purity: 99.58%

Purity: 97.63%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
Targets&IC50	JNK3:90 nM (cell free), JNK1:40 nM (cell free), JNK2:40 nM (cell free)
In vitro	METHODS: Mouse lung cancer cells LLC and mouse tumor cells 4T1 were treated with SP600125 (3-10 μM) for 72 h, and cell viability was detected using MTT assay. RESULTS: SP600125 dose-dependently inhibited the growth of LLC and 4T1 cells with IC50 of 8.14 μM and 7.37 μM. [1] METHODS: Jurkat T cells were pretreated with SP600125 (1-50 μM) for 10 min, and then stimulated with PMA (50 ng/mL), anti-CD3 (0.5 μg/mL), and anti-CD28 (2 μg/mL) for 30 min, and then the expression levels of target proteins were detected by Western Blot. RESULTS: SP600125 blocked the phosphorylation of c-Jun at an IC50 of 5-10 μM. At a concentration of 50 μM, SP600125 did not block ERK phosphorylation or inhibit IκBα degradation. Partial inhibition of phospho-p38 and ATF2 was observed at 50 μM, but not at 25 μM. [2]
In vivo	METHODS: To test the inhibitory activity of TNF-α in vivo, SP600125 (7.5-30 mg/kg, 30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline) was administered intravenously or orally to CD-1 mice 15 min after LPS-induced TNF-α expression was injected. LPS-induced TNF-α expression was injected 15 min later. RESULTS: Intravenous administration of 15 or 30 mg/kg SP600125 significantly inhibited TNF-α serum levels, while oral administration dose-dependently blocked TNF-α expression, with a significant inhibitory effect observed at 30 mg/kg per oral dose. [2] METHODS: To test the antitumor activity in vivo, SP600125 (5 mg/kg) and C-2 (10 mg/kg) were injected intraperitoneally into nude mice bearing the bladder cancer tumor BIU87 once a day for twenty-one days. RESULTS: C-2 treatment inhibited tumor growth, and tumors in the C-2/SP600125 group were significantly lower than those in mice treated with vector or C-2 alone. [3]
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	1PMV, JNK Inhibitor II, Nsc75890, Pyrazolanthrone
Molecular Weight	220.23
Formula	C14H8N2O
CAS No.	129-56-6

Storage

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

Solubility Information

DMSO: 22 mg/mL (100 mM)

Ethanol: 1.1 mg/mL (5 mM)), Heating is recommended.

References and Literature

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.

Citations

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. 34. Ni L, Zhu X, Zhao Q, et al.Dihydroartemisinin, a potential PTGS1 inhibitor, potentiated cisplatin-induced cell death in non-small cell lung cancer through activating ROS-mediated multiple signaling pathways.Neoplasia.2024, 51: 100991. 35. Shen X, Xia Y, Lu H, et al.Synergistic targeting of TrxR1 and ATM/AKT pathway in human colon cancer cells.Biomedicine & Pharmacotherapy.2024, 174: 116507. 36. Xin J, Wang Z, Shen Y, et al.S100 calcium‑binding protein A16 suppresses the osteogenic differentiation of rat bone marrow mesenchymal stem cells by inhibiting SMAD family member 4 signaling.Experimental and Therapeutic Medicine.2024, 27(6): 1-10.

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This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library Anti-Aging Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Anti-Cancer Compound Library Neural Regeneration Compound Library

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Keywords

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

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