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SP600125

Catalog No. T3109 CAS 129-56-6

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

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

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 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	JNK Inhibitor II, 1PMV, 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 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 )

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. 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.

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

Related compound libraries

This product is contained In the following compound libraries：

Preclinical Compound Library Target-Focused Phenotypic Screening Library Anti-Cancer Active Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Diabetic Compound Library Bioactive Compound Library Neural Regeneration Compound Library Reprogramming Compound Library Immunology/Inflammation Compound Library Osteogenesis Compound Library

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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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