Determine the necessary mass, volume, or concentration for preparing a solution.
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SKU | Size | Availability | Price | Qty |
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S131899-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $10.90 | |
S131899-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $42.90 | |
S131899-100mg | 100mg | In stock | $141.90 | |
S131899-500mg | 500mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $639.90 |
p38 MAPK inhibitor
Synonyms | ES-0013 | RWJ64809 | RWJ-64809 | CHEBI:90705 | UNII-OU13V1EYWQ | J-008891 | 4-[5-(4-Fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-4-yl]pyridine | CS-0140 | Prestwick3_001051 | RWJ 64809 | BCP01763 | HMS3244I15 | PYRIDINE, 4-(4-(4-FLUOROPHENYL)-2- |
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Specifications & Purity | Moligand™, ≥98%(HPLC) |
Biochemical and Physiological Mechanisms | Cell-permeable p38 MAPK inhibitor. Shows selectivity over many other kinases but also shown to have some inhibitory activity against GAK, CK1, RIP2, c-Raf and GSK3. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of cyclin G associated kinase;Inhibitor of mitogen-activated protein kinase 11;Inhibitor of mitogen-activated protein kinase 14 |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine |
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INCHI | InChI=1S/C21H16FN3OS/c1-27(26)18-8-4-16(5-9-18)21-24-19(14-2-6-17(22)7-3-14)20(25-21)15-10-12-23-13-11-15/h2-13H,1H3,(H,24,25) |
InChi Key | CDMGBJANTYXAIV-UHFFFAOYSA-N |
Canonical SMILES | CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F |
Isomeric SMILES | CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F |
WGK Germany | 3 |
PubChem CID | 176155 |
Molecular Weight | 377.43 |
CAS Registry No. | 152121-47-6 |
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Wikipedia | SB_203580 |
PubChem CID | 176155 |
DiscoveRx TREEspot | SB-203580| |
ChEMBL Ligand | CHEMBL10 |
Enter Lot Number to search for COA:
Solubility | Soluble in DMSO (50 mg/ml), aqueous buffers (Sparingly soluble), methanol, acetone, ethanol (~0.2 mg/ml), and 1:9 solution of DMF:PBS(PH 7.2) (~0.5 mg/ml). |
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Sensitivity | Heat Sensitive |
Refractive Index | 1.71 |
Boil Point(°C) | 615.6° C |
Melt Point(°C) | 280.73°C |
Pictogram(s) | GHS05, GHS07 |
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Signal | Danger |
Hazard Statements | H302:Harmful if swallowed H318:Causes serious eye damage |
Precautionary Statements | P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. |
WGK Germany | 3 |
1. Chen Huang, Tao Zhou, Lihua Ma, Shipeng Zhao. (2023) IFI6 Downregulation Reverses Oxaliplatin Resistance of Colorectal Cancer Cells by Activating the ROS-Induced p38MAPK Signaling Pathway. BIOLOGICAL & PHARMACEUTICAL BULLETIN, 46 (1): (26-34). [PMID:36596524] |
1. Lee JC, Kumar S, Griswold DE, Underwood DC, Votta BJ, Adams JL. (2000) Inhibition of p38 MAP kinase as a therapeutic strategy.. Immunopharmacology, 47 (2-3): (185-201). [PMID:10878289] |
2. Frantz B, Klatt T, Pang M, Parsons J, Rolando A, Williams H, Tocci MJ, O'Keefe SJ, O'Neill EA. (1998) The activation state of p38 mitogen-activated protein kinase determines the efficiency of ATP competition for pyridinylimidazole inhibitor binding.. Biochemistry, 37 (39): (13846-53). [PMID:9753474] |
3. Niu J et al.. (2017) Activation of dorsal horn cannabinoid CB2 receptor suppresses the expression of P2Y12and P2Y13receptors in neuropathic pain rats.. J Neuroinflammation, 14 (185). [PMID:28899427] |
4. Kim N et al.. (2016) AMPK, a metabolic sensor, is involved in isoeugenol-induced glucose uptake in muscle cells.. J Endocrinol, 228 (2): (105-14). [PMID:26585419] |
5. Singh TD et al.. (2015) Anticancer properties and enhancement of therapeutic potential of cisplatin by leaf extract of Zanthoxylum armatum DC.. Biol Res, 48 (46). [PMID:26290043] |
6. Joung EJ et al.. (2012) Anti-inflammatory effect of ethanolic extract from Myagropsis myagroides on murine macrophages and mouse ear edema.. BMC Complement Altern Med, 12 (171). [PMID:23031211] |
7. Wang W et al.. (2017) Antimicrobial peptide LL-37 promotes the viability and invasion of skin squamous cell carcinoma by upregulating YB-1.. Exp Ther Med, 14 (499-506). [PMID:28672959] |
8. Al-Owais MM et al.. (2012) Carbon monoxide mediates the anti-apoptotic effects of heme oxygenase-1 in medulloblastoma DAOY cells via K+ channel inhibition.. J Biol Chem, 287 (29): (24754-64). [PMID:22593583] |
9. Alsamri H et al.. (2022) Carnosol Induces p38-Mediated ER Stress Response and Autophagy in Human Breast Cancer Cells.. Front Oncol, 12 (911615). [PMID:35712465] |
10. El Hachmane MF et al.. (2014) Enhancement of TWIK-related acid-sensitive potassium channel 3 (TASK3) two-pore domain potassium channel activity by tumor necrosis factor a.. J Biol Chem, 289 (3): (1388-401). [PMID:24307172] |
11. Guo P et al.. (2022) Estrogen Suppresses Cytokines Release in cc4821 Neisseria meningitidis Infection via TLR4 and ERβ-p38-MAPK Pathway.. Front Microbiol, 13 (834091). [PMID:35422784] |
12. Guo X et al.. (2016) Inhibition of renalase expression and signaling has antitumor activity in pancreatic cancer.. Sci Rep, 6 (22996). [PMID:26972355] |
13. Elies J et al.. (2014) Inhibition of the cardiac na+ channel nav1.5 by carbon monoxide.. J Biol Chem, 289 (23): (16421-9). [PMID:24719320] |
14. Sakai S et al.. (2019) Long Noncoding RNA ELIT-1 Acts as a Smad3 Cofactor to Facilitate TGFß/Smad Signaling and Promote Epithelial-Mesenchymal Transition.. Cancer Res, 79 (11): (2821-2838). [PMID:30952633] |
15. Lan CN et al.. (2021) MAPK inhibitors protect against early-stage osteoarthritis by activating autophagy.. Mol Med Rep, 24 (6): [PMID:34590154] |
16. Zhang X et al.. (2020) MicroRNA-375 prevents TGF-ß-dependent transdifferentiation of lung fibroblasts via the MAP2K6/P38 pathway.. Mol Med Rep, 22 (3): (1803-1810). [PMID:32582987] |
17. Zhang Q et al.. (2013) NF-?B, ERK, p38 MAPK and JNK contribute to the initiation and/or maintenance of mechanical allodynia induced by tumor necrosis factor-alpha in the red nucleus.. Brain Res Bull, 99 (132-9). [PMID:24161765] |
18. Lu YQ et al.. (2017) NLRP3 inflammasome activation results in liver inflammation and fibrosis in mice infected with Schistosoma japonicum in a Syk-dependent manner.. Sci Rep, 7 (8120). [PMID:28808303] |
19. Li H et al.. (2018) p38 MAPK-MK2 pathway regulates the heat-stress-induced accumulation of reactive oxygen species that mediates apoptotic cell death in glial cells.. Oncol Lett, 15 (775-782). [PMID:29387240] |
20. Cheng Y et al.. (2013) Proliferation enhanced by NGF-NTRK1 signaling makes pancreatic cancer cells more sensitive to 2DG-induced apoptosis.. Int J Med Sci, 10 (5): (634-40). [PMID:23569426] |
21. Li HN et al.. (2021) Red nucleus IL-33 facilitates the early development of mononeuropathic pain in male rats by inducing TNF-a through activating ERK, p38 MAPK, and JAK2/STAT3.. J Neuroinflammation, 18 (150). [PMID:34225736] |
22. Guo YJ et al.. (2018) Red nucleus interleukin-1ß evokes tactile allodynia through activation of JAK/STAT3 and JNK signaling pathways.. J Neurosci Res, 96 (12): (1847-1861). [PMID:30216497] |
23. Mazrouei S et al.. (2019) Regulation of MAP kinase-mediated endothelial dysfunction in hyperglycemia via arginase I and eNOS dysregulation.. Biochim Biophys Acta Mol Cell Res, 1866 (9): (1398-1411). [PMID:31150695] |
24. Kim HJ et al.. (2012) Reverse signaling through the costimulatory ligand CD137L in epithelial cells is essential for natural killer cell-mediated acute tissue inflammation.. Proc Natl Acad Sci U S A, 109 (E13-22). [PMID:22160719] |
25. Sreekanth GP et al.. (2016) SB203580 Modulates p38 MAPK Signaling and Dengue Virus-Induced Liver Injury by Reducing MAPKAPK2, HSP27, and ATF2 Phosphorylation.. PLoS One, 11 (2): (e0149486). [PMID:26901653] |
26. Kang K & Wang Y. (2019) Sevoflurane Inhibits Proliferation and Invasion of Human Ovarian Cancer Cells by Regulating JNK and p38 MAPK Signaling Pathway.. Drug Des Devel Ther, 13 (4451-4460). [PMID:32021086] |
27. Coricor G & Serra R. (2016) TGF-ß regulates phosphorylation and stabilization of Sox9 protein in chondrocytes through p38 and Smad dependent mechanisms.. Sci Rep, 6 (38616). [PMID:27929080] |
28. Zhang J et al.. (2021) TGF-ß1-induced autophagy activates hepatic stellate\xa0cells via the ERK and JNK signaling pathways.. Int J Mol Med, 47 (256-266). [PMID:33236148] |
29. Zhang Y et al.. (2016) The Effects of Aquaporin-1 in Pulmonary Edema Induced by Fat Embolism Syndrome.. Int J Mol Sci, 17 (7): [PMID:27455237] |
30. Chen Huang, Tao Zhou, Lihua Ma, Shipeng Zhao. (2023) IFI6 Downregulation Reverses Oxaliplatin Resistance of Colorectal Cancer Cells by Activating the ROS-Induced p38MAPK Signaling Pathway. BIOLOGICAL & PHARMACEUTICAL BULLETIN, 46 (1): (26-34). [PMID:36596524] |