WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H530341
CAS#: 72873-74-6
Description: SKF86002 is a p38 MAP kinase inhibitor. SKF86002 inhibits IL-1 beta production by affecting at least two distinct steps in the biosynthesis of this cytokine.
Hodoodo Cat#: H530341
Name: SKF86002
CAS#: 72873-74-6
Chemical Formula: C16H12FN3S
Exact Mass: 297.07
Molecular Weight: 297.351
Elemental Analysis: C, 64.63; H, 4.07; F, 6.39; N, 14.13; S, 10.78
Synonym: SKF-86002; SKF 86002; SKF86002.
IUPAC/Chemical Name: 6-(4-Fluorophenyl)-5-(4-pyridyl)-2,3-dihydroimidazo[2,1-b]-thiazole
InChi Key: YOELZIQOLWZLQC-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H12FN3S/c17-13-3-1-11(2-4-13)14-15(12-5-7-18-8-6-12)20-9-10-21-16(20)19-14/h1-8H,9-10H2
SMILES Code: FC1=CC=C(C2=C(C3=CC=NC=C3)N4C(SCC4)=N2)C=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 297.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Khattab M, Van Dongen M, Wang F, Clayton AH. Solvatochromism and linear solvation energy relationship of the kinase inhibitor SKF86002. Spectrochim Acta A Mol Biomol Spectrosc. 2017 Jan 5;170:226-33. doi: 10.1016/j.saa.2016.07.027. PubMed PMID: 27450120.
2: Dai HL, Hu WY, Jiang LH, Li L, Gaung XF, Xiao ZC. p38 MAPK Inhibition Improves Synaptic Plasticity and Memory in Angiotensin II-dependent Hypertensive Mice. Sci Rep. 2016 Jun 10;6:27600. doi: 10.1038/srep27600. PubMed PMID: 27283322; PubMed Central PMCID: PMC4901328.
3: Bender Ignacio RA, Lee JY, Rudek MA, Dittmer DP, Ambinder RF, Krown SE; AIDS Malignancy Consortium (AMC)-059 Study Team.. Brief Report: A Phase 1b/Pharmacokinetic Trial of PTC299, a Novel PostTranscriptional VEGF Inhibitor, for AIDS-Related Kaposi's Sarcoma: AIDS Malignancy Consortium Trial 059. J Acquir Immune Defic Syndr. 2016 May 1;72(1):52-7. doi: 10.1097/QAI.0000000000000918. PubMed PMID: 26689971; PubMed Central PMCID: PMC4838493.
4: Mizukoshi Y, Takeuchi K, Arutaki M, Takizawa T, Hanzawa H, Takahashi H, Shimada I. Suppression of problematic compound oligomerization by cosolubilization of nondetergent sulfobetaines. ChemMedChem. 2015 Apr;10(4):736-41. doi: 10.1002/cmdc.201500057. PubMed PMID: 25760302; PubMed Central PMCID: PMC4471626.
5: Packer RJ, Rood BR, Turner DC, Stewart CF, Fisher M, Smith C, Young-Pouissant T, Goldman S, Lulla R, Banerjee A, Pollack I, Kun L, Onar-Thomas A, Wu S, Boyett JM, Fouladi M. Phase I and pharmacokinetic trial of PTC299 in pediatric patients with refractory or recurrent central nervous system tumors: a PBTC study. J Neurooncol. 2015 Jan;121(1):217-24. doi: 10.1007/s11060-014-1665-1. PubMed PMID: 25407389; PubMed Central PMCID: PMC4330963.
6: Poulsen JN, Larsen F, Duroux M, Gazerani P. Primary culture of trigeminal satellite glial cells: a cell-based platform to study morphology and function of peripheral glia. Int J Physiol Pathophysiol Pharmacol. 2014 Mar 13;6(1):1-12. PubMed PMID: 24665354; PubMed Central PMCID: PMC3961097.
7: Parker LJ, Taruya S, Tsuganezawa K, Ogawa N, Mikuni J, Honda K, Tomabechi Y, Handa N, Shirouzu M, Yokoyama S, Tanaka A. Kinase crystal identification and ATP-competitive inhibitor screening using the fluorescent ligand SKF86002. Acta Crystallogr D Biol Crystallogr. 2014 Feb;70(Pt 2):392-404. doi: 10.1107/S1399004713028654. PubMed PMID: 24531473.
8: Yokoyama K, Hiyama A, Arai F, Nukaga T, Sakai D, Mochida J. C-Fos regulation by the MAPK and PKC pathways in intervertebral disc cells. PLoS One. 2013 Sep 2;8(9):e73210. doi: 10.1371/journal.pone.0073210. PubMed PMID: 24023832; PubMed Central PMCID: PMC3759433.
9: Oh PS, Lim KT. Anti-inflammatory effect of glycoprotein isolated from Cudrania tricuspidata Bureau: involvement of MAPK/NF-κB signaling. Immunol Invest. 2011;40(1):76-91. doi: 10.3109/08820139.2010.516049. PubMed PMID: 20923328.
10: Oh PS, Lim KT. IgE, COX-2, and IL-4 are expressed by DEHP through p38 MAPK and suppressed by plant glycoprotein (75 kDa) in ICR mice. Inflammation. 2011 Oct;34(5):326-34. doi: 10.1007/s10753-010-9238-8. PubMed PMID: 20686831.
11: Santén S, Mihaescu A, Laschke MW, Menger MD, Wang Y, Jeppsson B, Thorlacius H. p38 MAPK regulates ischemia-reperfusion-induced recruitment of leukocytes in the colon. Surgery. 2009 Mar;145(3):303-12. doi: 10.1016/j.surg.2008.10.011. PubMed PMID: 19231583.
12: Tsirigotis M, Baldwin RM, Tang MY, Lorimer IA, Gray DA. Activation of p38MAPK contributes to expanded polyglutamine-induced cytotoxicity. PLoS One. 2008 May 7;3(5):e2130. doi: 10.1371/journal.pone.0002130. PubMed PMID: 18461158; PubMed Central PMCID: PMC2330164.
13: Lee SJ, Lim KT. Phytoglycoprotein inhibits interleukin-1beta and interleukin-6 via p38 mitogen-activated protein kinase in lipopolysaccharide-stimulated RAW 264.7 cells. Naunyn Schmiedebergs Arch Pharmacol. 2008 Mar;377(1):45-54. doi: 10.1007/s00210-007-0253-8. PubMed PMID: 18204996.
14: Gomez-Lazaro M, Galindo MF, Concannon CG, Segura MF, Fernandez-Gomez FJ, Llecha N, Comella JX, Prehn JH, Jordan J. 6-Hydroxydopamine activates the mitochondrial apoptosis pathway through p38 MAPK-mediated, p53-independent activation of Bax and PUMA. J Neurochem. 2008 Mar;104(6):1599-612. PubMed PMID: 17996028.
15: Gomez-Lazaro M, Galindo MF, Melero-Fernandez de Mera RM, Fernandez-Gómez FJ, Concannon CG, Segura MF, Comella JX, Prehn JH, Jordan J. Reactive oxygen species and p38 mitogen-activated protein kinase activate Bax to induce mitochondrial cytochrome c release and apoptosis in response to malonate. Mol Pharmacol. 2007 Mar;71(3):736-43. PubMed PMID: 17172466.
16: Tu Y, Perdue MH. CD23-mediated transport of IgE/immune complexes across human intestinal epithelium: role of p38 MAPK. Am J Physiol Gastrointest Liver Physiol. 2006 Sep;291(3):G532-8. PubMed PMID: 16899715.
17: Ateghang B, Wartenberg M, Gassmann M, Sauer H. Regulation of cardiotrophin-1 expression in mouse embryonic stem cells by HIF-1alpha and intracellular reactive oxygen species. J Cell Sci. 2006 Mar 15;119(Pt 6):1043-52. PubMed PMID: 16507596.
18: Nofer JR, Noll C, Feuerborn R, Assmann G, Tepel M. Low density lipoproteins inhibit the Na+/H+ antiport in human platelets via activation of p38MAP kinase. Biochem Biophys Res Commun. 2006 Feb 17;340(3):751-7. PubMed PMID: 16380078.
19: Baldwin RM, Garratt-Lalonde M, Parolin DA, Krzyzanowski PM, Andrade MA, Lorimer IA. Protection of glioblastoma cells from cisplatin cytotoxicity via protein kinase Ciota-mediated attenuation of p38 MAP kinase signaling. Oncogene. 2006 May 11;25(20):2909-19. PubMed PMID: 16331246.
20: Wagner G, Laufer S. Small molecular anti-cytokine agents. Med Res Rev. 2006 Jan;26(1):1-62. Review. PubMed PMID: 16283677.
