SKF86002
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MedKoo CAT#: 530341

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.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 2 Weeks
25mg USD 250 2 Weeks
50mg USD 450 2 Weeks
100mg USD 650 2 Weeks
200mg USD 950 2 Weeks
500mg USD 1650 2 Weeks
1g USD 2850 2 Weeks
2g USD 3950 2 Weeks
5g USD 6950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-27. Prices are subject to change without notice.

SKF-86002, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 530341
Name: SKF86002
CAS#: 72873-74-6
Chemical Formula: C16H12FN3S
Exact Mass: 297.0736
Molecular Weight: 297.3514
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


Technical Data

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


References

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.