S-methyl-KE-298

  Cat. No.:  DC10713   Featured
Chemical Structure
143584-75-2
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Field of application
S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.
Cas No.: 143584-75-2
SMILES: CC1=CC=C(C=C1)C(=O)CC(CSC)C(=O)O
Formula: C13H16O3S
M.Wt: 252.33
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.
In Vitro: S-methyl-KE-298 is a methyl conjugate of deacetyl-KE-298 is plasma[1]. In vitro protein binding of KE-298 and its plasma metabolites, deacetyl-KE-298 (M-1) and S-methyl-KE-298 (M-2), is high in rat (>97%), dog (>89%) and human plasma (>99%), respectively[2]. KE-298 blocks this IL-1β-induced pro-MMP-2 activation and MT1-MMP expression, but does not affect IL-1β-induced tissue inhibitor of metalloproteinase-2 (TIMP-2) secretion from rheumatoid synovial cells. KE-298 inhibits MMP-1 production from rheumatoid arthritis (RA) synovial cells by affecting a transcription factor, AP-1. KE-298 inhibits the basal levels of MT1-MMP expression of unstimulated rheumatoid synovial cells[3].
References: [1]. Yoshida H, et al. Identification of metabolites of KE-298, a new antirheumatic drug, and its physiological properties in rats. Biol Pharm Bull. 1996 Mar;19(3):424-9. [2]. Endo H, et al. Stereoselectivity and species difference in plasma protein binding of KE-298 and its metabolites. Biol Pharm Bull. 2001 Jul;24(7):800-5. [3]. Honda S, et al. Expression of membrane-type 1 matrix metalloproteinase in rheumatoid synovial cells. Clin Exp Immunol. 2001 Oct;126(1):131-6.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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