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506121 p38 MAP Kinase Inhibitor III - CAS 581098-48-8 - Calbiochem

506121
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
581098-48-8C₂₃H₂₁FN₄S

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506121-1MG
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      Description
      OverviewA cell-permeable methylsulfanylimidazole compound that acts as a potent, selective, reversible, and ATP-competitive p38 MAP kinase inhibitor (IC50 = 0.38 µM for p38α). Shown to effectively suppresses LPS-induced cytokine release both in vitro (IC50 = 0.16 and 0.039 µM for TNF-α and IL-1β release, respectively, in human PBMC) and in vivo (ED50 = 1.33 mg/kg for TNF-α release in mouse). When compared with SB 203580 (Cat. No. 559389 and 559398), it exhibits reduced inhibitory activity against cytochrome P450-2D6 isoform and, therefore, is better suited for in vivo use. A 10 mM (1 mg/247 µl) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506148) in DMSO is also available.
      Catalogue Number506121
      Brand Family Calbiochem®
      SynonymsML3403, (RS)-{4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]pyridin-2-yl}-(1-phenylethyl)amine]
      References
      ReferencesLaufer, S.A., et al. 2003. J. Med. Chem. 46, 3230.
      Product Information
      CAS number581098-48-8
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₂₃H₂₁FN₄S
      Chemical formulaC₂₃H₂₁FN₄S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetp38 MAP kinase
      Primary Target IC<sub>50</sub>0.38 µM for p38 MAP kinase α; 0.16 and 0.039 µM in suppressing LPS-induced TNF-α and IL-1β release, respectively, in human PBMC
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Carcinogenic / Teratogenic
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      p38 MAP Kinase Inhibitor III - CAS 581098-48-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      p38 MAP Kinase Inhibitor III - CAS 581098-48-8 - Calbiochem Certificates of Analysis

      TitleLot Number
      506121

      References

      Reference overview
      Laufer, S.A., et al. 2003. J. Med. Chem. 46, 3230.

      Brochure

      Title
      MAPK Pathway Poster ( 750 KB )
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision15-April-2010 RFH
      SynonymsML3403, (RS)-{4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]pyridin-2-yl}-(1-phenylethyl)amine]
      DescriptionA cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of p38 MAP kinase (IC50 = 380 nM for p38α). Shown to effectively suppress LPS-induced cytokine release in vitro (IC50 = 160 nM for TNF-α release and 39 nM for IL-1β release, human PBMC) and in vivo (ED50 = 1.33 mg/kg for TNF-α release in mice). Exhibits reduced inhibitory activity against cytochrome P450-2D6 compared to SB 203580 (Cat. No 559389) and is better suited for use in animal models.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number581098-48-8
      Chemical formulaC₂₃H₂₁FN₄S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Carcinogenic / Teratogenic
      ReferencesLaufer, S.A., et al. 2003. J. Med. Chem. 46, 3230.