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

506121
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₃H₂₁FN₄S 581098-48-8

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      506121-1MG
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          Plastic ampoule 1 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          506121

          References

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

          Brochure

          Title
          DNA Repair Pathway Poster
          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.