A part of MilliporeSigma

530486 | p38 MAP Kinase Inhibitor XX, FGA-19 - Calbiochem

530486
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₃H₉ClN₄O₃

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.30486.0001
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service

          Glass bottle 10 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          Description
          OverviewA cell-permeable, benzoxadiazole compound designed to target p38 c-terminal "docking domain" that mediates interactions with upstream regulators and downstream substrates outside p38 active center. Selectively inhibits MEF-2A phosphorylation by activated p38α (IC50 = 6.31 µM; [p38] = 1 nM, [MEF-2a] = 10 nM, [ATP] = 25 µM) with little or no potency against a panel of other kinases or the docking site interaction-independent MBP phosphorylation by p38. Shown to inhibit LPS-stimulated phosphorylation of p38, MK2, and Hsp27 in THP-1 cells (1 to 5 µM; 1 h drug preincubation), while reduced inhibition against JNK1 & Erk1/2 is only observed at a high concentration of 5 µM. Although SB203580 (Cat. Nos. 559389, 559395, and 559398) exhibits similar potency as FGA-19 in inhibiting LPS-induced TNFα secretion in THP-1 cultures in vitro, only FGA-19 (1 µg/5 µL/mouse), but not SB203580 (up to 5 µg/mouse), intrathecal injection results in lasting (>5 days) reduction of heat sensitivity of paws received carrageenan injection among either wild-type or LysM-GRK2+/- mice in vivo.
          Catalogue Number530486
          Brand Family Calbiochem®
          SynonymsN-(5-Chloro-2-methylphenyl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, FGA 19
          References
          ReferencesWillemen, H. L., et al. 2014. Biochem. J. 459, 427.
          Product Information
          FormOrange red powder
          Hill FormulaC₁₃H₉ClN₄O₃
          Chemical formulaC₁₃H₉ClN₄O₃
          ReversibleY
          Applications
          Biological Information
          Primary Targetp38 MAPK
          Primary Target IC<sub>50</sub>6.31 µM for p38 MAPK-mediated phosphorylation of MEF-2A-Thr312
          Purity≥98% 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 Ambient Temperature Only
          Toxicity Standard Handling
          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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          References

          Reference overview
          Willemen, H. L., et al. 2014. Biochem. J. 459, 427.
          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.

          Revision08-September-2014 JSW
          SynonymsN-(5-Chloro-2-methylphenyl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, FGA 19
          DescriptionA cell-permeble, benzoxadiazole compound designed to target p38 c-terminal "docking domain" that mediates interactions with upstream regulators and downstream substrates outside p38 active center. Selectively inhibits MEF-2A phosphorylation by activated p38α (IC50 = 6.31 µM; [p38] = 1 nM, [MEF-2a] = 10 nM, [ATP] = 25 µM) with little or no potency against a panel of other kinases or the docking site interaction-independent MBP phosphorylation by p38. Shown to inhibit LPS-stimulated phosphorylation of p38, MK2, and Hsp27 in THP-1 cells (1 to 5 µM; 1 h drug preincubation prior to 30 to 60 min LPS exposure), while reduced inhibition against JNK1 & Erk1/2 is only observed at a high concentration of 5 µM, indicating weaker potency in targeting JNK & Erk docking domain. Although SB203580 (Cat. Nos. 559389, 559395, and 559398) exhibits similar potency as FGA-19 in inhibiting LPS-induced TNFα secretion in THP-1 cultures in vitro, only FGA-19 (1 µg/5 µL/mouse), but not SB203580 (up to 5 µg/mouse), intrathecal injection results in lasting (>5 days) reduction of heat sensitivity of paws received carrageenan injection among either wild-type (6 d prior to drug treatment; 20 µL 2% carrageenan per paw) or LysM-GRK2+/- mice (5 µL 1% carrageenan per paw) in vivo.
          FormOrange red powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₃H₉ClN₄O₃
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
          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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesWillemen, H. L., et al. 2014. Biochem. J. 459, 427.