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

530486
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₃H₉ClN₄O₃

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      Glass bottle 10 mg
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      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
      Quality LevelMQ100
      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

      p38 MAP Kinase Inhibitor XX, FGA-19 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      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.