530820 Rac1 Inhibitor V - Calbiochem

530820
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₁H₂₂N₄O₄S

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30820.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable {piperidinylsulfonylphenyl}-pyrazolocarboxamide compound that inhibits celluar Rac-GTP level upon PDGF-BB stimulation (Cat. No. 521225) in serum-starved human vascular smooth muscle cell (SMC) A617 with a higher potency (IC50 = 8.7 µM; 4 h drug preincubation) than Z62954982 (Cat. Nos. 553511 & 553512; 37% inhibition at 50 µM) via a similar mode of action as NSC23766 (Cat. Nos. 553502 & 553508), exhibiting no potency against cellular RhoA-GTP level even at a high concentration of 25 µM. Effectively inhibits SMC adhesion and PDGF-BB-stimulated lamellipodia formation of starved A617 cells. Effectively inhibits Rac activation mediated by Rac-specific Tiam-1 & TrioN GEF as well as non-Rac-specific GEF Vav2, while EHop-016 (Cat. No. 553513) is selective against Vav2- over Tiam-1-mediated Rac activation.
          Catalogue Number530820
          Brand Family Calbiochem®
          Synonyms3-(2-Hydroxyphenyl)-N-(4-(1-piperidinylsulfonyl)phenyl)-1H-pyrazole-5-carboxamide, TCMDC-124310
          References
          ReferencesFerri, N., et al. 2013. Med. Chem. Commun. 4, 537.
          Product Information
          FormBeige powder
          Hill FormulaC₂₁H₂₂N₄O₄S
          Chemical formulaC₂₁H₂₂N₄O₄S
          ReversibleY
          Applications
          Biological Information
          Primary TargetRac
          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 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

          Rac1 Inhibitor V - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Ferri, N., et al. 2013. Med. Chem. Commun. 4, 537.
          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.

          Revision19-August-2014 JSW
          Synonyms3-(2-Hydroxyphenyl)-N-(4-(1-piperidinylsulfonyl)phenyl)-1H-pyrazole-5-carboxamide, TCMDC-124310
          DescriptionA cell-permeable {piperidinylsulfonylphenyl}-pyrazolocarboxamide compound that inhibits celluar Rac-GTP level upon PDGF-BB stimulation (Cat. No. 521225; 20 ng/mL for 2 min) in 48 h 0.4% FCS-starved A617 human vascular smooth muscle cell (SMC) cultures with a higher potency (IC50 = 8.7 µM; 4 h drug preincubation) than Z62954982 (Cat. Nos. 553511 & 553512; 37% inhibition at 50 µM) via a similar mode of action as NSC23766 (Cat. Nos. 553502 & 553508), exhibiting no potency against cellular RhoA-GTP level even at a high concentration of 25 µM. Effectively inhibits SMC adhesion (IC50 = 8.7 µM post 4 h drug treatment) and PDGF-BB-stimulated lamellipodia formation (complete inhibition with 4 h 10 µM; drug treatment prior to 10 min 10 ng/mL PDGF-BB stimulation) of 48 h starved A617 cells. Effectively inhibits Rac activation mediated by Rac-specific Tiam-1 & TrioN GEF as well as non-Rac-specific GEF Vav2, while EHop-016 (Cat. No. 553513), in comparison, is selective against Vav2- over Tiam-1-mediated Rac activation.
          FormBeige powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₁H₂₂N₄O₄S
          Purity≥95% by HPLC
          SolubilityDMSO (100 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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesFerri, N., et al. 2013. Med. Chem. Commun. 4, 537.