530820 Rac1 Inhibitor V - Calbiochem

530820
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₁H₂₂N₄O₄S

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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
      Quality LevelMQ100
      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.