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530820 Rac1 Inhibitor V - Calbiochem

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530820
  
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₁H₂₂N₄O₄S
Description
Overview

This product has been discontinued.



A 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
Global Trade Item Number
Catalogue Number GTIN
530820 0

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 Protect from light
+2°C to +8°C
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.