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Sigma-Aldrich

Rac1 Inhibitor V

Synonym(e):

Rac1 Inhibitor V, 3-(2-Hydroxyphenyl)-N-(4-(1-piperidinylsulfonyl)phenyl)-1H-pyrazole-5-carboxamide, TCMDC-124310

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About This Item

Empirische Formel (Hill-System):
C21H22N4O4S
CAS-Nummer:
Molekulargewicht:
426.49
UNSPSC-Code:
12352200
PubChem Substanz-ID:
NACRES:
NA.77
Preise und Verfügbarkeit sind derzeit nicht verfügbar.

Assay

≥95% (HPLC)

Qualitätsniveau

Form

powder

Hersteller/Markenname

Calbiochem®

Lagerbedingungen

OK to freeze
protect from light

Farbe

beige

Löslichkeit

DMSO: 100 mg/mL

Lagertemp.

2-8°C

SMILES String

CC(C)CNC1=NC(=NC=C1)NCC2=CSC(=N2)C3=CC=CC=C3

Allgemeine Beschreibung

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.
A 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.

Biochem./physiol. Wirkung

Cell permeable: yes
Primary Target
Rac
Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Sonstige Hinweise

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

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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