553326

Ras Superfamily GTPases GTP/GDP Binding Antagonist, CID 1067700

The Ras Superfamily GTPases GTP/GDP Binding Antagonist, CID 1067700 controls the biological activity of Rab7. This small molecule/inhibitor is primarily used for Membrane applications.

• Synonyme(s) : Ras Superfamily GTPases GTP/GDP Binding Antagonist, CID 1067700, 2-(benzoylcarbamothioylamino)-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic acid, CID1067700, Cdc42 GTPase Inhibitor I, Rab2 GTPase Inhibitor, Rab GTPase Inhibitor, CDC42 Inhibitor I, Rab7 GTPase Inhibitor, Rac1 GTPase Inhibitor, Rac1 Inhibitor, Rac1 GTPase Inhibitor, Rac1 Inhibitor IV, Ras GTPase Inhibitor, 2-(benzoylcarbamothioylamino)-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic acid, CID1067700, Cdc42 GTPase Inhibitor I, Rab2 GTPase Inhibitor, Rab GTPase Inhibitor, CDC42 Inhibitor I, Rab7 GTPase Inhibitor
• Formule empirique (notation de Hill): C₁₈H₁₈N₂O₄S₂
• Numéro CAS: 314042-01-8
• Poids moléculaire : 390.48
• Numéro MDL: MFCD01557530
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Puissance: 12.89-19.70 nM K_i
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: beige
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• Chaîne SMILES: O=C(C1=C(NC(NC(C2=CC=CC=C2)=O)=S)SC3=C1CC(C)(C)OC3)O

Description

Description générale

A thiourea-derived small molecule that acts as a competitive inhibitor of nucleotide (BODIPY-GTP and BODIPY-GDP) binding by Rab7 (K_i = 12.89-19.70 nM). Equilibrates rapidly with Rab7 without affecting the rate of release of bound BODIPY-GTP or BODIPY-GDP. However, it exhibits a slightly lower potency against BODIPY-GDP bound Rab7 than BODIPY-GTP bound Rab7A. Acts by binding to the nucleotide binding pocket of Rab7. Also shown to inhibit nucleotide binding by mutant forms of Rab7 (Rab7Q67L and Rab7T22N) that are constitutively in the GTP and GDP bound states, with good potency. Also shown to block the nucleotide binding of several other Ras-related GTPases, but with reduced potency.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Rab7

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Agola, J. O., et al. 2012. ACS Chem Bio.7, 1095.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable