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.

• Synonym(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
• Empirical Formula (Hill Notation): C₁₈H₁₈N₂O₄S₂
• CAS Number: 314042-01-8
• Molecular Weight: 390.48
• MDL number: MFCD01557530
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• potency: 12.89-19.70 nM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: beige
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: O=C(C1=C(NC(NC(C2=CC=CC=C2)=O)=S)SC3=C1CC(C)(C)OC3)O

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Rab7

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable