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Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C18H18N2O4S2
CAS Number:
314042-01-8
Molecular Weight:
390.48
MDL number:
MFCD01557530
UNSPSC Code:
12352200
NACRES:
NA.32

Quality Level

100

assay

≥98% (HPLC)

form

powder

potency

12.89-19.70 nM Ki

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

General description

A thiourea-derived small molecule that acts as a competitive inhibitor of nucleotide (BODIPY-GTP and BODIPY-GDP) binding by Rab7 (Ki = 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

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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