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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C18H18N2O4S2
CAS Number:
314042-01-8
Molecular Weight:
390.48
UNSPSC Code:
12352200
NACRES:
NA.32
MDL number:
MFCD01557530
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, protect from light

Key Documents

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form

powder

potency

12.89-19.70 nM Ki

InChI key

ATSWBWHRHAQVFM-UHFFFAOYSA-N

SMILES string

O=C(C1=C(NC(NC(C2=CC=CC=C2)=O)=S)SC3=C1CC(C)(C)OC3)O

assay

≥98% (HPLC)

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

Quality Level

100

Related Categories

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Natalia R Roque et al.
Biochimica et biophysica acta. Molecular and cell biology of lipids, 1865(8), 158703-158703 (2020-04-02)
Lipid droplets (LDs) are organelles that have multiple roles in inflammatory and infectious diseases. LD act as essential platforms for immunometabolic regulation, including as sites for lipid storage and metabolism, inflammatory lipid mediator production, and signaling pathway compartmentalization. Accumulating evidence

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