Skip to Content
Merck
All Photos(1)

Key Documents

345885

Sigma-Aldrich

GGTI-2147

≥95% (HPLC), solid, GGTase I inhibitor, Calbiochem®

Synonym(s):

GGTI-2147, 4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester

Sign Into View Organizational & Contract Pricing


About This Item

Empirical Formula (Hill Notation):
C28H30N4O3
CAS Number:
Molecular Weight:
470.56
UNSPSC Code:
12352200
NACRES:
NA.77

product name

GGTI-2147, A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I).

Quality Level

Assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)

color

off-white

solubility

DMSO: 200 mg/mL

shipped in

ambient

storage temp.

−20°C

General description

A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I). Blocks the geranyl-geranylation of Rap1A with an IC50 value that is over 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC50 = 500 nM for Rap1A versus IC50 >30 µM for H-Ras).
Methyl ester derivative of GGTI-2133 (Cat. No. 345884). A potent and selective non-thiol inhibitor of geranylgeranyltransferase I (GGTase I) over farnesyltransferase (FTase) in whole cells. Blocks the geranylgeranylation of Rap1A with an IC50 value greater than 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC50 = 500 nM for Rap1A versus IC50<30 µM for H-Ras).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
GGTase-I
Product does not compete with ATP.
Reversible: no
Target IC50: 500 nM in blocking the geranyl-geranylation of Rap1A

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

Bernot, D., et al. 2003. J. Cardiovasc. Pharmacol.41, 316.
Vasudevan, A., et al. 1999. J. Med. Chem. 42, 1333.

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

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’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service