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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

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About This Item

Empirical Formula (Hill Notation):
C28H30N4O3
CAS Number:
191102-87-1
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

100

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

wgk_germany

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’.

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