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Merck

345885

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
MDL number:
MFCD22581512
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).

InChI key

TUQRZGWNDBXSNP-SANMLTNESA-N

SMILES string

[nH]1cnc(c1)CNc2cc(c(cc2)C(=O)N[C@@H](CC(C)C)C(=O)OC)c3c4c(ccc3)cccc4

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

Quality Level

100

Related Categories

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

Disclaimer

Toxicity: Standard Handling (A)

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).

Other Notes

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

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.

Legal Information

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

Storage Class

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’.

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