345885

GGTI-2147

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

• Synonym(e): GGTI-2147, 4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester
• Empirische Formel (Hill-System): C₂₈H₃₀N₄O₃
• CAS-Nummer: 191102-87-1
• Molekulargewicht: 470.56
• MDL number: MFCD22581512
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, desiccated (hygroscopic)

Eigenschaften

• Produktname: GGTI-2147, A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I).
• Quality Segment: 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
• SMILES string: [nH]1cnc(c1)CNc2cc(c(cc2)C(=O)N[C@@H](CC(C)C)C(=O)OC)c3c4c(ccc3)cccc4
• InChI key: TUQRZGWNDBXSNP-SANMLTNESA-N

Beschreibung

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Was ist los?: WGK 1
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable