345885
GGTI-2147
≥95% (HPLC), solid, GGTase I inhibitor, Calbiochem®
别名:
GGTI-2147, 4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester
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关于此项目
经验公式（希尔记法）:
C28H30N4O3
化学文摘社编号:
分子量:
470.56
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
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
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
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.
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)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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