345885
GGTI-2147
≥95% (HPLC), solid, GGTase I inhibitor, Calbiochem®
別名:
GGTI-2147, 4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester
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この商品について
実験式（ヒル表記法）:
C28H30N4O3
CAS番号:
分子量:
470.56
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic)
製品名
GGTI-2147, A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I).
Quality Segment
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
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)
保管分類
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
試験成績書（COA）
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