GGTI298
GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
Product Specifications
CAS Number
180977-44-0
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis
Type
Reference compound
Related Pathways
Apoptosis
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/GGTI298.html
Purity
85.0
Solubility
10 mM in DMSO|10 mM in H2O
Smiles
CC(C)C[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O
Molecular Formula
C27H33N3O3S
Molecular Weight
479.63
Precautions
H302, H315, H319, H335
References & Citations
[1]Sheikh IA, et al. The Epac1 signaling pathway regulates Cl- secretion via modulation of apical KCNN4c channels in diarrhea. J Biol Chem. 2013 Jul 12;288 (28) :20404-15|[2]Chen S, et al. Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis. Mol Cancer. 2010 Jan 29;9:23.|[3]McGuire TF, et al. Platelet-derived growth factor receptor tyrosine phosphorylation requires protein geranylgeranylation but not farnesylation. J Biol Chem. 1996 Nov 1;271 (44) :27402-7.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Citation 01
Int Immunopharmacol. 2023 Apr:117:110014.|Arthritis Res Ther. 2024 Dec 19;26 (1) :222.|J Neuroinflammation. 2024 Nov 14;21 (1) :295.|J Oral Biosci. 2023 Dec;65 (4) :347-355.|Mol Cell Proteomics. 2023 Aug;22 (8) :100593.|Nat Commun. 2025 Nov 21;16 (1) :10263.
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