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.