GGTI-2418

GGTI-2418

• CAS Number: 501010-06-6
• UNSPSC Description: GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors[1].
• Target Antigen: Apoptosis
• Type: Reference compound
• Related Pathways: Apoptosis
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/ggti-2418.html
• Solubility: DMSO : 125 mg/mL (ultrasonic)
• Smiles: CC(C)C[C@@H](C(O)=O)NC(N1[C@@H](CC2=CC=CC=C2)C(N(CC3=C(C)N=CN3)CC1)=O)=O
• Molecular Weight: 441.52
• References & Citations: [1]Kazi A, et al. Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: implications for breast cancer therapy. Mol Cell Biol. 2009 Apr;29(8):2254-63.|[2]Kuchay S, et al. PTEN counteracts FBXL2 to promote IP3R3- and Ca²⁺-mediated apoptosis limiting tumour growth. Nature. 2017 Jun 22;546(7659):554-558.
• Shipping Conditions: Room Temperature
• Clinical Information: Phase 1