GGTI-2154 (hydrochloride)

GGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 hydrochloride shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM) . GGTI-2154 hydrochloride can be used for the research of cancer[1][2].

Product Specifications

CAS Number

[478908-50-8]

UNSPSC

12352005

Target

Apoptosis; GGTase

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ggti-2154-hydrochloride.html

Purity

98.93

Solubility

DMSO : 250 mg/mL (ultrasonic) |H2O : 4.76 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CN=CN2)C=C1C3=CC=CC=C3C)=O.[H]Cl

Molecular Formula

C24H29ClN4O3

Molecular Weight

456.97

References & Citations

[1]Sun J, et, al. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 1999 Oct 1;59 (19) :4919-26.|[2]Sun J, et, al. Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice. Cancer Res. 2003 Dec 15;63 (24) :8922-9.