CAS 1217480-14-2

GGTI-2133

CAS: 1217480-14-2

GGTI-2133 is a chemokine that has been shown to be a potent autophagy inducer. Autophagy is the process by which cells break down and recycle their own components in order to maintain homeostasis. GGTI-2133 has been shown to inhibit cholesterol synthesis, decrease lung damage, and induce bronchial dilation. The drug has also been shown to increase the production of geranylgeranylated proteins, which may have therapeutic potential for cancer treatment. A molecular modeling study of GGTI-2133 shows that it binds to the same binding site as statins on HMG-CoA reductase, an enzyme involved in cholesterol synthesis. This may lead to synergistic effects when taken with statins for the treatment of cardiovascular disease and diabetes mellitus type II.

Formula: C₂₉H₂₉F₃N₄O₅

Purity: Min. 95%

Molecular weight: 570.6 g/mol

Ref: 3D-SYB48014

GGTI 2133 TFA

CAS: 1217480-14-2

GGTI 2133, a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50= 38 nM), exhibits 140-fold selectivity towards GGTase I compared to farnesyltransferase (IC50= 5,400 nM). The compound effectively inhibits the geranylgeranylation of RAP1A (IC50= 10 µM) without affecting the farnesylation of H-Ras (IC50= >30 µM). Moreover, GGTI 2133 reduces the growth, migration, and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control levels, respectively. When administered intraperitoneally at 5 mg/kg per day, it prevents eosinophil infiltration into the airways in a mouse model of allergic bronchial asthma, although it does not reduce chemokine levels. Additionally, GGTI 2133 thwarts naloxone-induced contraction of ileum in rats experiencing morphine withdrawal syndrome and mitigates the severity of withdrawal symptoms in vivo (ED50= 0.076 mg/kg).

Formula: C₂₉H₂₉F₃N₄O₅

Color and Shape: Solid

Molecular weight: 570.569

Ref: TM-T85180