钛-2133

C₂₇H₂₈N₄O₃ · C₂HF₃O₂

570.56

MFCD07776925

24724491

NA.77

GGTI-2133 has been used

• To understand the role of geranylgeranyl transferase in the regulation of CXC chemokine production and neutrophil recruitment in the lung.
• To study the importance of geranylgeranylation in cell adhesion.
• To measure ligand-induced ADP-ribosylation factor 6 (Arf6) activation in breast cancer cells.

GGTase I mediates prenylation to induce the oncogenic functions of the Ras and Rho proteins. Thus, GGTase I inhibitors can be utilized as effective anticancer drugs. They are also useful in treating inflammation, atherosclerosis, multiple sclerosis and other diseases.
GGTI-2133 is a cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I; IC50 = 38 nM) with a 140-fold selectivity over farnesyltransferase (FTase; IC₅₀ = 5.4 μM).

100

≥98% (HPLC)

solid

white to beige

103-118.5 ℃

DMSO: 25 mg/mL
H₂O: insoluble

−20℃

OC(=O)C(F)(F)F.CC(C)C[C@H](NC(=O)c1ccc(NCc2c[nH]cn2)cc1-c3cccc4ccccc34)C(O)=O

1S/C27H28N4O3.C2HF3O2/c1-17(2)12-25(27(33)34)31-26(32)23-11-10-19(29-15-20-14-28-16-30-20)13-24(23)22-9-5-7-18-6-3-4-8-21(18)22;3-2(4,5)1(6)7/h3-11,13-14,16-17,25,29H,12,15H2,1-2H3,(H,28,30)(H,31,32)(H,33,34);(H,6,7)/t25-;/m0./s1

FXXUNOYBYJFSRB-UQIIZPHYSA-N

human ... FNTA(2339), PGGT1B(5229)

1, 5 mg in glass bottle

GHS07

Warning

H315 - H319 - H335

P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Respiratory system

11 - Combustible Solids

WGK 3

dust mask type N95 (US), Eyeshields, Gloves