Ggti 2133

Manufactured by Merck Group

Sourced in United States

GGTI-2133 is a chemical compound that functions as a Geranylgeranyltransferase I (GGTase I) inhibitor. It is used in laboratory research settings to study cellular processes involving protein prenylation.

Automatically generated - may contain errors

Lab products found in correlation

13 protocols using ggti 2133

Antibody Characterization in Cell Lines

Check if the same lab product or an alternative is used in the 5 most similar protocols

GGTI-2133, FTI-277, and zaragozic acid were purchased from Sigma. Antibodies (Abs) used in this study were: anti-β-tubulin III (Tuj-1, Covance, MMS-435P), anti-sarcomeric α-actinin (Abcam, ab9465), anti-GAPDH (Millipore, MAB374), anti-synaptophysin (Invitrogen, 18–0130), anti-NF68 (Sigma, N5139), anti-Lamin B1 (Abcam, ab16048) and anti-MYC (Santa Cruz, sc-40). All antibodies were used in 1:1000 dilution.

Okamoto-Uchida Y., Yu R., Miyamura N., Arima N., Ishigami-Yuasa M., Kagechika H., Yoshida S., Hosoya T., Nawa M., Kasama T., Asaoka Y., Alois R.W., Elling U., Penninger J.M., Nishina S., Azuma N, & Nishina H. (2016). The mevalonate pathway regulates primitive streak formation via protein farnesylation. Scientific Reports, 6, 37697.

+ Open protocol

+ Expand

Inhibition of Geranylgeranylation in Cells

Cited 1 time

Check if the same lab product or an alternative is used in the 5 most similar protocols

Brefeldin A and GGTI-2133 were obtained from Sigma-Aldrich (St Louis, MO, USA). Professor David Wiemer at the University of Iowa kindly provided the GGDPSi VSW1198 [8 (link)] and RAM2061 [10 (link)], as well as the GGTase II inhibitor NHB2005 [31 (link)].

Haney S.L., Varney M.L., Chhonker Y.S., Shin S., Mehla K., Crawford A.J., Smith H.J., Smith L.M., Murry D.J., Hollingsworth M.A, & Holstein S.A. (2019). Inhibition of geranylgeranyl diphosphate synthase is a novel therapeutic strategy for pancreatic ductal adenocarcinoma. Oncogene, 38(26), 5308-5320.

+ Open protocol

+ Expand

Inhibition of Geranylgeranylation in Cells

Cited 1 time

Check if the same lab product or an alternative is used in the 5 most similar protocols

+ Open protocol

+ Expand

Geranylgeranyl Transferase-I Inhibitor Assay

Check if the same lab product or an alternative is used in the 5 most similar protocols

GGTase-I was obtained from Jena Bioscience (Jena, Germany) and D*-GCVLL (dansyl gly-cys-val-leu-leu) from Calbiochem (Darmstadt, Germany). Ammonium hydroxide solution 28–30% was purchased from Alfa Aesar (Karlsruhe, Germany), the phosphatase inhibitors Halt® and Phosstop® from Thermo-Fisher/Piercenet (Bonn, Germany) and Roche Diagnostics GmbH (Mannheim, Germany) and the GGTase-I inhibitor GGTI-2133 from Sigma Aldrich (Schnelldorf, Germany). All solvents were of analytical grade or higher quality. Acetonitrile was obtained from Carl Roth GmbH (Karlsruhe, Germany), 1-butanol, n-hexane, 2-propanol, methanol, acetone, ammonium acetate and assay buffer compounds: Tris–HCl, MgCl₂, ZnCl₂ and Na₂CO₃ were obtained from Merck (Darmstadt, Germany). GGPP, octyl- -Dglucopyranoside and dithiothreitol were from Sigma-Aldrich (Schnelldorf, Germany). Millipore water was used for all solutions (Schwalbach, Germany).

Afshordel S., Wood W.G., Igbavboa U., Muller W.E, & Eckert G.P. (2014). Impaired Geranylgeranyltransferase-I Regulation Reduces Membrane-Associated Rho-Protein Levels in Aged Mouse Brain. Journal of neurochemistry, 129(4), 732-742.

+ Open protocol

+ Expand

Compound Preparation for Experimental Studies

Check if the same lab product or an alternative is used in the 5 most similar protocols

Pitavastatin (Livalo, Adooq), zoledronic acid and risedronate (Selleck), and GGTI-2133, Tipifarnib, farnesol, geranylgeraniol and mevalonate (Sigma-Aldrich) were prepared as 20 mM solutions in DMSO except zoledronic acid which was dissolved in H₂O.

Abdullah M.I., Abed M.N, & Richardson A. (2017). Inhibition of the mevalonate pathway augments the activity of pitavastatin against ovarian cancer cells. Scientific Reports, 7, 8090.

+ Open protocol

+ Expand

Pharmacological Interventions in Cell Modeling

Cited 1 time

Check if the same lab product or an alternative is used in the 5 most similar protocols

The drugs employed in this study were FTI-277, Pravastatin, Zoledronic acid, Rapamycin, Insulin-like growth factor 1, N-acetyl-l-cysteine and GGTI-2133 and were all obtained from Sigma Aldrich, UK. Drugs were added to the media and incubated for fixed periods of time. The final concentration and duration of drug treatments were: FTI-277—2.5 µM for 48 h (Mehta et al. 2011 (link)), Pravastatin—1 µM for 24 h (Varela et al. 2008 (link)), Zoledronic acid—1 µM for 24 h, Rapamycin—10 nM for 24 h (Cao et al. 2011b ), Insulin-like growth factor 1—50.0 ng/mL for 24 h (Mariño et al. 2010 (link)), N-acetyl-l-cysteine—20 µM for 1 h (Richards et al. 2011 (link)), FTI-277 and GGTI-2133—both 2.5 µM for 48 h) (Mehta et al. 2011 (link); Kieran et al. 2007 (link)), Pravastatin and Zoledronic acid—both 1 µM for 24 h (Varela et al. 2008 (link)) and FTI-277—2.5 µM for 48 h, Pravastatin and Zoledronic acid—both 1 µM for 24 h.

Bikkul M.U., Clements C.S., Godwin L.S., Goldberg M.W., Kill I.R, & Bridger J.M. (2018). Farnesyltransferase inhibitor and rapamycin correct aberrant genome organisation and decrease DNA damage respectively, in Hutchinson–Gilford progeria syndrome fibroblasts. Biogerontology, 19(6), 579-602.

+ Open protocol

+ Expand

Investigating Chemokine-mediated Cell Signaling

Check if the same lab product or an alternative is used in the 5 most similar protocols

Recombinant human CXCL1 (275-GR-010, R&D Systems), recombinant human CXCL2 (276-GB-010, R&D Systems), recombinant human CXCL8 (208-IL-010, R&D Systems), recombinant mouse Ccl2 (479-JE-010, R&D Systems), recombinant mouse Ccl7 (456-MC-010, R&D Systems), GGTI-2133 (G5294, Sigma-Aldrich), FTI-277 (F9803, Sigma-Aldrich), YM-53601 (18113, Cayman Chemical), simvastatin (S1792, Selleckchem), and human cholesterol (C8667, Sigma-Aldrich).

Han B., Alonso-Valenteen F., Wang Z., Deng N., Lee T.Y., Gao B., Zhang Y., Xu Y., Zhang X., Billet S., Fan X., Shiao S., Bhowmick N., Medina-Kauwe L., Giuliano A, & Cui X. (2021). A chemokine regulatory loop induces cholesterol synthesis in lung-colonizing triple-negative breast cancer cells to fuel metastatic growth. Molecular Therapy, 30(2), 672-687.

+ Open protocol

+ Expand

Signaling Pathways Modulation Assay

Check if the same lab product or an alternative is used in the 5 most similar protocols

EGCG, luteolin, GGTI-2133, and TGF-β recombinant protein were obtained from Sigma Aldrich. Other materials include U0126 (Calbiochem) and LY294002 (Enzo Life Sciences, Inc.).

Gray A.L., Stephens C.A., Bigelow R.L., Coleman D.T, & Cardelli J.A. (2014). The Polyphenols (−)-Epigallocatechin-3-Gallate and Luteolin Synergistically Inhibit TGF-β-Induced Myofibroblast Phenotypes through RhoA and ERK Inhibition. PLoS ONE, 9(10), e109208.

+ Open protocol

+ Expand

Synthesis and Characterization of GGTI Inhibitors

Cited 1 time

Check if the same lab product or an alternative is used in the 5 most similar protocols

GGTI-2133 was obtained from Sigma-Aldrich (St Louis, MO, USA). NHB2005 and RAM2061 were kindly provided by Dr. David Wiemer at the University of Iowa (Coxon et al., 2014 (link); Matthiesen et al., 2018 (link)). Compound purity was determined as ≥95% by high-performance liquid chromatography and verified by nuclear magnetic resonance (Matthiesen et al., 2018 (link)). Structures of the compounds used in this study can be found in Supplemental Fig 1.

Haney S.L., Feng D., Chhonker Y.S., Varney M.L., Williams J.T., Smith L.M., Ford J.B., Murry D.J, & Holstein S.A. (2022). Evaluation of geranylgeranyl diphosphate synthase inhibition as a novel strategy for the treatment of osteosarcoma and Ewing sarcoma. Drug development research, 84(1), 62-74.

+ Open protocol

+ Expand

Regulating Cholesterol Metabolism and Cell Cycle

Check if the same lab product or an alternative is used in the 5 most similar protocols

The reagents used and working concentrations were as follows: Nutlin-3 (10 μM, Sigma-Aldrich, catalog #N6287), LG100268 (Sigma-Aldrich, catalog #SML0279), T0901317 (Sigma-Aldrich, catalog #T2320), 25-hydroxycholesterol (1 μg/ml, Santa Cruz Biotechnology, catalog #sc-214091), N-Acetyl-Leucyl-Leucyl-norleucinal (ALLN, 100 μM, Sigma-Aldrich, catalog #A6185), Simvastatin (10 μM, Sigma-Aldrich, catalog #S6196), mevalonic acid 5-phosphate (1 mM, Sigma-Aldrich, catalog #79849), geranylgeranyl pyrophosphate (10 μM, Sigma-Aldrich, catalog #G6025), GGTI-2133 (20 μM, Sigma-Aldrich, catalog #G5294), Palbociclib (500 nM, Selleck Chemicals, catalog #S1116) and Roscovitine (10 μM, Selleck Chemicals, catalog #S1153).

Moon S.H., Huang C.H., Houlihan S.L., Regunath K., Freed-Pastor W.A., Morris JP I.V., Tschaharganeh D.F., Kastenhuber E.R., Barsotti A.M., Culp-Hill R., Xue W., Ho Y.J., Baslan T., Li X., Mayle A., de Stanchina E., Zender L., Tong D.R., D’Alessandro A., Lowe S.W, & Prives C. (2018). p53 Represses the Mevalonate Pathway to Mediate Tumor Suppression. Cell, 176(3), 564-580.e19.

+ Open protocol

+ Expand

About PubCompare

Our mission is to provide scientists with the largest repository of trustworthy protocols and intelligent analytical tools, thereby offering them extensive information to design robust protocols aimed at minimizing the risk of failures.

We believe that the most crucial aspect is to grant scientists access to a wide range of reliable sources and new useful tools that surpass human capabilities.

However, we trust in allowing scientists to determine how to construct their own protocols based on this information, as they are the experts in their field.

Ready to get started?

Revolutionizing how scientists
search and build protocols!