| Company Name: |
Sigma-Aldrich
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021-61415566 800-8193336 |
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orderCN@merckgroup.com |
| Products Intro: |
Product Name:GGTI-2133
CAS:1217480-14-2
Purity:>=98% (HPLC), solid Package:1MG Remarks:G5294-1MG
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| Company Name: |
BOC Sciences
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| Tel: |
16314854226 |
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info@bocsci.com |
| Products Intro: |
Product Name:GGTI 2133 trifluoroacetate salt
CAS:1217480-14-2
Purity:95% Package:1G;10G;100G Remarks:GGTI 2133 is a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I) with an IC50 value of 38 nM, whch is 140-fold selective for GGTase I over farnesyltransferase (IC50 = 5,400 nM).
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| Company Name: |
Shanghai Yifei Biotechnology Co. , Ltd.
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| Tel: |
021-65675885 18964387627 |
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customer_service@efebio.com |
| Products Intro: |
Product Name:GGTI 2133 (trifluoroacetate salt)
CAS:1217480-14-2
Purity:95% Package:500μg;1mg
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| Company Name: |
Cayman Chemical Company
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| Tel: |
(800) 364-9897 |
| Email: |
cayman@caymanchem.com |
| Products Intro: |
Product Name:GGTI 2133 (trifluoroacetate salt)
CAS:1217480-14-2
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| | GGTI 2133 (trifluoroacetate salt) Basic information |
| | GGTI 2133 (trifluoroacetate salt) Chemical Properties |
| Melting point | 103-118.5 °C | | storage temp. | -20°C | | solubility | DMSO: 25 mg/ml | | form | A crystalline solid |
| | GGTI 2133 (trifluoroacetate salt) Usage And Synthesis |
| Description | GGTI 2133 is a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50 = 38 nM). It is 140-fold selective for GGTase I over farnesyltransferase (IC50 = 5,400 nM). In vitro, it inhibits geranylgeranylation of RAP1A (IC50 = 10 μM) without inhibiting farnesylation of H-Ras (IC50 = >30 μM). It also inhibits cell growth and decreases migration and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control values, respectively. GGTI 2133 (5 mg/kg per day, i.p.) prevents ovalbumin-induced eosinophil infiltration into airways in a mouse model of allergic bronchial asthma but does not prevent an increase in chemokines. It also blocks naloxone-induced contraction of ileum isolated from rats with morphine withdrawal syndrome and dose-dependently decreases withdrawal severity in vivo (ED50 = 0.076 mg/kg). | | Uses | 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.
| | Biochem/physiol Actions | 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 (trifluoroacetate salt) Preparation Products And Raw materials |
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