1. Metabolic Enzyme/Protease
  2. GGTase
  3. GGTI-2133 TFA

GGTI-2133 TFA, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 TFA shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 TFA inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 TFA can be used for the study of eosinophilic airway inflammation such as asthma.

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GGTI-2133 TFA Chemical Structure

GGTI-2133 TFA Chemical Structure

CAS No. : 1217480-14-2

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Description

GGTI-2133 TFA, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 TFA shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 TFA inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 TFA can be used for the study of eosinophilic airway inflammation such as asthma[1][2].

In Vivo

GGTI-2133 (5 mg/kg; intraperitoneal injection; once a day; for 10 days) TFA inhibits infiltration of inflammatory cells into airways in mouse experimental asthma[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c mice (8 weeks of age) were actively sensitized byintraperitoneal injections of 8 ug ovalbumin with 2 mg Imject Alum on days 0 and 5[2].
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; once a day; for 10 days from Day 11 to Day 20
Result: Inhibited the antigen-induced eosinophil infiltration into airways almost completely.
Molecular Weight

570.56

Formula

C29H29F3N4O5

CAS No.
SMILES

CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CN=CN2)C=C1C3=C4C=CC=CC4=CC=C3)=O.O=C(O)C(F)(F)F

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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GGTI-2133 TFA Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GGTI-2133 TFA
Cat. No.:
HY-12369A
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