GGTI-2133

SKU: orb1703426

Description

GGTI-2133 is a potent and selective peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase-I), exhibiting an IC50 of 38 nM. This compound has been shown to reduce inflammatory cell infiltration in murine models of asthma, supporting its use in researching protein prenylation, cell signaling, and inflammatory diseases in both in vitro and in vivo contexts.

Research Area

Metabolism Research

Key Properties

• CAS Number: 191102-79-1
• MW: 456.54
• Purity: 99.80% (May vary between batches)
• Formula: C₂₇H₂₈N₄O₃
• SMILES: C(N[C@@H](CC(C)C)C(O)=O)(=O)C1=C(C=2C3=C(C=CC2)C=CC=C3)C=C(NCC4=CN=CN4)C=C1
• Target: Others,Transferase
• Solubility: DMSO:50 mg/mL (109.52 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.38 mM)

Bioactivity

• In Vivo:
  Animals also were treated with GGTI-2133 (5 mg/kg; i.p.; once a day; mice with experimental asthma) during the antigen inhalation period. Repeated antigen inhalation caused a BSM hyperresponsiveness to acetylcholine with the increased expressions of RhoA and the anti-farnesyl-positive 21-kDa proteins, probably geranylgeranylated RhoA. The in vivo GGTI-2133 treatments significantly inhibited BSM hyperresponsiveness induced by antigen exposure.
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• In Vitro:
  BSM tissues isolated from the repeatedly antigen-challenged mice were cultured for 48 h in the absence or presence of GGTI-2133. Under these conditions, the putative geranylgeranylated RhoA was decreased in a GGTI-2133 concentration-dependent manner. The in vitro incubation with GGTI-2133 also inhibited BSM hyperresponsiveness induced by antigen exposure. These findings suggest that GGTI-2133 inhibits antigen-induced BSM hyperresponsiveness, probably by reducing downstream signal transduction of RhoA.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GGTase I, GGTI 2133, GGTI2133, GGTI-2133

Compound Identifiers

PubChem CID

9846868