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GGTI298

GGTI298
GGTI298, a CAAZ peptidomimetic and potent geranylgeranyltransferase I (GGTase I) inhibitor, efficiently blocks the processing of geranylgeranylated Rap1A while exerting minimal impact on the processing of farnesylated Ha-Ras. The inhibitor displays in vivo IC50 values of 3 μM for Rap1A and >20 μM for Ha-Ras, respectively.
Catalog No. T11397Cas No. 180977-44-0
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GGTI298

Catalog No. T11397Cas No. 180977-44-0
GGTI298, a CAAZ peptidomimetic and potent geranylgeranyltransferase I (GGTase I) inhibitor, efficiently blocks the processing of geranylgeranylated Rap1A while exerting minimal impact on the processing of farnesylated Ha-Ras. The inhibitor displays in vivo IC50 values of 3 μM for Rap1A and >20 μM for Ha-Ras, respectively.
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Product Introduction

Bioactivity
Description
GGTI298, a CAAZ peptidomimetic and potent geranylgeranyltransferase I (GGTase I) inhibitor, efficiently blocks the processing of geranylgeranylated Rap1A while exerting minimal impact on the processing of farnesylated Ha-Ras. The inhibitor displays in vivo IC50 values of 3 μM for Rap1A and >20 μM for Ha-Ras, respectively.
Targets&IC50
Ha-Ras:> 20 μM , Rap1A:3 μM
In vitro
GGTI298/TRAIL activates NF-κB and inhibits Akt. knockdown of DR5, preventes GGTI298/TRAIL-induced IκBα and p-Akt reduction, suggesting that DR5 mediates reduction of IκBα and p-Akt induced by GGTI298/TRAIL. In contrast, DR4 knockdown further facilitates GGTI298/TRAIL-induced p-Akt reduction.Both RhoA inhibitor (GGTI298) and ROCK inhibitor (H1152) significantly reduce cAMP agonist-stimulated IK(ap), whereas the latter additionally reduces colocalization of KCNN4c with the apical membrane marker wheat germ agglutinin in T84WT cells.?Knockdown of DR4 abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 and TRAIL.
In vivo
The in vivo mouse ileal loop experiments demonstrate that TRAM-34, GGTI298, or H1152, when co-administered with cholera toxin, significantly reduce fluid accumulation in a dose-dependent manner.
Chemical Properties
Molecular Weight479.63
FormulaC27H33N3O3S
Cas No.180977-44-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (208.49 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0849 mL10.4247 mL20.8494 mL104.2470 mL
5 mM0.4170 mL2.0849 mL4.1699 mL20.8494 mL
10 mM0.2085 mL1.0425 mL2.0849 mL10.4247 mL
20 mM0.1042 mL0.5212 mL1.0425 mL5.2124 mL
50 mM0.0417 mL0.2085 mL0.4170 mL2.0849 mL
100 mM0.0208 mL0.1042 mL0.2085 mL1.0425 mL

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