Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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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 | Rap1A, in vivo:3 μM , Ha-Ras, in vivo:> 20 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. |
Molecular Weight | 479.63 |
Formula | C27H33N3O3S |
CAS No. | 180977-44-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (208.49 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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GGTI298 180977-44-0 Others GGTI 298 GGTI-298 inhibitor inhibit