N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT
GGTI-298
CAS: 180977-44-0
Molecular Formula: C27H33N3O3S
N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT - Names and Identifiers
N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT - Physico-chemical Properties
| Molecular Formula | C27H33N3O3S |
| Molar Mass | 479.63 |
| Melting Point | 99.5-100°C |
| Solubility | DMSO: 22mg/mL |
| Appearance | solid |
| Color | off-white |
| Storage Condition | −20°C |
| In vitro study | 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. 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. |
| In vivo study | The vivo mouse ileal loop experiments show fluid accumulation is reduced in a dose-dependent manner by TRAM-34, GGTI298, or H1152 when injected together with cholera toxin into the loop. |
N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.684 ml | 8.422 ml | 16.845 ml |
| 5 mM | 0.337 ml | 1.684 ml | 3.369 ml |
| 10 mM | 0.168 ml | 0.842 ml | 1.684 ml |
| 5 mM | 0.034 ml | 0.168 ml | 0.337 ml |
Last Update：2024-01-02 23:10:35
N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT - Reference Information
| biological activity | GGTI298 is an effective GGTase I inhibitor, which can inhibit the process of geranylgeranylated Rap1A and also has certain influence on the process of farnesylated Ha-Ras. in vivo, IC50 values are 3 and> 20 μM respectively. |
| target | IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo) |
| in vitro study | 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 wing erm agglutinin in T84WT cells. Knockdown of DR4 abolishes NκB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 and TRAIL. 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. |
| in vivo study | the vivo mouse ilal loop experiments show fluid accumulation is reduced in a dose-dependent banner by TRAM-34, GGTI298, or H1152 when injected together with cholera toxin into the loop. |
Last Update：2024-04-10 22:29:15
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