GGTI-298

中文名称:

GGTI-298

中文同义词:

GGTASE I抑制剂(GGTI298)

英文名称:

GGTI-298

英文同义词:

GGTI-298;N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT;N-4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-NAPHTHYLBENZOYL-(L)-LEUCINE METHYL ESTER, TFA;GGTI-298 trifluoroacetate salt;N-[[4-(2-(R)-Amino-3-mercaptopropyl)amino]-2-naphthylbenzoyl]leucine methyl ester trifluoroacetate salt;N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-(1-naphthalenyl)benzoyl]-L-leucinemethylestertrifluoroacetatesalt;GGTI298 (CF3CO2H)salt;CS-2228

CAS号:

180977-44-0

分子式:

C27H33N3O3S

分子量:

479.63

EINECS号:

604-604-1

相关类别:

细胞生物学试剂;A cell-permeable, prodrug form of the GGTase I inhibitor GGTI-297.

Mol文件:

Mol File

熔点 

99.5-100 °C

储存条件 

−20°C

溶解度 

DMSO: 22 mg/mL

形态

solid

颜色

off-white

生物活性

GGTI298 是有效的 GGTase I 抑制剂，能够抑制 geranylgeranylated Rap1A 的过程，对 farnesylated Ha-Ras 的过程也有一定影响，在体内，IC50 值分别为 3 和 > 20 μM。

靶点

IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)

体外研究

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.

体内研究

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.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26-36

WGK Germany 

3