GGTI-298
| 中文名称 | GGTI-298 |
|---|---|
| 中文同义词 | GGTASE I抑制剂(GGTI298);(S)2-(4-(((R)-2-氨基-3-巯基丙基)氨基)-2-(萘-1-基)苯甲酰胺基)-4-甲基戊酸甲酯;GGTI298试剂;化合物:GGTI298 CAS:180977-44-0;GGTI298试剂;化合物：GGTI298 CAS:180977-44-0 |
| 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 |
| 结构式 |  |
GGTI-298 性质
| 熔点 | 99.5-100 °C |
|---|---|
| 沸点 | 673.7±55.0 °C(Predicted) |
| 密度 | 1.190±0.06 g/cm3(Predicted) |
| 储存条件 | −20°C |
| 溶解度 | 二甲基亚砜：22 mg/毫升 |
| 形态 | 固体 |
| 酸度系数(pKa) | 9.83±0.10(Predicted) |
| 颜色 | 米白色 |
IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)
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.
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.
| 提供商 | 语言 |
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英文
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/05/22 | HY-100876 | GGTI-298 GGTI298 | 180977-44-0 | 1mg | 900元 |
| 2025/05/22 | HY-100876 | GGTI-298 GGTI298 | 180977-44-0 | 5mg | 1800元 |