GGTI-298
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- CAS号:
- 180977-44-0
- 英文名:
- GGTI-298
- 英文别名:
- CS-2228;GGTI-298;GGTI298
(GGTI-298;GGTI-298 free base;GGTI298 (CF3CO2H)salt;GGTI-298 trifluoroacetate salt;N-4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-NAPHTHYLBENZOYL-(L)-LEUCINE METHYL ESTER, TFA;L-Leucine, N-[4-[[(2R)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)benzoyl]-, methyl ester;(S)-Methyl 2-(4-(((R)-2-amino-3-mercaptopropyl)amino)-2-(naphthalen-1-yl)benzamido)-4-methylpentanoate;N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT
- 中文名:
- GGTI-298
- 中文别名:
- 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
- CBNumber:
- CB6450528
- 分子式:
- C27H33N3O3S
- 分子量:
- 479.63
- MOL File:
- Mol file
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GGTI-298化学性质
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熔点:
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99.5-100 °C
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沸点:
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673.7±55.0 °C(Predicted)
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密度:
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1.190±0.06 g/cm3(Predicted)
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储存条件:
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−20°C
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溶解度:
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DMSO: 22 mg/mL
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形态:
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solid
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酸度系数(pKa):
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9.83±0.10(Predicted)
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颜色:
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off-white
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GGTI-298性质、用途与生产工艺
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。
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.
GGTI-298
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-100876 | GGTI-298
GGTI298 | 180977-44-0 | 1mg | 900元 |
| 2024/04/30 | HY-100876 | GGTI-298
GGTI298 | 180977-44-0 | 10mg | 2800元 |
180977-44-0, GGTI-298 相关搜索:
- A cell-permeable, prodrug form of the GGTase I inhibitor GGTI-297.
- 细胞生物学试剂
- C27H33N3O3SCF3CO2H
- C27H33N3O3SC2HF3O2
- (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
- GGTASE I抑制剂(GGTI298)
- 180977-44-0
- (S)-Methyl 2-(4-(((R)-2-amino-3-mercaptopropyl)amino)-2-(naphthalen-1-yl)benzamido)-4-methylpentanoate
- GGTI-298 free base
- L-Leucine, N-[4-[[(2R)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)benzoyl]-, methyl ester
- methyl (2S)-2-[[4-[[(2R)-2-amino-3-sulfanylpropyl]amino]-2-naphthalen-1-ylbenzoyl]amino]-4-methylpentanoate,2,2,2-trifluoroacetic acid
- GGTI298
(GGTI-298
- CS-2228
- GGTI298 (CF3CO2H)salt
- N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-(1-naphthalenyl)benzoyl]-L-leucinemethylestertrifluoroacetatesalt
- N-[[4-(2-(R)-Amino-3-mercaptopropyl)amino]-2-naphthylbenzoyl]leucine methyl ester trifluoroacetate salt
- GGTI-298 trifluoroacetate salt
- N-4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-NAPHTHYLBENZOYL-(L)-LEUCINE METHYL ESTER, TFA
- N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT
- GGTI-298