ggtase i

GGTI-2418 是一种具有选择性和高效性的香叶基香叶基转移酶 I (GGTase I) 抑制剂,具有潜在的抗肿瘤活性，抑制人乳腺肿瘤的生长，抑制 FTase 活性，可用于研究乳腺癌。

FTI-277 hydrochloride (FTI 277 HCl) 是一种法尼基转移酶FTase 抑制剂，高效 Ras CAAX 肽模拟物，可抑制H-Ras 和K-Ras 信号转导，还可抑制hepatitis delta virus 感染。

GGTI298 Trifluoroacetate (GGTI 298 TFA salt) 是一种GGTase I 抑制剂，能够抑制Rap1A 且IC50值为3μM，对Ha-Ras 的作用很小IC50值 > 20 μM。

FGTI-2734 是 有效的RAS C-末端法尼基转移酶 (FT) 和香叶烯基转移酶-1 (GGT-1) 抑制剂，IC50s 分别为 250 nM 和 520 nM。 它可以阻断 KRAS 的膜定位，从而解决 KRAS 耐药性问题，并抑制突变的 KRAS 胰腺肿瘤。

OU749 是一种 γ-谷氨酰转移酶 (GGT) 抑制剂，固有 Ki 值为 17.6 μM。

GGTI-2133 是一种有效的仿肽基香叶基转移酶 I 型抑制剂（GGTase I），IC50值为38 nM。GGTI-2133 可抑制小鼠实验性哮喘中炎症细胞向气道的侵袭。

L-778123 hydrochloride 是一种FPTase 和GGPTase-I 双重抑制剂，IC50分别为2 nM 和 98 nM。

GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.

BAY 593作为一种geranylgeranyltransferase-I (GGTase-I)抑制剂，能够阻断Rho-GTPases的激活，进而抑制YAP1 TAZ信号通路。在异种移植小鼠模型中，该化合物能剂量依赖性地抑制肿瘤生长，具体IC50值分别为MT-1080细胞中的38.4 nM和MDA-MB-231细胞中的564 nM，同时也抑制了PXF 541异种移植物的生长。

GGTI-2154 is a potent, selective geranylgeranyltransferase I (GGTase I) inhibitor, boasting an IC50 of 21 nM and demonstrating over 200-fold selectivity against FTase (IC50=5600 nM). Its efficacy and specificity make it a valuable tool for cancer research[1][2].

GGTI-286 是一种高效的、具有细胞通透性 GGTase I 抑制剂 (IC50: 2 μM)。GGTI-286 对 NIH3T3 细胞中的 Rap1A 香叶香叶基化的(IC50: 2 μM)抑制作用强于 H-Ras 的法尼化作用(IC50>30 μM)。GGTI-286 也可以有效抑制 K-Ras4B 刺激(IC50: 1 μM)。

GGTI-2154 hydrochloride 是一种有效的、选择性的 geranylgeranyltransferase I (GGTase I) 抑制剂 (IC50: 21 nM)。GGTI-2154 hydrochloride 对 GGTase I 的选择性是 FTase (IC50: 5600 nM) 的 200 倍以上。GGTI-2154 hydrochloride 能够用于研究癌症。

GGTI-286 hydrochloride 是一种 GGTase I 的高效抑制剂 (IC50: 2 μM)，也能够有效抑制 K-Ras4B (IC50: 1 μM)。GGTI-286 hydrochloride 在 NIH3T3 细胞中，对 Rap1A 香叶香叶基化的抑制作用高于 H-Ras 的法尼化作用 (IC50=2和 >30 μM)。

BIM-46050 is a potent and specific inhibitor of human farnesyltransferase. BIM-46050 is free acidic form of BIM-46068. The IC50 values for in vitro inhibition of human brain FTase indicate that BIM-46050 and the ester form BIM-46068 are potent inhibitors of farnesyltransferase. Their potencies are in the nanomolar range and compare favorably with the compounds B581, FTI-277 and L745,631. B581 is an analog of the tetrapeptide Cys-Val-Phe-Met obtained by replacement of the amino-terminal amide bonds inhibiting processing of farnesylated proteins specifically. FTI-277 is a methyl ester of FTI-276, reported as a preferential inhibitor of FTase over GGTase I (100-fold). L745,631 is a 2-substituted piperazine reported to be a highly selective inhibitor of FTase over GGTase (2,000-fold). The selectivity of BIM-46050 and BIM-46068 for FTase over GGTase is very similar for both compounds (3,000-fold).

GGTI-297 is a potent, cell-permeable, and selective peptidomimetic inhibitor of GGTase I compared to Farnesyl Transferase (FTase).

GGTI-286 TFA 是一种高效的细胞通透性 GGTase I 抑制剂，(IC50为 2 μM。在 NIH3T3 细胞中，GGTI-286 TFA 对 Rap1A 香叶香叶基化的抑制作用高于 H-Ras 的法尼化作用 (IC50s=2 和 >30 μM)。GGTI-286 TFA 还能有效抑制 K-Ras4B 刺激，IC50为 1 μM。

GGTI 2133, a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50= 38 nM), exhibits 140-fold selectivity towards GGTase I compared to farnesyltransferase (IC50= 5,400 nM). The compound effectively inhibits the geranylgeranylation of RAP1A (IC50= 10 µM) without affecting the farnesylation of H-Ras (IC50= >30 µM). Moreover, GGTI 2133 reduces the growth, migration, and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control levels, respectively. When administered intraperitoneally at 5 mg/kg per day, it prevents eosinophil infiltration into the airways in a mouse model of allergic bronchial asthma, although it does not reduce chemokine levels. Additionally, GGTI 2133 thwarts naloxone-induced contraction of ileum in rats experiencing morphine withdrawal syndrome and mitigates the severity of withdrawal symptoms in vivo (ED50= 0.076 mg/kg).

BAY-593是一种口服活性的GGTase-I抑制剂，具有抗肿瘤活性并阻断体内[YAP1 TAZ]信号传导。

(7S)-BAY-593为BAY-593的S型异构体,该化合物为口服有效的GGTase-I抑制剂,具备抑制肿瘤的潜能并能阻断体内的YAP1 TAZ信号传导.