farnesyl transferase

LB42708 是一种口服有活力的特异性法尼基转移酶抑制剂。它对H-Ras、N-Ras 和K-Ras4B 的法尼基化均有抑制作用，其IC50分别为 0.8 nM、1.2 nM 和 2.0 nM。

Perillyl alcohol (Isocarveol) 是一种单萜，可在不影响正常细胞的情况下诱导肿瘤细胞凋亡。

ABT-100 is a potent, highly selective, and orally active farnesyl transferase inhibitor with broad-spectrum antitumor activity.

BMS-214662是一种有效的、有选择性的 farnesyl transferase 抑制剂，可诱导原始CD34+慢性髓性白血病(CML)干细胞 祖细胞的线粒体凋亡，具有选择性靶向CML 干细胞 祖细胞的能力，具有抗肿瘤活性。

Lonafarnib (Sch66336) 是一种可口服的 FPTase 抑制剂，作用于 H-ras、K-ras 和 N-ras，IC50分别为 1.9 nM、5.2 nM 和 2.8 nM。它具有抗肝炎三角洲病毒的活性。

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

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。

Tipifarnib S enantiomer ((S)-(-)-R-115777) 是Tipifarnib 的 S 型对映体，它比 Tipifarnib 特性低。其中 Tipifarnib 是farnesyltransferase 高效特异性抑制剂，IC50=0.6 nM。

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。

CP-609754 是高效的、可逆的法尼基转移酶抑制剂，对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng mL 和 46 ng mL。CP-609754有潜在的抗癌作用。

R 115777 is an inhibitor of farnesyl transferase.

FTase-IN-1 (compound 17a) is a highly effective inhibitor of fanesyl transferase (FTase), exhibiting a remarkable IC50 value of 0.35 μM. This compound demonstrates significant cytotoxicity potential and exhibits powerful antitumor activity [1].

Tipifarnib (IND 58359) 能够抑制法尼基转移酶 (FTase)，IC50=0.86 nM，具有潜在抗肿瘤特性。

Methyl ganoderate A, an inhibitor of Farnesyl protein transferase (FPT) with an IC50 of 38 µM, exhibits potential anticancer effects. Additionally, it inhibits fatty acid amide hydrolase (FAAH), further underscoring its therapeutic potential.

FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.

XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kinase activation and anchorage-independent growth in NIH 3T3 transformed with v12 H-ras. Since the antiproliferative effect of the compound is not related to the ras phenotype, XR3054 may also have effects on other cell signaling mechanisms.

(Rac)-Lonafarnib (Sch66336外消旋体) 作为Lonafarnib的外消旋体，属于一种口服有效的法尼基蛋白转移酶 (FPTase) 抑制剂，针对H-ras、K-ras及N-ras展现出杰出的抑制效能，其IC50值分别为1.9 nM、5.2 nM和2.8 nM。此外，Lonafarnib还显示出对抗肝炎三角洲病毒 (HDV) 的潜在活性。

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

Zaragozic acid D inhibits squalene synthase and ras farnesyl-protein transferase isolated from the keratinophilic fungus Amauroascus niger.

FTI-2148 is an inhibitor of RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) (IC50s: 1.4 nM and 1.7 μM, respectively).

Tubulin polymerization-IN-25 是一种选择性的、双重 tubulin polymerization (IC50: 1.11 μM) 和 farnesyl transferase (FTase) (IC50: 0.39 μM) 抑制剂。Tubulin polymerization-IN-25 对癌细胞表现出细胞毒性，能够阻断细胞增殖。

FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.

Tectol 是从Lippia sidoides 中分离的，对人白血病细胞株 HL60 和 CEM 具有显著的抑制作用。它是法尼基转移酶抑制剂，在人和布氏锥虫的IC50分别为 2.09 和 1.73 μM。它具有抗疟原虫活性，是一种中等活性的生长抑制剂，IC50 为 3.44±0.20μM。

α-hydroxy Farnesyl phosphonic acid is a nonhydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of farnesyl transferase (FTase). At concentrations greater than 1 μM, α-hydroxy farnesyl phosphonic acid inhibits the processing of Ras in Ha-ras-transformed NIH3T3 cells.

L 739749 is a CAAX peptidomimetic. It is also an inhibitor of farnesyl-protein transferase.

Lipiferolide is an inhibitor of farnesyl protein transferase(FPTase), it inhibits the FPTase activity in a dose-dependent manner, and shows cell growth inhibitory activity against several tumor cells, it possesses cytotoxic activity against KB cells. Liriodenine also has antiplasmodial activity.

Zaragozic acid D(2) inhibits squalene synthase and ras farnesyl-protein transferase isolated from the keratinophilic fungus Amauroascus niger.

Arglabin ((+)-Arglabin) 是从青蒿中分离出的一种天然产物，是一种 NLRP3 炎性体抑制剂，具有抗动脉粥样硬化和抗癌作用。