ftase

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].

Ftase Inhibitor III, derived from a phenotypic screen, functions as an anion-dependent inhibitor of Farnesyltransferase.

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。

J-104871 (UNII-6137X5QNJF) 是一种新型法尼基转移酶抑制剂 (FTase) ，以竞争性方式阻断体内 Ras 法尼基化，抑制活化的 H-ras 转化的 NIH3T3 细胞中的 Ras 加工，抑制移植有活化 H-ras 转化的 NIH3T3 细胞的裸鼠的肿瘤生长。

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。

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。

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。

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

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。

FTI-2153 TFA 是一种高选择性的、有效的法尼基转移酶 farnesyltransferase (FTase) 抑制剂 (IC50: 1.4 nM)。FTI-2153 TFA 可有效抑制 H-Ras 蛋白的加工修饰 (IC50: 10 nM)，对其抑制活性是对 Rap1A 蛋白加工的 3000 多倍。

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。

FTI-2153 is a potent and highly selective farnesyltransferase (FTase) inhibitor (IC50: 1.4 nM). FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing.

AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be correlated to the antiproliferative activity of the drug. AZD3409 might be active in gefitinib-resistant breast carcinoma.

FTI-277 是一种法尼基转移酶 FTase 抑制剂，也是一种高效 Ras CAAX 肽模拟物。FTI-277 对 H-Ras 和 K-Ras 信号转导具有抑制作用，能够抑制 hepatitis delta virus (HDV) 感染。

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。

FTI-249 is a Farnesyltransferase inhibitor, which potently inhibited FTase (IC50 = 100–200 nM).

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。

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).

(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).

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。

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.

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].

FTI 277 TFA is a prodrug form of FTI 276 that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10μM respectively) and disrupts constitutive H-Ras-specific activation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.

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。