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26

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40331	Ftase inhibitor III
	Ftase Inhibitor III, derived from a phenotypic screen, functions as an anion-dependent inhibitor of Farnesyltransferase.
T61682	FTase-IN-1
	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].
T11282	FGTI-2734	Transferase	Metabolism
	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。
T6302	Lonafarnib Sarasar,氯那法尼,Sch66336	Raf; Transferase; Autophagy; Ras	Autophagy; GPCR/G Protein; MAPK; Metabolism
	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。
T2678	LB42708	Transferase	Metabolism
	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。
T3182	L-778123 hydrochloride L 778123	Telomerase; Transferase	DNA Damage/DNA Repair; Metabolism
	L-778123 hydrochloride 是一种FPTase 和GGPTase-I 双重抑制剂，IC50分别为2 nM 和 98 nM。
T2700	FTI-277 hydrochloride FTI 277 HCl	Apoptosis; Transferase; Ras	Apoptosis; GPCR/G Protein; MAPK; Metabolism
	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。
T38050	CP-609754	Transferase	Metabolism
	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。
T6271	Tipifarnib 替吡法尼,R115777,Zarnestra,IND 58359	Transferase	Metabolism
	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。
T17102	Tipifarnib (S enantiomer) Tipifarnib S enantiomer,(S)-(-)-R-115777,(S)-Tipifarnib,IND-58359 S enantiomer	Transferase	Metabolism
	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。
T24188	J-104871 UNII-6137X5QNJF,J 104871
	J-104871 is an FTase inhibitor. J-104871 inhibits FTase in an FPP-competitive manner in whole cells as well as in the in vitro system. J-104871 suppressed tumor growth in nude mice transplanted with activated H-ras-transformed NIH3T3 cells.
T11396	GGTI-2418	Transferase	Metabolism
	GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors. GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor.
T70372	FTI-249
	FTI-249 is a Farnesyltransferase inhibitor, which potently inhibited FTase (IC50 = 100Â–200 nM).
T70157	GGTI-297
	GGTI-297 is a potent, cell-permeable, and selective peptidomimetic inhibitor of GGTase I compared to Farnesyl Transferase (FTase).
T37446	GGTI-2154
	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].
T69994	BIM-46050
	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 bon...
T35433	α-hydroxy Farnesyl Phosphonic Acid
	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.
T41212	FTI 277
	FTI 277 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.
T62135	Tubulin polymerization-IN-25
	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。
T15353	FTI-2153	Others	Others
	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.
T62675	FTI-277
	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。
T64101	FTI-2153 TFA
	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。
T72707	(Rac)-Lonafarnib Sch66336 racemate
	(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。
T69403	AZD-3409
	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 corre...
T62844	GGTI-2154 hydrochloride
	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。
T10567	BMS-214662	Raf	MAPK
	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。

化合物

Ftase inhibitor III

Cat.No: T40331

Cat.No: T61682

Cat.No: T11282

Target: Transferase

Cat.No: T6302

Synonym: Sarasar,氯那法尼,Sch66336

Target: Raf, Transferase, Autophagy, Ras

Cat.No: T2678

Target: Transferase

L-778123 hydrochloride

Cat.No: T3182

Synonym: L 778123

Target: Telomerase, Transferase

FTI-277 hydrochloride

Cat.No: T2700

Synonym: FTI 277 HCl

Target: Apoptosis, Transferase, Ras

Cat.No: T38050

Target: Transferase

Cat.No: T6271

Synonym: 替吡法尼,R115777,Zarnestra,IND 58359

Target: Transferase

Tipifarnib (S enantiomer)

Cat.No: T17102

Synonym: Tipifarnib S enantiomer,(S)-(-)-R-115777,(S)-Tipifarnib,IND-58359 S enantiomer

Target: Transferase

Cat.No: T24188

Synonym: UNII-6137X5QNJF,J 104871

Cat.No: T11396

Target: Transferase

Cat.No: T70372

Cat.No: T70157

Cat.No: T37446

Cat.No: T69994

α-hydroxy Farnesyl Phosphonic Acid

Cat.No: T35433

Cat.No: T41212

Tubulin polymerization-IN-25

Cat.No: T62135

Cat.No: T15353

Target: Others

Cat.No: T62675

Cat.No: T64101

(Rac)-Lonafarnib

Cat.No: T72707

Synonym: Sch66336 racemate

Cat.No: T69403

GGTI-2154 hydrochloride

Cat.No: T62844

Cat.No: T10567

Target: Raf

Cat. No.	Product Name	Target	Signaling Pathways
TN6512	Tectol	Transferase; Parasite	Metabolism; Microbiology/Virology
	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。
TQ0165	Arglabin 阿格拉宾,(+)-Arglabin	NOD-like Receptor (NLR); Transferase; NOD; Autophagy	Autophagy; Immunology/Inflammation; Metabolism; NF-κB
	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。
T16011	Manumycin A	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Manumycin A is an antibiotic. Manumycin A induces apoptosis and exerts antitumor activity. Manumycin A inhibits exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A acts as a selective, competitive inhibitor of

天然产物

Cat.No: TN6512

Target: Transferase, Parasite

Cat.No: TQ0165

Synonym: 阿格拉宾,(+)-Arglabin

Target: NOD-like Receptor (NLR), Transferase, NOD, Autophagy

Cat.No: T16011

Target: Prostaglandin Receptor

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