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22

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1892	Kobe2602	Raf; Ras	GPCR/G Protein; MAPK
	Kobe2602 是 Ras-Raf 相互作用抑制剂，具有抗癌化疗活性。它抑制 H-Ras·GTP 与 c-Raf-1 RBD 结合的Ki 值为 149 μM。
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。
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。
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。
T1876	Kobe0065	Apoptosis; Raf; Ras	Apoptosis; GPCR/G Protein; MAPK
	Kobe0065 是一种新型 Ras-Raf 相互作用抑制剂，可完全抑制 H-Ras·GTP 与 c-Raf-1 RBD 的结合，Ki 值为 46±13 μM。
T5469	K-Ras-IN-1	Raf; Ras	GPCR/G Protein; MAPK
	K-Ras-IN-1 是K-Ras 抑制剂。K-Ras-IN-1 能与 K-Ras (WT)、K-Ras (G12D)、K-Ras (G12V) 和 H-Ras 结合。它对胰腺癌、结肠癌和肺癌的具潜在的研究价值。
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。
T22106	MLS-573151	CDK; Ras	Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	MLS-573151 是 GTPase Cdc42 的选择性抑制剂，EC50 为 2 μM。它通过阻止 GTP 与 Cdc42 的结合来发挥作用。
T27089	CRT0066854 CRT0066854 HCl,CRT-0066854 HCl,CRT 0066854,CRT-0066854
	CRT-0066854 is a PKCι and PKCζ inhibitor. CRT0066854 was able to restore polarized morphogenesis in the dysplastic H-Ras spheroids.
T69710	LB42908
	LB42908 is a highly potent Ras farnesyltransferase inhibitor(IC(50)=0.9 nM against H-Ras and 2.4 nM against K-Ras) with potential anticancer activity.
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.
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。
T26469	A-176120
	A-176120 is a potent farnesyl pyrophosphate (FPP) analogues, it selectively inhibits farnesyltransferase. It has anti-angiogenic potential and may reduce H-ras NIH3T3 tumour growth.
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.
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。
T68227	BMS-214662 HCl
	BMS-214662 is a Farnesyltransferase inhibitor , is also a nonsedating benzodiazepine derivative with potential antineoplastic activity. BMS-214662 inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction, which may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. This agent may reverse the malignant phenotype of H-Ras-transformed cells and has been shown to be active against tumor cell...
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.
T62379	GGTI-286
	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)。
T69618	XR3054
	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 kina...
T73822	GGTI-286 TFA
	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。
T62980	GGTI-286 hydrochloride
	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)。
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。

化合物

Cat.No: T1892

Target: Raf, Ras

Cat.No: T2678

Target: Transferase

Cat.No: T38050

Target: Transferase

Cat.No: T6302

Synonym: Sarasar,氯那法尼,Sch66336

Target: Raf, Transferase, Autophagy, Ras

Cat.No: T1876

Target: Apoptosis, Raf, Ras

Cat.No: T5469

Target: Raf, Ras

FTI-277 hydrochloride

Cat.No: T2700

Synonym: FTI 277 HCl

Target: Apoptosis, Transferase, Ras

Cat.No: T22106

Target: CDK, Ras

Cat.No: T27089

Synonym: CRT0066854 HCl,CRT-0066854 HCl,CRT 0066854,CRT-0066854

Cat.No: T69710

Cat.No: T41212

Cat.No: T62675

Cat.No: T26469

Cat.No: T15353

Target: Others

(Rac)-Lonafarnib

Cat.No: T72707

Synonym: Sch66336 racemate

Cat.No: T68227

Cat.No: T24188

Synonym: UNII-6137X5QNJF,J 104871

Cat.No: T62379

Cat.No: T69618

Cat.No: T73822

GGTI-286 hydrochloride

Cat.No: T62980

Cat.No: T64101

Cat. No.	Product Name	Target	Signaling Pathways
T5368	Eicosapentaenoic Acid	Histone Demethylase; Others; Endogenous Metabolite	Chromatin/Epigenetic; Metabolism; Others
	Eicosapentaenoic Acid 是一种 ω-3 脂肪酸。
T5S0620	3-Dehydrotrametenolic acid Dehydrotrametenolic acid,松苓新酸,3-氢化去氢松苓酸	Apoptosis; Others; Dehydrogenase	Apoptosis; Metabolism; Others
	3-Dehydrotrametenolic acid 是从茯苓菌核分离的一种乳酸脱氢酶抑制剂，可诱导细胞凋亡，具有抗癌活性。它促进体外脂肪细胞分化，在体内起胰岛素增敏剂的作用。
T72152	Eicosapentaenoic Acid sodium 二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium
	Eicosapentaenoic Acid (EPA) sodium 为口服活性 ω-3 长链多不饱和脂肪酸 (ω-3 LC-PUFAs)。其通过DNA去甲基化，促进肿瘤抑制基因CCAAT/增强子结合蛋白δ (C/EBPδ)的重新表达，并通过H-RAS内含子1 CpG岛的去甲基化，激活U937白血病细胞中RAS/ERK/C/EBPβ途径。此外，该化合物能够促进血管平滑肌细胞松弛和血管舒张。

天然产物

Eicosapentaenoic Acid

Cat.No: T5368

Target: Histone Demethylase, Others, Endogenous Metabolite

3-Dehydrotrametenolic acid

Cat.No: T5S0620

Synonym: Dehydrotrametenolic acid,松苓新酸,3-氢化去氢松苓酸

Target: Apoptosis, Others, Dehydrogenase

Eicosapentaenoic Acid sodium

Cat.No: T72152

Synonym: 二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium

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