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Search Results for " farnesylation "

11

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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...
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...
T35607	10'-Desmethoxystreptonigrin
	10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and tenipo...
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)。
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...
T73755	Farnesyl pyrophosphate
	Farnesyl pyrophosphate (Farnesyl diphosphate) 是一种由15个碳原子组成的异戊二烯类化合物，作为甲羟戊酸 (MVA) 途径的关键代谢中间体。它充当TRPM2 (TRP Channel) 的激动剂，通过激活并打开TRPM2通道，促使离子流入细胞。此外，Farnesyl pyrophosphate 在胆固醇合成、泛醌合成、蛋白质法尼基化修饰以及香叶基-香叶基焦磷酸 (GGPP) 合成过程中扮演着至关重要的底物角色。
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)。
T78081	Farnesyl Pyrophosphate ammonium Farnesyl diphosphate ammonium
	Farnesyl pyrophosphate ammonium salt为15碳类异戊二烯代谢中间体，源自MVA途径，兼具TRPM2激动剂功能，能够触发TRPM2通道开放并促进离子流入细胞。它亦是胆固醇合成、泛醌合成、蛋白质法尼基化修饰以及GGPP合成的关键底物。

化合物

Cat.No: T38050

Target: Transferase

Cat.No: T6271

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

Target: Transferase

Cat.No: T68227

Cat.No: T69403

10'-Desmethoxystreptonigrin

Cat.No: T35607

Cat.No: T73822

GGTI-286 hydrochloride

Cat.No: T62980

Cat.No: T69618

Farnesyl pyrophosphate

Cat.No: T73755

Cat.No: T62379

Farnesyl Pyrophosphate ammonium

Cat.No: T78081

Synonym: Farnesyl diphosphate ammonium

Cat. No.	Product Name	Target	Signaling Pathways
T3314	Perillyl alcohol Isocarveol,Perilla alcohol,紫苏醇	Apoptosis; Endogenous Metabolite	Apoptosis; Metabolism
	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。
T8282	(S)-(−)-Perillyl alcohol Perillyl alcohol,(-)-Perillyl Alcohol,L-紫苏醇	Apoptosis; Endogenous Metabolite	Apoptosis; Metabolism
	(S)-(−)-Perillyl alcohol (Perillyl alcohol) 是一种在薰衣草中发现的单萜，可抑制 Ras 的法尼基化，上调 6-磷酸甘露糖受体并诱导细胞凋亡。它还具有抗癌活性。

天然产物

Perillyl alcohol

Cat.No: T3314

Synonym: Isocarveol,Perilla alcohol,紫苏醇

Target: Apoptosis, Endogenous Metabolite

(S)-(−)-Perillyl alcohol

Cat.No: T8282

Synonym: Perillyl alcohol,(-)-Perillyl Alcohol,L-紫苏醇

Target: Apoptosis, Endogenous Metabolite

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