目录号 | 产品详情 | 靶点 | |
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T38050 | Transferase | ||
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 | Transferase | ||
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。 | |||
T3314 | Apoptosis Endogenous Metabolite | ||
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。 | |||
T69403 | |||
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. | |||
T8282 | Apoptosis Endogenous Metabolite | ||
(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。 | |||
T68227 | |||
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 cells with and without Ras mutations. | |||
T35607 | |||
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 teniposide and cisplatin-resistant A2780 cells (IC50s = 0.003, 0.001, and 0.01 μg/ml, respectively). 10'-Desmethoxystreptonigrin is also an inhibitor of p21ras farnesylation (IC50 = 21 nM). | |||
T62980 | |||
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)。 | |||
T73822 | |||
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。 | |||
T62379 | |||
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)。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPJ-00053 | PRL-2 Protein, Human, Recombinant (His) | Human | E. coli | ||
PTP4A2, also known as PRL2 or PTPCAAX2, is short for Protein tyrosine phosphatase type IVA 2. This protein exists in cell membrane, cytoplasm,endosome and membrane. PTP4A2 is often farnesylated during post-translational modification. Farnesylation is required for membrane targeting and for interaction with RABGGTB. The unfarnesylated forms are redirected to the nucleus and cytosol. It can stimulate progression from G1 into S phase during mitosis and promotes tumors. It also inhibits geranylgeranyl transferase type II activity by blocking the association between RABGGTA and RABGGTB.
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TMPH-01323 | FDPS Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Key enzyme in isoprenoid biosynthesis which catalyzes the formation of farnesyl diphosphate (FPP), a precursor for several classes of essential metabolites including sterols, dolichols, carotenoids, and ubiquinones. FPP also serves as substrate for protein farnesylation and geranylgeranylation. Catalyzes the sequential condensation of isopentenyl pyrophosphate with the allylic pyrophosphates, dimethylallyl pyrophosphate, and then with the resultant geranylpyrophosphate to the ultimate product farnesyl pyrophosphate.
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TMPY-03430 | RheB Protein, Human, Recombinant (His) | Human | Baculovirus-Insect Cells | ||
RHEB is a recently discovered member of the Ras superfamily that may be involved in neural plasticity. This function is novel and not typically associated with the Ras proteins. RHEB gene is a member of the small GTPase superfamily and encodes a lipid-anchored, cell membrane protein with five repeats of the RAS-related GTP-binding region. RHEB is vital in regulation of growth and cell cycle progression due to its role in the insulin / TOR / S6K signaling pathway. The protein has GTPase activity and shuttles between a GDP-bound form and a GTP-bound form, and farnesylation of RHEB is required for this activity. Three pseudogenes have been mapped, two on chromosome 1 and one on chromosome 22.
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TMPJ-01126 | RheB Protein, Human, Recombinant (GST) | Human | E. coli | ||
GTP-Binding Protein Rheb (RHEB) is a member of the small GTPase superfamily and encodes a lipid-anchored, cell membrane protein with five repeats of the RAS-related GTP-binding region. Highest levels of RHEB can be found in the skeletal and cardiac muscle, and it is vital in the regulation of growth and cell cycle progression due to its role in the Insulin/TOR/S6K signaling pathway. RHEB stimulates the phosphorylation of S6K1 and EIF4EBP1 through activation of mTORC1 signaling, and it activates the protein kinase activity of mTORC1. RHEB has GTPase activity and shuttles between a GDP-bound form and a GTP-bound form, farnesylation of the protein is required for this activity.
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TMPY-02654 | FDPS Protein, Human, Recombinant (His) | Human | E. coli | ||
Z-farnesyl diphosphate synthase (FDPS) is an enzyme belonging to the family of transferases, specifically those transferring aryl or alkyl groups other than methyl groups. Z-farnesyl diphosphate synthase (FDPS) functions as key enzyme in isoprenoid biosynthesis which catalyzes the formation of farnesyl diphosphate, a precurcor for several classes of essential metabolites. FDPS catalyzes the production of geranyl pyrophosphate and farnesyl pyrophosphate from isopentenyl pyrophosphate and dimethylallyl pyrophosphate. The resulting product, farnesyl pyrophosphate, is a key intermediate in cholesterol and sterol biosynthesis, a substrate for protein farnesylation and geranylgeranylation, and a ligand or agonist for certain hormone receptors and growth receptors. Drugs that inhibit this enzyme prevent the post-translational modifications of small GTPases and have been used to treat diseases related to bone resorption. Functions of FDPS may be inactivated by interferon-induced RSAD2. This inactivation may result of disruption of lipid rafts at the plasma membrane, and thus have an antiviral effect since many enveloped viruses need lipid rafts to bud efficiently out of the cell.
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TMPY-00451 | FDPS Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
Z-farnesyl diphosphate synthase (FDPS) is an enzyme belonging to the family of transferases, specifically those transferring aryl or alkyl groups other than methyl groups. Z-farnesyl diphosphate synthase (FDPS) functions as key enzyme in isoprenoid biosynthesis which catalyzes the formation of farnesyl diphosphate, a precurcor for several classes of essential metabolites. FDPS catalyzes the production of geranyl pyrophosphate and farnesyl pyrophosphate from isopentenyl pyrophosphate and dimethylallyl pyrophosphate. The resulting product, farnesyl pyrophosphate, is a key intermediate in cholesterol and sterol biosynthesis, a substrate for protein farnesylation and geranylgeranylation, and a ligand or agonist for certain hormone receptors and growth receptors. Drugs that inhibit this enzyme prevent the post-translational modifications of small GTPases and have been used to treat diseases related to bone resorption. Functions of FDPS may be inactivated by interferon-induced RSAD2. This inactivation may result of disruption of lipid rafts at the plasma membrane, and thus have an antiviral effect since many enveloped viruses need lipid rafts to bud efficiently out of the cell.
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