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CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL . CP-609754 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo . YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent . YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation .
LB42708 is a potent, selective and orally active farnesyltransferase inhibitor. LB42708 inhibits farnesylation of H-Ras, N-Ras and K-Ras4B with IC50s of 0.8 nM, 1.2 nM and 2.0 nM, respectively .
FTI 276 TFA is a farnesyltransferase (FTase) inhibitor with an IC50 of 0.5 nM, and it exhibits selectivity for FTase over geranylgeranyltransferase I (GGTase I). FTI 276 TFA blocks the farnesylation of H-Ras and K-Ras4B, causes inactive Ras-Raf complexes to accumulate in the cytoplasm, and inhibits constitutive MAPK activation. FTI 276 TFA reduces the number, incidence and volume of tumors, and restricts the growth of tumors expressing activated K-ras. FTI 276 TFA can be used in research related to pulmonary adenoma .
FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity .
Farnesylthioacetic acid is a competitive, non-substrate inhibitor of Prenylcysteine α-carboxyl methyltransferase. It acts as a non-substrate competitive inhibitor of Arabidopsis thaliana Prenylcysteine α-carboxyl methyltransferase and blocks methyltransferase activity. Farnesylthioacetic acid does not inhibit protein farnesyltransferase activity in Arabidopsis. It induces Apoptosis. Farnesylthioacetic acid regulates the subcellular localization of Ras protein, reducing the proportion of cytoplasmic Ras protein without disrupting membrane binding. It enhances ABA-induced seed dormancy, delays seed germination, and promotes maximum stomatal closure at lower exogenous ABA concentrations. Farnesylthioacetic acid can be used in studies related to promyelocytic leukemia .
Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM. Tipifarnib S enantiomer is the less active isomer.
GGTI-2133, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 can be used for the study of eosinophilic airway inflammation such as asthma .
BMS-214662 hydrochloride is an inhibitor of farnesyltransferase(FarnesylTransferase). BMS-214662 hydrochloride can effectively block the localization and function of Ras proteins on the cell membrane by inhibiting the prenylation modification of Ras proteins, thereby exerting anti-tumor activity. The IC50 value of BMS-214662 hydrochloride for H-Ras is 1.3 nM, and for K-Ras it is 8.4 nM. BMS-214662 hydrochloride can be used in the research of tumor diseases related to Ras .
FTI-277 is a farnesyltransferase (FTase) inhibitor. FTI-277 inhibits Ras farnesylation, blocks the phosphorylation of downstream ERK1/2 and mTOR, and reduces membrane-bound active N-ras protein. FTI-277 activates caspase 3, upregulates Bim expression, induces cell apoptosis, suppresses regulatory T cell expansion, enhances macrophage phagocytosis, and improves bacterial clearance. FTI-277 activates the PI3K/Akt signaling pathway, inhibits osteoblast differentiation, and reduces the proliferation ability of neuroblastoma cells. FTI-277 can be used in research related to head and neck squamous cell carcinoma, neuroblastoma, sepsis, and vascular calcification .
FTI-277 TFA is a farnesyltransferase (FTase) inhibitor. FTI-277 TFA inhibits Ras farnesylation, blocks the phosphorylation of downstream ERK1/2 and mTOR, and reduces membrane-bound active N-ras protein. FTI-277 TFA activates caspase 3, upregulates Bim expression, induces cell apoptosis, suppresses regulatory T cell expansion, enhances macrophage phagocytosis, and improves bacterial clearance. FTI-277 TFA activates the PI3K/Akt signaling pathway, inhibits osteoblast differentiation, and reduces the proliferation ability of neuroblastoma cells. FTI-277 TFA can be used in research related to head and neck squamous cell carcinoma, neuroblastoma, sepsis, and vascular calcification .
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM . Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM .
YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo . YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent . YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation .
L-739750 is a selective protein farnesyltransferase (PFTase) inhibitor (IC50: 0.4 nM). PFTase utilizes farnesyl diphosphate to farnesylate the cysteine residue of protein substrates having a C-terminal CAAX motif. L-739750 is a selective CAAX peptidomimetic .
GGTI-2133 TFA, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 TFA shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 TFA inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 TFA can be used for the study of eosinophilic airway inflammation such as asthma .
L-744832 is a farnesyltransferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer .
BIM-46068 is a potent, selectively human brain Farnesyltransferase (FTase) inhibitor (IC50 = 91.4 nM). BIM-46068 can specifically inhibit Ras processing in MiaPaCa-2 cancer cells. BIM-46068 can be used for the study of pancreatic cancer .
Prenyl-IN-1 is a protein prenylation inhibitor, especially a geranylgeranyltransferase (GGT) or a farnesyltransferase (FT) inhibitor, exhibiting potent activity against oxidative stress, and particularly in the treatment of Parkinson's Disease.
Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species .
FTI-2153 TFA is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 TFA is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity .
J 104871 (J-104135) is a farnesyl pyrophosphate (FPP)-competitive farnesyltransferase (FTase) inhibitor. J 104871 inhibits rat brain FTase with an IC50 of 3.9 nM in the presence of farnesyl pyrophosphate (FPP) .
10'-Desmethoxystreptonigrin is an inhibitor for Ras Farnesyltransferase with an IC50 of 21 μM. 10'-Desmethoxystreptonigrin is a broad-spectrum antibiotic with antibacterial activity. 10'-Desmethoxystreptonigrin exhibits antitumor activity against P388 leukemia, without significant cytotoxicity (LD50 is 8.8 mg/kg) .
LB42908 is a potent, selective and orally active farnesyltransferase inhibitor. LB42908 inhibits farnesylation of H-Ras, K-Ras with IC50 values of 0.9 nM, 2.4 nM for H-Ras, K-Ras, respectively. LB42908 shows antiproliferative activity. LB42908 shows antitumor activity .
YM-53601 (Standard) is the analytical standard of YM-53601 (HY-100313A). This product is intended for research and analytical applications. YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo . YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent . YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation .
Tipifarnib (Standard) is the analytical standard of Tipifarnib (HY-10502). This product is intended for research and analytical applications. Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC50 of 0.86 nM. Antineoplastic activity and antiparasitic activity .
Farnesylthioacetic acid is a competitive, non-substrate inhibitor of Prenylcysteine α-carboxyl methyltransferase. It acts as a non-substrate competitive inhibitor of Arabidopsis thaliana Prenylcysteine α-carboxyl methyltransferase and blocks methyltransferase activity. Farnesylthioacetic acid does not inhibit protein farnesyltransferase activity in Arabidopsis. It induces Apoptosis. Farnesylthioacetic acid regulates the subcellular localization of Ras protein, reducing the proportion of cytoplasmic Ras protein without disrupting membrane binding. It enhances ABA-induced seed dormancy, delays seed germination, and promotes maximum stomatal closure at lower exogenous ABA concentrations. Farnesylthioacetic acid can be used in studies related to promyelocytic leukemia .
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM . Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM .
YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo . YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent . YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation .
Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species .
10'-Desmethoxystreptonigrin is an inhibitor for Ras Farnesyltransferase with an IC50 of 21 μM. 10'-Desmethoxystreptonigrin is a broad-spectrum antibiotic with antibacterial activity. 10'-Desmethoxystreptonigrin exhibits antitumor activity against P388 leukemia, without significant cytotoxicity (LD50 is 8.8 mg/kg) .
FDFT1 is a key enzyme in cellular metabolism responsible for coordinating the condensation of two farnesyl pyrophosphate (FPP) molecules, a key step in sterol biosynthesis. The process proceeds in two distinct steps: First, two FPP molecules react to form the stable squalene diphosphate intermediate (PSQPP), releasing protons and inorganic diphosphate. FDFT1 Protein, Human (His) is the recombinant human-derived FDFT1 protein, expressed by E. coli , with N-6*His labeled tag.
FNTA protein is a key subunit in the farnesyltransferase and geranylgeranyltransferase complexes, which can transfer farnesyl or geranylgeranyl moieties to proteins with Cys-aliphatic-aliphatic-X sequence cysteine residues in proteins. This enzymatic activity contributes to post-translational protein modifications. FNTA Protein, Human is the recombinant human-derived FNTA protein, expressed by E. coli , with tag free.
FNTA protein is a key subunit in the farnesyltransferase and geranylgeranyltransferase complexes, which can transfer farnesyl or geranylgeranyl moieties to proteins with Cys-aliphatic-aliphatic-X sequence cysteine residues in proteins. This enzymatic activity contributes to post-translational protein modifications. FNTA Protein, Human (His, Strep) is the recombinant human-derived FNTA protein, expressed by E. coli , with N-Strep, N-6*His labeled tag.
CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL . CP-609754 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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