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Farnesyl Pyrophosphate ammonium salt, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate ammonium salt is a TRPM2 (TRP Channel) agonist, and activates TRPM2 opening for ion influx. Farnesyl pyrophosphate ammonium salt is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
Farnesyl pyrophosphate (Farnesyl diphosphate), a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
Farnesyl acetate is a sesquiterpene isolated from the leaves of Amomum gagnepainii. Farnesyl acetate has significant toxicity against red palm weevil larvae with a LD50 of 7867 ppm .
Farnesyl thiosalicylic acid amide (FTS-A) is an orally active derivative of farnesyl thiosalicylic acid (HY-14754). Farnesyl thiosalicylic acid amide reduces Ras-GTP levels and inhibits cell growth with IC50s of 20 and 10 μM for Panc-1 and U87 cells, respectively. Farnesyl thiosalicylic acid amide can be used for the research of cancer .
S-Farnesyl thioacetic acid is an analog of S-farnesyl cysteine, which is a prenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase) competitive inhibitors. It also inhibits the methylation of farnesylated and geranylgeranylated substrates.
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site .
NE21650 potently inhibits farnesyl diphosphate (FPP) synthase. NE21650 is a weak inhibitor of isopentenyl diphosphate (IPP) isomerase. NE21650 is a potent inhibitor of protein prenylation in osteoclasts and macrophages and bone resorption in vitro .
FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity .
ICMT-IN-21 (compound 6ag) is an ICMT inhibitor (IC50=8.8 μM), a sulfonamide-modified farnesyl cysteine (SMFC). The farnesyl and carboxylic acid motifs of ICMT-IN-21 are important structures for inhibiting ICMT .
NE 10790, a poor farnesyl pyrophosphate synthase inhibitor, is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak antiresorptive agent.
H-Met-OiPr hydrochloride is an Methionine derivative. H-Met-OiPr hydrochloride participates in the synthesis preparation of inhibitors of farnesyl-protein transferase (FTase), and can be used in cancer research .
Alendronic acid, a bisphosphonate, is a farnesyl diphosphate synthase (FDPS) inhibitor. Alendronic acid inhibits osteoclast-mediated bone resorption. Alendronic acid shows efficacy in postmenopausal osteoporosis, malignant hypercalcemia and Paget’s disease .
Alendronate prodrug-1(compound 2) is an inhibitor of farnesyl diphosphate synthase (FPPS). Alendronate prodrug-1 has an antiproliferative effect with an IC50 value of 34.0 μM .
MMV019313 is a potent, non-bisphosphonate inhibitor of farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) with an IC50 of 0.82 µM. MMV019313 has activity against P. falciparum (Parasite) .
Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras) .
FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 can inhibit hepatitis delta virus (HDV) infection.
FTI-277 hydrochloride is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 hydrochloride can inhibit hepatitis delta virus (HDV) infection.
K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM .
Alendronic acid-d6 is the deuterium labeled Alendronic acid. Alendronic acid, a bisphosphonate, is a farnesyl diphosphate synthase (FDPS) inhibitor. Alendronic acid inhibits osteoclast-mediated bone resorption. Alendronic acid shows efficacy in postmenopausal osteoporosis, malignant hypercalcemia and Paget’s disease[1].
BPH-1358 (NSC50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL) .
Arglabin ((+)-Arglabin), a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor. Arglabin shows anti-inflammatory and antitumor activities . The antitumor activity of Arglabin proceeds through its inhibition of farnesyl transferase which leads to the activation of RAS proto-oncogene .
FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively .
Lonafarnib (Sch66336) is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities.
Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway . Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research .
FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively .
BPH-1358 mesylate (NSC50460 mesylate) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively. BPH-1358 mesylate is active against S. aureus in vitro (MIC ~250 ng/mL) .
BPH-1358 free base (NSC50460 free base) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL) .
(Rac)-Lonafarnib (Sch66336 racemate) is the racemate of Lonafarnib. Lonafarnib is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities .
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 .
ICMT-IN-54 (compound 7c) is an adamantyl analogue and an ICMT inhibitor (IC50=12.4 μM), which can inhibit ICMT Methylation. ICMT-in-54 inhibits BFC (N-biotinyl-(6-aminohexanoic)-S-farnesyl-L-cysteine) methylation in saccharomyces cerevisiae expressing ICMT, which is an indirect effect of inhibiting ICMT methylation .
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 .
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
S-Farnesyl thioacetic acid is an analog of S-farnesyl cysteine, which is a prenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase) competitive inhibitors. It also inhibits the methylation of farnesylated and geranylgeranylated substrates.
H-Met-OiPr hydrochloride is an Methionine derivative. H-Met-OiPr hydrochloride participates in the synthesis preparation of inhibitors of farnesyl-protein transferase (FTase), and can be used in cancer research .
Farnesyl Pyrophosphate ammonium salt, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate ammonium salt is a TRPM2 (TRP Channel) agonist, and activates TRPM2 opening for ion influx. Farnesyl pyrophosphate ammonium salt is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
Arglabin ((+)-Arglabin), a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor. Arglabin shows anti-inflammatory and antitumor activities . The antitumor activity of Arglabin proceeds through its inhibition of farnesyl transferase which leads to the activation of RAS proto-oncogene .
Farnesyl pyrophosphate (Farnesyl diphosphate), a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
Farnesyl acetate is a sesquiterpene isolated from the leaves of Amomum gagnepainii. Farnesyl acetate has significant toxicity against red palm weevil larvae with a LD50 of 7867 ppm .
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 .
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
FDPS Protein, a key enzyme in isoprenoid biosynthesis, catalyzes the formation of farnesyl diphosphate (FPP). FPP is a precursor for essential metabolites like sterols, dolichols, carotenoids, and ubiquinones. It also serves as a substrate for protein farnesylation and geranylgeranylation. FDPS sequentially condenses isopentenyl pyrophosphate with dimethylallyl pyrophosphate and then with geranylpyrophosphate to produce farnesyl pyrophosphate. FDPS Protein, Human (His) is the recombinant human-derived FDPS protein, expressed by E. coli , with N-His labeled tag. The total length of FDPS Protein, Human (His) is 353 a.a., with molecular weight of ~41 kDa.
FDPS proteins are key enzymes in isoprenoid biosynthesis and play a crucial role in the formation of farnesyl diphosphate (FPP). FPP is a precursor of essential metabolites involved in protein farnesylation and geranylgeranylation. FDPS Protein, Mouse (His) is the recombinant mouse-derived FDPS protein, expressed by E. coli , with N-His labeled tag. The total length of FDPS Protein, Mouse (His) is 353 a.a., with molecular weight of ~42.8 kDa.
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. The total length of FDFT1 Protein, Human (His) is 416 a.a., with molecular weight of ~52 kDa.
The GGPS1 protein is responsible for catalyzing the trans-addition of three molecules of isopentenyl pyrophosphate (IPP) to dimethylallyl pyrophosphate (DMAPP) to synthesize geranylgeranyl pyrophosphate. This compound is an important precursor for the biosynthesis of carotenoids and geranylated proteins. GGPS1 Protein, Human (His) is the recombinant human-derived GGPS1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of GGPS1 Protein, Human (His) is 300 a.a., with molecular weight of ~35.0 kDa.
Alendronic acid-d6 is the deuterium labeled Alendronic acid. Alendronic acid, a bisphosphonate, is a farnesyl diphosphate synthase (FDPS) inhibitor. Alendronic acid inhibits osteoclast-mediated bone resorption. Alendronic acid shows efficacy in postmenopausal osteoporosis, malignant hypercalcemia and Paget’s disease[1].
