fpps

BPH-1358 (NSC-50460) (NSC-50460) 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 it is active against S. aureus in vitro (MIC ~250 ng/mL)[1][2].

Pamidronate Disodium (CGP 23339A), a nitrogen-containing bisphosphonate, can help to strengthen bones.

Ibandronic acid (Bonviva) is a third-generation amino-bisphosphonate with anti-resorptive and anti-hypercalcemic activities.

NE 10790 (3-PEHPC) is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak anti-resorptive agent. Although NE10790 was a poor inhibitor of FPP synthase

TH-Z145 is a potent FPPS inhibitor for the study of myeloma and lung cancer.

FPPS-IN-11 is a potent inhibitor of farnesyl pyrophosphate synthase (FPPS) that effectively blocks a key enzymatic step in the mevalonate pathway, thereby modulating downstream isoprenoid biosynthesis, protein prenylation processes, and cholesterol-associated signaling pathways that are critically involved in cell proliferation, immune regulation, and metabolic disease progression.

FPPS ligand 3 (compound 2) is a ligand of farnesyl pyrophosphate synthase (FPPS). It binds to the hydrophobic base region of the FPPS pocket and is utilized in the design and synthesis of FPPS inhibitors.

FPPS-IN-2 (compound 4a) is an effective orally active HFPPS inhibitor with an IC50 value of 1.108 µM, showing potential for use in osteoporosis research.

Alendronate sodium hydrate (MK 217) is a nitrogen-containing bisphosphonate, which is an effective inhibitor of bone resorption. It is utilized for the treatment and prevention of osteoporosis.

BPH-1358 (NSC50460) free base is a potent human undecaprenyl diphosphate synthase (UPPS) and farnesyl diphosphate synthase (FPPS) inhibitor (IC50s: 110 nM and 1.8 μM) and is active against S. aureus in vitro (MIC ~250 ng/mL).

Alendronate prodrug-1 (compound 2) is an inhibitor of farnesyl diphosphate synthase (FPPS) and exhibits antiproliferative activity with an IC50 value of 34.0 μM.

Monosodium neridronate is an amino-containing bisphosphonate bone resorption inhibitor. Binding with high affinity to hydroxyapatite surfaces, it induces osteoclast apoptosis by strongly inhibiting farnesyl pyrophosphate synthase (FPPS) activity, demonstrating outstanding efficacy in models of osteogenesis imperfecta and Paget's disease.

RAM1147 is an inhibitor of farnesyl pyrophosphate synthase (FPPS). It disrupts the isoprenylation process of proteins, thereby inhibiting tumor cell proliferation. RAM1147 shows potential for research in cancer (such as myeloma and breast cancer) as well as in bone metabolic disorders (such as osteoporosis).

Alendronate sodium is a nitrogen-containing bisphosphonate that inhibits bone resorption. Alendronate sodium interferes with the mevalonate pathway by inhibiting farnesyl-3-phosphate (FPP) synthase in osteoclasts, thereby blocking osteoclast activity and inducing their apoptosis. Sodium alendronate is used in the treatment of metabolic bone diseases such as osteoporosis and Paget’s disease of bone.

BPH-1358 mesylate (NSC50460 mesylate), a highly effective inhibitor of both human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS), exhibits IC50 values of 1.8 μM and 110 nM, respectively. Additionally, this compound demonstrates potent in vitro activity against S. aureus, with a minimum inhibitory concentration (MIC) approximately 250 ng/mL.

TH-Z93 is a potent FPPS inhibitor (IC50:90 nM) and a lipophilic bisphosphonate.