synthase

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

Phenylbutazone (Butazolidine) is a butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ankylosing spondylitis, rheumatoid arthritis, and reactive arthritis.

ML406 shows anti-tubercular activity via MtbbioA (DAPA synthase) enzyme inhibition(IC50 : 30 nM)

AT56, a specific inhibitor of prostaglandin D2 synthase enzymatic activity, blunted adipogenic aldosterone effects.

FIN56 is an iron death-specific inducer that binds to and activates squalene synthase, inducing ferroptosis by triggering GPX4 degradation. FIN56 can be used in studies of ferroptosis regulatory mechanisms, autophagy-ferroptosis crosstalk, and tumor therapy.

yGsy2p-IN-1 is a potent inhibitor of yeast glycogen synthase 2 (yGsy2p) and human glycogen synthase 1 (hGYS1). Additionally, yGsy2p-IN-H23, a pyrazole inhibitor, is utilized in the treatment of glycogen storage diseases (GSDs).

G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS).

PF-04802367 is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. It shows desirable central nervous system (CNS) properties and potency. It is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively.

GSK3-IN-1 is a GSK3B-glycogen synthase kinase-3 beta inhibitor.

ATP synthase inhibitor 1 is an inhibitor of the c subunit of the F1/FO-ATP synthase complex. It inhibits mitochondrial permeability transition pore (mPTP) opening and does not affect ATP levels.

Squalene synthase-IN-2 (compound isomer A-(1S, 3R)-14i) is an orally active inhibitor of squalene synthase, with IC50 values of 3.4 nM for squalene synthase and 99 nM for cholesterol synthesis enzymes. Squalene synthase-IN-2 effectively reduces plasma cholesterol and triglycerides.

Chitin synthase-IN-15 (Compound 6k) is an inhibitor of chitin synthase and exhibits insecticidal activity against the diamondback moth (Plutella xylostella) with LC50 values of 0.789 and 0.951 μg/mL. It effectively disrupts molting, causes larval death, and leads to abnormal pupation, resulting in a significant reduction in pest populations. Chitin synthase-IN-15 is considered an insecticide with favorable ecological safety.

S.pombe lumazine synthase-IN-1 is a compound that inhibits lumazine synthases, with Ki values of 243 μM for Schizosaccharomyces pombe and 9.6 μM for Mycobacterium tuberculosis, respectively[1].

Polyketide synthase 13-IN-3 (compound 41) is a potent inhibitor of polyketide synthase 13, with a minimum inhibitory concentration (MIC) range of 0.0625-0.125 μg/mL against the M. tuberculosis strain H37Rv.

Polyketide synthase 13-IN-1 (compound 32) is an inhibitor of polyketide synthase 13.

Phospho-Glycogen Synthase Peptide-2, a substrate for glycogen synthase kinase-3 (GSK-3), serves as a peptide substrate effective in the affinity purification of protein-serine kinases.

Ac-CoA Synthase Inhibitor1 (ACSS2 inhibitor) is the most potent and specific inhibitor of acetate-dependent acetyl-CoA synthetase 2 (ACSS2).

Chitin synthase inhibitor 2 (compound 2b) is a highly potent inhibitor of chitin synthase, with an IC50 of 0.09 mM and a K i of 0.12 mM. This compound exhibits antimicrobial activity in vitro and demonstrates synergistic or additive effects when combined with fluconazole or polyoxin B [1].

Chitin Synthase Inhibitor 3 (Compound 2d) is a potent inhibitor of chitin synthase, exhibiting an IC50 value of 0.16 mM and demonstrating antifungal activity with a minimum inhibitory concentration (MIC) of 1 μg/mL against Candida albicans [1].

Polyketide synthase 13-IN-2 (comp 42) is a potent inhibitor of polyketide synthase 13 in Mycobacterium tuberculosis, demonstrating a minimum inhibitory concentration (MIC) of 0.25 μg/mL [1].

Glucosylceramide synthase-IN-3 (compound BZ1) is a highly potent, brain-penetrant, and orally active inhibitor of glucosylceramide synthase (GCS), with an IC50 value of 16 nM for human GCS, and has potential applications in Gaucher's disease research [1] [2].

GlcN-6-P Synthase-IN-1 (Compound 4d) is a potent inhibitor of Glucosamine-6-phosphate (GlcN-6-P) synthase with an IC50 of 3.47 μM. This compound exhibits remarkable antimicrobial activity, excellent central nervous system penetration, and inhibits cytochrome P450, specifically the CYP3A4 isoform [1].

Chitin synthase inhibitor 1 is a potent and selective chitin synthase (CHS) inhibitor with an IC50 of 0.12 mM, effectively inhibiting drug-resistant fungi variants.

Chitin synthase inhibitor 8 is a chitin synthase (CHS) inhibitor with broad-spectrum antifungal properties, suitable for research on fungal infections.