isomerase

AY 9944 is a specific cholesterol biosynthesis inhibitor that targets the 7-dehydrocholesterol Δ7-reductase (DHCR7) enzyme (IC50=13 nM). At high doses, AY 9944 also inhibits sterol Δ7-Δ8 isomerase in cultured embryos, leading to the accumulation of cholest-8-en-3β-ol[1][2][3]. Additionally, AY 9944 causes hypocholesterolemia and accumulation of 7DHC.

6-Phosphogluconic acid is a potent and competitive inhibitor of phosphoglucose isomerase (PGI), with an apparent Ki of 0.048 mM for glucose 6-phosphate and 0.042 mM for fructose 6-phosphate as the substrate.

ML359 is a protein disulfide isomerase inhibitor.

Glucose 6-phosphate isomerase (GPI), also known as phosphoglucose isomerase phosphoglucoisomerase (PGI) or phosphohexose isomerase (PHI), is a highly conserved glycolytic and dimeric enzyme often used in biochemical studies that catalyzes the reversible isomerization of glucose-6-phosphate to fructose-6-phosphate [1].

Triosephosphate isomerase (TPI), a glycolytic enzyme, efficiently catalyzes the interconversion between dihydroxyacetone phosphate and D-glyceraldehyde-3-phosphate. The catalytic site of TPI is located at the dimer interface [1].

Phosphomannose isomerase, the initial enzyme in GDP-Man biosynthesis, catalytically facilitates the interconversion of fructose-6-phosphate (Fru6P) and mannose-6-phosphate (Man6P), playing a crucial role in cell wall synthesis and protein glycosylation. It is also recognized as a significant antifungal target against threats from A. flavus [1].

Protein disulfide isomerase is a biochemical reagent that serves as either a biomaterial or organic compound in life science research.

Peptidylprolyl isomerase is a biochemical reagent that serves as a biomaterial or organic compound for research in the life sciences.

Phosphoglucose isomerase, bacillus stearothermophilus, is a highly conserved glycolytic enzyme and dimerase. It catalyzes the isomerization of glucose-6-phosphate into fructose-6-phosphate.

Phosphoglucose isomerase, bacillus stearothermophilus, is a highly conserved glycolytic enzyme and dimerase. It catalyzes the isomerization of glucose-6-phosphate into fructose-6-phosphate.

Topoisomerase II inhibitor 13 inhibits topoisomerase II (Topo II) that shows strong anti-proliferation activity against HL-60/MX2 cancer cells derived from HL-60 against Topo II toxicity.

Compound EN300-20599, with CAS No. 16346-97-7, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound EN300-20599 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

Topoisomerases ribosomes-IN-1 (compound 30f) serves as an inhibitor targeting both ribosomes and topoisomerases, specifically exhibiting inhibitory actions against constitutively macrolide-resistant bacteria. This compound effectively suppresses bacterial protein synthesis (IC 50 : 0.647 μM) and hampers DNA replication (IC 50 : 0.218 μM).

Topoisomerase inhibitor4 (compound 45) acts as an effective inhibitor of Topoisomerase1 2, arresting the cell cycle at the G2 M phase and inducing Apoptosis. This compound exhibits potent antitumor activity.

TopoisomeraseI II inhibitor 5 (compound 1) stabilizes G4 structures through binding and concurrently inhibits the relaxation activities of TopoI and II.

TopoisomeraseI II inhibitor 6 (compound 3i) acts as an effective inhibitor of topoisomerase I and II, with IC50 values of 4.77 µM and 15 µM, respectively. Additionally, it exhibits antiproliferative activity against the human melanoma cell line LOX IMVI, demonstrating IC50 values of 26.7 µM and 25.4 µM.

TopoisomeraseII Inhibitor 20 TFA is a potent inhibitor of topoisomerase II with an IC50 of 0.98 µM. It can induce cell apoptosis and exhibits broad-spectrum anticancer activity.

TopoisomeraseI inhibitor 17 (Compound 7h) is an inhibitor of TopoisomeraseI (Top1). It reduces DDX5 and reverses the locking effect of DDX5 on Top1 activity. This compound induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. It triggers apoptosis by decreasing anti-apoptotic proteins XIAP, Bcl-2, and Survivin, while increasing pro-apoptotic proteins Bax and γH2AX. Moreover, TopoisomeraseI inhibitor 17 halts progression at the G2 M checkpoint, leading to cell cycle arrest. It significantly impairs colorectal cancer cell colony formation and migration, and effectively reduces tumor size in human PDX tumor mouse models.

Topoisomerase inhibitor 5 (compound 158) is an inhibitor of bacterial topoisomerase, with a minimum inhibitory concentration of 0.125 μg mL, and exhibits anti-tuberculosis activity.

Compound 5h (Topoisomerase I II inhibitor 7) is a Topoisomerase I II inhibitor.

TopoisomeraseIIα-IN-10 (Compound 13r) is a topoisomerase IIα inhibitor that binds to the active site of DNA when complexed with topoisomerase IIα. This binding is stabilized through interactions with DNA base pairs and amino acid residues. By intercalating into DNA, TopoisomeraseIIα-IN-10 induces apoptosis and disrupts the mitochondrial membrane potential in HCT116 cells, effectively inhibiting their growth with an IC50 of 4.37 μM. It is applicable for cancer research studies.

TopoisomeraseI II inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of TopoisomeraseI II that induces DNA damage and activates PARP-1, leading to the activation of RIPK1, RIPK3, and MLKL, ultimately causing necroptosis. It shows significant anticancer activity by effectively targeting cancer cell nuclei and inducing cell death through necroptosis, offering substantial clinical potential in overcoming resistance in cancer treatment.

Topoisomerase I inhibitor 14 (Compound 4h) acts as an inhibitor of topoisomerase I. It suppresses the proliferation of A549 and C6 cells, with IC50 values of 4.56 μM and 13.17 μM, respectively. The compound shows no significant toxicity towards healthy NIH3T3 cells (IC50 of 74.44 μM) and demonstrates anticancer activity.

TopoisomeraseII/EGFR-IN-1 is a dual inhibitor of topoisomerase II and EGFR, exhibiting strong cytotoxic activity against the MCF-7, A549, and HCT-116 cell lines. It also demonstrates significant apoptotic activity, making it useful for cancer research.