Dehydrogenase

Epostane acts as an antiprogestogen and terminates pregnancy by inhibiting 3β-hydroxysteroid dehydrogenase and preventing the biosynthesis of progesterone and pregnenolone. [4]

FX-11 (LDHA Inhibitor FX11) is A potent, selective and competitive specific inhibitor of lactate dehydrogenase A (LDHA) with a Ki of 8 μM. FX-11 can activate PKM2 (pyruvate kinase M2). FX-11 can reduce ATP levels, induce oxidative stress and ROS production, and cause cell death. FX-11 appeared antitumor activity during xenotransplantation of lymphoma and pancreatic cancer.

Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. It specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of the oncometabolite 2-hydroxyglutarate (2 hG), which may induce cellular differentiation and inhibit cellular proliferation in IDH1-expressing tumor cells.

Olorofim（F-901318）is a novel selective antifungal compound targeting pyrimidine biosynthesis in mycobacteria, with inhibitory effect on Aspergillus fumigatus DHODH (IC50: 44 nM), but little inhibitory effect on human DHODH (>100 uM).Olorofim has good efficacy against a variety of pathogenic filamentous and dimorphic fungi, such as Penicillium spp, P. dermatitidis spp and Fusarium spp.

Succinyl phosphonate trisodium salt is an inhibitor of α-ketoglutarate dehydrogenase (KGDHC).

Disulfiram (TETD) is an inhibitor of the acetaldehyde dehydrogenase ALDH, inhibiting hALDH1 and hALDH2 (IC50=0.15 1.45 μM) with specificity. Disulfiram is acutely sensitized to alcohol and also inhibits GSDMD pore formation.

A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.

Manitimus (FK778) is an inhibitor of dehydroorotate dehydrogenase and an immunosuppressant with immunosuppressive and antiproliferative activity, prevents vascular remodeling after mechanical endothelial injury, and can be used to study immune dysfunction.

Sodium Oxamate (Oxamic acid sodium salt) is an LDH inhibitor that specifically inhibits LDHA. Sodium Oxamate has antitumor activity and induces cell cycle arrest and apoptosis.

Galloflavin is a lactate dehydrogenase inhibitor that inhibits the activity of lactate dehydrogenase. Galloflavin inhibits both human LDH isoforms (type A and type B) by preferentially binding to the free enzyme without competing with substrates or cofactors, with Ki values ​​calculated by pyruvate of 5.46 μM (LDH-A) and 15.06 μM (LDH-B).

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM).

Devimistat (6,8-Bis(benzylthio)octanoic acid) , a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts tumor cell mitochondrial metabolism. It has potential chemopreventive and antineoplastic activities, and has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Advanced Cancer, and Pancreatic Cancer, among others.

LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor.

Leflunomide (HWA486) is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis.

HSD-016 is an orally active, selective and potent type 1 11β-hydroxysteroid dehydrogenase (11β-HSD1) inhibitor with strong inhibitory effects on human, mouse and rat 11β-HSD1.HSD-016 can be used in the study of diabetes and metabolic syndrome.

CPS-11 (N-(Hydroxymethyl)thalidomide) is a Thalidomide analogue with significant antitumor activity, exhibiting a broader and more potent effect on the MM (multiple myeloma) cell line.

RRx-001 is a potent inhibitor ofglucose 6-phosphate dehydrogenase(G6PD) and with potent antimalarial activity

DS-1001b is an inhibitor of mutant IDH-1 (Isocitrate Dehydrogenase-1)

4-Hydroxynonenal (4-HNE) (4-HNE) is an oxidative nitrosative stress biomarker. It is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2).

BAY-2402234 is an inhibitor of dihydroorotate dehydrogenase (DHODH) for the treatment of myeloid malignancies.BAY 2402234 is a selective low-nanomolar inhibitor of human DHODH enzymatic activity.

Perfluorooctanoic acid (PFOA) (PFOA) is a persistent and widespread industry-made chemical.

Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.

Brequinar (NSC-368390) is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.

IMB-XMA0038 is a novel inhibitor targeting Mycobacterium tuberculosis aspartate semialdehyde dehydrogenase with antimicrobial activity for use in tuberculosis research.

alpha-Mangostin (Mangostin) is a natural xanthonoid, a type of organic compound isolated from various parts of the mangosteen tree.

CP-642931 (Sorbitol dehydrogenase-IN-1) is an orally active and highly potent sorbitol dehydrogenase inhibitor for the study of diabetes and cardiovascular disease.

Enasidenib (AG-221) is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity.

CAY10566 shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM). CAY10566 is a potent, orally bioavailable and selective stearoyl

NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=2.5 µM) with no activity against other dehydrogenases. NCT-503 has antitumor activity and inhibits the growth of PHGDH-dependent tumors.

MK-8245 is a liver-targeting SCD inhibitor for human SCD1 (IC50: 1 nM) and for rat/mouse SCD1 (IC50: 3 nM), with anti-diabetic and anti-dyslipidemic function.

IMPDH2-IN-2 is a potent inhibitor of inosine 5'-monophosphate dehydrogenase (IMPDH) (Ki,app: 14 μM) and a potential anti-tuberculosis agent, exhibiting moderate antibacterial effects with MIC values of 6.3 and 11 μM in minimal GAST Fe and rich 7H9 ADC Tween media, respectively.

SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues.

(R)-GNE-140 (GNE-140) is an effective LDHA LDHB inhibitor (IC50s: 3 5 nM) and is 18-fold more potent than S enantiomer.

Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a peripherally selective dopamine beta-hydroxylase inhibitor that reduces hypertension.

GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) with IC50 values of 1.9 nM for LDHA and 14 nM for LDHB.

Daidzin (Daidzoside) is an isoflavone isolated from soya bean with anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities.

Glycyrrhizic acid (Glycyrrhizin) is a triterpenoid saponinl with anti-tumor and anti-diabetic activities.

Alda-1 is an ALDH2 agonist, a cell-permeable activator of both the wild-type ALDH2*1 and the Asian E487K mutant ALDH2*2 forms of mitochondrial aldehyde dehydrogenase 2 (mtALDH2).

KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.

G6PDi-1 is an effective G6PD inhibitor. It depletes NADPH and decreases inflammatory cytokine production.

1. Prunetin (Prunusetin) significantly reduces serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide. 2. Prunetin mediates anti-obesity adipogenesis effects by suppressing obesity-related transcription through a feedback mechanism that regulates the expression of adiponectin, adipoR1, adipoR2, and AMPK. 3. Prunetin and biochanin A are potent reducers of NF-κB and ERK activation, zonula occludens 1 tyrosine phosphorylation, and metalloproteinase-mediated shedding activity, which may account for the barrier-improving ability of these isoflavones. 4. Prunetin significantly suppresses ATP-induced mucin secretion from cultured RTSE cells; Prunetin inhibits the production of MUC5AC mucin protein induced by EGF or PMA from NCI-H292 cells; Prunetin also inhibits the expression of MUC5AC mucin gene induced by EGF or PMA from NCI-H292 cells.

MF-438 is an effective and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor (EC50: 2.3 nM for rSCD1).

hDHODH-IN-4 (DHODH-IN-5) is a potent inhibitor of human dihydrogen dehydrogenase (DHODH). For human recombinant DHODH, its pIC50 is 7.8. hDHODH-IN-4 inhibits measles virus replication with a pMIC50 of 8.8.

Vidofludimus (SC12267) (4SC-101, SC12267) is a novel small molecule inhibitor of dihydroorotate dehydrogenase (DHODH).

LDH-IN-1 is a pyrazole-based human lactate dehydrogenase (LDH) inhibitor(IC50s of 32 and 27 nM for LDHA and LDHB, respectively).

Isoniazid (Isonicotinic hydrazide) is an antibacterial agent used primarily as a tuberculostatic.

AVN-944 (VX-944)(VX-944) is a selective, noncompetitive inhibitor of human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.