hDHODH-IN-9 (Compound 3k) is a potent inhibitor of hDHODH with an IC50 of 0.34 μM. hDHODH-IN-9 demonstrates high cytotoxic activity against MCF-7 and A375 cells and good selectivity. hDHODH-IN-9 has the potential for the research of cancer diseases[1].
DHODH-IN-11 (Compound 14b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.03[1].
D-Lactate dehydrogenase (D-LDH) is an oxidoreductase that uses NAD+ or NADP+ as an acceptor and acts on the donor CH-OH group, and can catalyze the oxidation of D-lactate to pyruvate. D-Lactate dehydrogenase widely exists in bacteria and fungi, and is often used in biochemical research[1].
DHODH-IN-12 (Compound 12b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.07[1].
Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
Isomalt (Palatinitol), a well-tolerated, non-toxic polyol and a protein-stabilizing excipient, stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying, and performs better during storage. Isomalt is traditionally used as a sweetening agent in the food industry and as a tabletting excipient for pharmaceutical purposes[1].
RS6212 is a specific LDH (lactate dehydrogenase) inhibitor with an IC50 value of 12.03 μM . RS6212 inhibits tumor growth and exhibits potent anticancer activity in multiple cancer cell lines[1].
DHODH-IN-15 (Compound 7b) is a hydroxyfurazan analog of A771726. DHODH-IN-15 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 11 μM for rat liver DHODH. DHODH-IN-15 can be used for rheumatoid arthritis[1].
3-Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-Dehydrotrametenolic acid induces apoptosis and has anticancer activity[1][2].
CHK-336 (Example 1) is an orally active LDHA inhibitor (IC50<1 nM) that inhibits lactate production in mouse hepatocytes. CHK-336 can be used in the study of hyperoxaluria[1].
DHODH-IN-4 (compound 17) is a human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) inhibitor, with IC50 values of 4 μM and 0.18 μM for PfDHODH and HsDHODH, respectively. DHODH-IN-4 (compound 17) possess antimalarial activity[1].
DHODH-IN-13 (Compound 7a) is a hydroxyfurazan analog of A771726. DHODH-IN-13 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for rat liver DHODH. DHODH-IN-13 can be used for rheumatoid arthritis[1].
LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression[1].
DHODH-IN-5 is a potent human dihydroorotate dehydrogenase (DHODH) inhibitor, with a pIC50 of 7.8 for human recombinant DHODH. DHODH-IN-5 inhibits measles virus replication, with a pMIC50 of 8.8[1].
hDHODH-IN-2 is an analogue of the active metabolite of Leflunomide. hDHODH-IN-2 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory activity[1][2].
FX-11 is a potent LDH-A inhibitor with an IC50 of 23.3 μM for HeLa cell，a Ki value of 8 μM.
Anticancer agent 122, an inhibitor of human lactate dehydrogenase A enzyme (hLDHA), has good anticancer activities and can be used for anticancer research[1].
DHODH-IN-1 (compound 18d) is a potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 25 nM. DHODH-IN-1 is an inhibitor of pyrimidine biosynthesis pathway[1].
GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. (R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor.
DHODH-IN-14 (Compound 7l) is a hydroxyfurazan analog of A771726. DHODH-IN-14 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.49 μM for rat liver DHODH. DHODH-IN-14 can be used for rheumatoid arthritis[1].
DHODH-IN-9 (Compound 10k) is an azine-bearing analogue and is a human dihydroorotate dehydrogenase inhibitor. DHODH-IN-9 has antiviral effect with a pMIC50 of 7.4[1].
DHODH-IN-8 (Compound 27) is an inhibitor of human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM, and Kis of 0.016 μM and 5.6 μM, respectively. DHODH-IN-8 has antimalarial activity[1].
DHODH-IN-3 (compound 3) is a potent inhibitor of Human Dihydroorotate Dehydrogenases (HsDHODH) with an IC50 value of 261 nM. DHODH-IN-3 binds to the the ubiquinone binding cavities in DHODH with a Kiapp of 32 nM. DHODH-IN-3 has the potential for malaria treatment[1].
PfDHODH-IN-1 is an analogue of the active metabolite of Leflunomide. PfDHODH-IN-1 is a Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor. PfDHODH-IN-1 has antimalarial activity[1][2].
Anticancer agent 121, an inhibitor of human lactate dehydrogenase A enzyme (hLDHA), has good anticancer activities and can be used for anticancer research[1].
Nedosiran sodium is a GalNAc-dsRNA conjugate designed to inhibit production of the hepatic lactate dehydrogenase (LDH) enzyme.
DHODH-IN-2 (compound 21d) is a human dihydroorotate dehydrogenase (HsDHODH) inhibitor, inhibits measles virus replication with a pMIC50 value of 8.6[1].
hDHODH-IN-1 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory effect[1].
DHODH-IN-7 is a human dihydroorotate dehydrogenase (DHODH) inhibitor, with an IC50 of 0.91 μM. DHODH-IN-7 induces differentiation in acute myeloid leukemia[1].
Oxamic acid (oxamate) sodium salt is a lactate dehydrogenase-A (LDH-A) inhibitor. Oxamic acid sodium salt shows anti-tumor activity, and anti-proliferative activity against cancer cells, and can induce apoptosis[1][2][3].