Dihydroorotate Dehydrogenase Inhibitor

Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC₅₀ of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity.

Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic agent.

BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.

Olorofim (F901318) selectively inhibits fungal dihydroorotate dehydrogenase (DHODH), a key enzyme in the pyrimidine biosynthesis pathway. Olorofim (F901318). Olorofim exhibits excellent activity against A. fumigatus and other Aspergillus spp..

Indoluidin D is a selective dihydroorotate dehydrogenase (DHODH) inhibitor with a human DHODH IC₅₀ of 210 nM. Indoluidin D selectively inhibits human DHODH activity, with induced effects rescuable by orotic acid. Indoluidin D promotes myeloid differentiation and inhibits cancer cell proliferation. Indoluidin D can be used for the research of acute promyelocytic leukemia.

MEDS700 is a blood-brain barrier permeable inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC₅₀ of 1.5 nM. MEDS700 induces apoptosis and differentiation, and inhibits proliferation of cancer cells. MEDS700 can be used in research on acute myeloid leukemia and other conditions.

Vidofludimus is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus also can be used for the research of fatty liver by targeting FXR.

Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC₅₀ of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.

PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies.

Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC₅₀s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).

JNJ-74856665 (DHODH-IN-16) is a potent dihydroorotate dehydrogenase (DHODH) inhibitor with an IC₅₀ of 0.396 nM for human DHODH.

Lapachol, a natural naphthoquinone, is an orally active, potent DHODH inhibitor. Lapachol has immunosuppressive activity on lymphocytes through its direct ability to block DHODH activity and inhibit pyrimidine synthesis. Lapachol is a vitamin K antagonist with antitumor activity and can inhibit DNA and RNA synthesis in neoplastic cells. Lapachol has anti-Leishmania activity.

DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC₅₀ of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC₅₀ of 4.3 nM.

ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models.

Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor.

DHODH-IN-17, a 2-anilino nicotinic acid, is a human DHODH inhibitor (IC₅₀=0.40 μM). DHODH-IN-17 can be used for theresearch of acute myeloid leukemia (AML).

Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC₅₀s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH).

Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC₅₀ values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor.

AG-636 is a potent, reversible, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC₅₀ of 17 nM. AG-636 has strong anticancer effects.

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.