Dihydroorotate Dehydrogenase Inhibitor

P1788 is a dihydroorotate dehydrogenase (DHODH) inhibitor. P1788 induces DNA damage.

Leflunomide (Standard) is the analytical standard of Leflunomide. This product is intended for research and analytical applications. Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic agent.

ML390 (Standard) is the analytical standard of ML390 (HY-100688). This product is intended for research and analytical applications. 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.

DHODH-IN-34 (Compound 21q) is a potent human dihydroorotate dehydrogenase (DHODH) inhibitor with an IC₅₀ value of 13 nM. DHODH-IN-34 is promising for research of RNA viruses such as measles virus and chikungunya virus.

Olorofim (Standard) is the analytical standard of Olorofim (HY-104029). This product is intended for research and analytical applications. 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..

hDHODH-IN-17 (Compound 10) is a human dihydroorotate dehydrogenase (hDHODH) inhibitor, with an IC₅₀ of 0.188 μM. hDHODH-IN-17 is in good agreement with the hDHODH activity pocket and interacted well with amino acid residues. hDHODH-IN-17 is the potential broad-spectrum antiviral agent.

DSM267 is a triazolopyrimidine inhibitor of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH), with an IC₅₀ of 38 nM, while its IC₅₀ against human DHODH exceeds 100000 nM. DSM267 is used for the in vitro systematic screening and characterization of the resistance evolution pathways of Plasmodium falciparum to DHODH inhibitors.

Leflunomide-¹³C₆ (HWA486-¹³C₆) is ¹³C labeled Leflunomide. Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic agent.

Genz-669178 is an inhibitor for dihydroorotate dehydrogenase (DHODH) with IC₅₀ of 0.015-0.05 μM in Plasmodium spp.. Genz-669178 inhibits P. berghei, P. falciparum strains 3D7 and Dd2 with IC₅₀ of 0.068, 0.008 and 0.01 μM, respectively. Genz-669178 exhibits anti-malarial efficacy in P. berghei-infected mice with ED₅₀ of 13-21 mg/kg/day. Genz-669178 exhibits good pharmacokinetic characteristics in mice.

Brequinar-d₃ (DUP785-d₃) is deuterium labeled Brequinar. 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.

Laflunimus (Standard) is the analytical standard of Laflunimus. This product is intended for research and analytical applications. 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.

RORγ/DHODH-IN-1 (compound 1404), a deuterium labeled compound, is a dual RORγ and DHODH inhibitor with IC₅₀ values of 9.7 nM and 100 nM, repaectively. RORγ/DHODH-IN-1 blocks the replication of SARS-CoV-2, HCMV, and non-enveloped DNA virus (HAdV5).

SARS-CoV-2-IN-115 (Compound 3e) is a SARS-CoV-2 inhibitor. SARS-CoV-2-IN-115 has potent antiviral activity against SARS-CoV-2 in infected Calu-3 cells (EC₅₀: 1.7  μM). SARS-CoV-2-IN-115 effectively inhibits the activity of human dihydroorotate dehydrogenase (HsDHODH) (IC₅₀: 1.5  μM). SARS-CoV-2-IN-115 preserves immune response without antiproliferative effects on CD4 T cells .

DSM-421 is an orally active Dihydroorotate dehydrogenase inhibitor. DSM-421 has antiplasmodium activity.

S-8660 is an orally active and selective inhibitor of dihydroorotate dehydrogenase (DHODH). S-8660 is an analog of Brequinar (HY-108325) and exhibits immunosuppressive activity. When combined with Cyclosporin A (HY-B0579), it enhances the effect of prolonging cardiac allograft survival. S-8660 can be used for research on cardiac transplant rejection.

RORγ/DHODH-IN-2 (Compound 1311) is an orally active dual inhibitor of RORγ/DHODH with IC₅₀ values of 11.9 nM and 90 nM, respectively. RORγ/DHODH-IN-2 exhibits antiviral activity by inhibiting the activity of SARS-CoV-2, HCMV, HAdV5, and MPXV, with IC₅₀ values of 27 nM, 20 nM, 9.1 nM, and 1.8 nM, respectively.

Lapachol (Standard) is the analytical standard of Lapachol. This product is intended for research and analytical applications. 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.

DHODH-IN-30 (compound 4g) is a potent human dihydroorotate dehydrogenase (hDHODH) inhibitor with an IC₅₀ of 32 nM. DHODH-IN-30 exhibits protective effects against oxidative stress.

BRD7539 is a PfDHODH inhibitor (IC₅₀ = 0.033 μM). BRD7539 has potent activity against both multidrug-resistant asexual blood-stage (P. falciparum, Dd2 strain, EC₅₀ = 0.010 μM) and liver-stage (P. berghei, EC₅₀ = 0.015 μM) parasites.

Redoxal is a dihydroorotate dehydrogenase (DHODH) inhibitor and anti-HIV-1 agent. Redoxal induces intracellular pyrimidine depletion by inhibiting the de novo pyrimidine biosynthesis pathway, enhances the protein stability of APOBEC3G (A3G), upregulates the abundance of A3G protein in cells and progeny viral particles, thereby strengthening the host endogenous antiviral restriction mediated by A3G. Redoxal selectively targets DHOdehase at the mitochondrial level, with an IC₅₀ of 430 nM for inhibiting DHO oxidation in human mitochondria and an IC₅₀ of 910 nM in rat mitochondria. Redoxal can be used in studies related to HIV-1 infection.