Dihydroorotate Dehydrogenase Inhibitor

BRD9185 is a Dihydroorotate dehydrogenase (DHODH) inhibitor, with an EC₅₀ of 16 nM against multidrug-resistant blood-stage parasites in vitro and is curative after just three doses in a P. berghei mouse model.

DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs. DSM705 is a potent antimalarial compound.

Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR.

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 K_is of 0.016 μM and 5.6 μM, respectively. DHODH-IN-8 has antimalarial activity.

DHODH-IN-32 (Compound A1) is a DHODH inhibitor. DHODH-IN-32 shows significant cytotoxicity against NCI-60 cell lines, especially being sensitive to breast cancer, prostate cancer and leukemia cell lines. DHODH-IN-32 can induce cell apoptosis by activating the Caspase pathway. DHODH-IN-32 causes G0/G1 phase cell cycle arrest and inhibits cellular metabolism by ROS. DHODH-IN-32 exhibits significant anti-tumor properties in mouse breast cancer models. DHODH-IN-32 can be used for the study of breast cancer.

DHODH-IN-20 (Compound 133) is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-20 inhibits tumor growth. DHODH-IN-20 has the potential for the research of acute myelogenous leukemia.

DHODH-IN-29 (Compound 2i) is a covalent inhibitor of Leishmania braziliensis Dihydroorotate Dehydrogenase (LbDHODH) with an IC₅₀ value of 0.5 μM. DHODH-IN-29 is promising for research of antileishmaniasis.

Leflunomide-d₄ (HWA486-d₄) is the deuterium labeled Leflunomide. Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic agent.

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 K_i^app of 32 nM. DHODH-IN-3 has the potential for malaria treatment.

DHODH-IN-12 (Compound 12b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pK_a of 5.07.

RORγt/DHODH-IN-1 (compound (R)-14d) is a potent and orally active dual RORγt/DHODH inhibitor, with IC₅₀s of 0.083 μM and 0.172 μM, respectively. RORγt/DHODH-IN-1 exhibits remarkable in vivo anti-inflammatory activity.

RORγt/DHODH-IN-3 (compound (S)-14d) is a dual RORγt/DHODH inhibitor, with IC₅₀s of 0.098 μM and 0.432 μM, respectively. RORγt/DHODH-IN-3 exhibits remarkable in vivo anti-inflammatory activity.

hDHODH-IN-11 is a potent human dihydroorotate dehydrogenase (hDHODH) inhibitor with an IC₅₀ value of 7.2 nM. hDHODH-IN-11 has low cytotoxicity. hDHODH-IN-11 can be used in research of acute myeloid leukemia (AML).

PfDHODH-IN-3 (compound 2) is an orally active PfDHODH inhibitor with strong antimalarial activity (IC₅₀=47 nM). PfDHODH-IN-3 can inhibit the growth of Plasmodium in animals.

hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC₅₀ of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC₅₀ of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy.

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.

hDHODH-IN-10 is a selective, potent and orally active hDHODH inhibitor, with an IC₅₀ value of 10.9 nM. hDHODH-IN-10 forms hydrogen bonds with key residues Arg136 and Gln47. hDHODH-IN-10 inhibits the proliferation of cancer cells. hDHODH-IN-10 can be used in the research of cancers, such as AML, colorectal cancer.

RORγt/DHODH-IN-2 (compound 1) is a potent dual RORγt/DHODH inhibitor. RORγt/DHODH-IN-2 can be used for inflammatory bowel disease (IBD) research.

DHODH-IN-18 is a human DHODH inhibitor (IC₅₀ = 0.2 nM).

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.