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Dehydrogenase
Isoform-selective Products
Signaling Pathway
Dehydrogenase Products
- All (71)
- Dehydrogenase Inhibitors (70)
- Dehydrogenase Agonist (1)
- New Dehydrogenase Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S1680 | Disulfiram | Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD). |
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| S2302 | Glycyrrhizin (NSC 167409) | Glycyrrhizin (NSC 167409, Glycyrrhizic Acid) is a direct HMGB1(high mobility group box 1) inhibitor that inhibits HMGB1-dependent inflammatory molecule expression and oxidative stress; modulates P38 and P-JNK but not p-ERK signalling; Also inhibits 11 beta-hydroxysteroid dehydrogenase and monoamine oxidase (MAO). |
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| S2776 | Devimistat (CPI-613) | Devimistat (CPI-613), a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. CPI-613 induces apoptosis in pancreatic cancer cells. Phase 2. | ||
| S4169 | Teriflunomide | Teriflunomide (A77 1726, HMR-1726) is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent. |
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| S5097 | Methotrexate disodium | Methotrexate sodium, an analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis. | ||
| S2303 | Gossypol Acetate | Gossypol Acetate (Gossypol Acetic acid, Pogosin, AT101) is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes such as lactate dehydrogenase, NAD-linked enzymes. |
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| S8205 | Enasidenib (AG-221) | Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme. | ||
| S1247 | Leflunomide | Leflunomide is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR. |
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| S2295 | Emodin | Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica). |
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| S7185 | AGI-5198 | AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM. |
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| S8206 | Ivosidenib (AG-120) | Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. |
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| S7241 | AGI-6780 | AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM. |
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| S8615 | DCA (Sodium dichloroacetate) | DCA (Sodium dichloroacetate), a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na+-K+-2Cl- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth. | ||
| S1501 | Mycophenolate mofetil | Mycophenolate mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. Mycophenolate Mofetil induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells. |
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| S2487 | Mycophenolic acid | Mycophenolic acid (Mycophenolate, RS-61443) is a potent IMPDH inhibitor and the active metabolite of an immunosuppressive drug, used to prevent rejection in organ transplantation. | ||
| S1404 | Trilostane | Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome. |
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|
| S9783 | 6AN (6-Aminonicotinamide) | 6AN (6-Aminonicotinamide) is an antimetabolite used to inhibit the NADPH-producing pentose phosphate pathway (PPP) in many cellular systems, making them more susceptible to oxidative stress. 6-Aminonicotinamide is a competitive inhibitor of NADP+-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) with Ki of 0.46 μM. | ||
| S8619 | NCT-503 | NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with the IC50 value of 2.5 μM. It is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs. | ||
| S8000 | Tenovin-1 | Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH). |
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| S6626 | Brequinar | Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro. | ||
| S4900 | Tenovin-6 | Tenovin-6 is a small molecule activator of p53 transcriptional activity and inhibits dihydroorotate dehydrogenase (DHODH). Tenovin-6 is also an inhibitor of SirT1 and SirT2. | ||
| S7900 | SW033291 | SW033291 is a selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) with IC50 and Ki of 1.5 nM and 0.1 nM, respectively. | ||
| S8405 | RRx-001 | RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. RRx-001 triggers apoptosis and exhibits anticancer activity.RRx-001 is also a downregulator of the CD47- SIRPα checkpoint pathway. | ||
| S6852 | Gossypol | Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells. | ||
| S9721 | Farudodstat | Farudodstat(LAS 186323,ASLAN003) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors. |
||
| S8847 | Orludodstat (BAY 2402234) | Orludodstat (BAY 2402234) is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM. | ||
| S4929 | Enasidenib(AG-221) Mesylate | Enasidenib (AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2). | ||
| S7262 | Vidofludimus | Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2. | ||
| S1717 | Fomepizole | Fomepizole (4-methylpyrazole, Antizol, Antizol-Vet) is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. | ||
| S8611 | Vorasidenib (AG-881) | Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2). | ||
| S2376 | Ammonium Glycyrrhizinate | Ammonium Glycyrrhizinate (AMGZ, Glycyram, Glycyrrhizin ammonium salt, Glycyrrhizic acid ammonium salt) is a unique product from Licorice root with a very high sweetness. Ammonium glycyrrhizinate is a direct inhibitor of HMGB1 with anti-inflammatory, anti-tumor, anti-diabetic activities. Ammonium Glycyrrhizinate inhibits growth and cytopathology of several unrelated DNA and RNA viruses. Ammonium Glycyrrhizinate also inhibits both hepatic delta 4-5-reductase and 11 beta-hydroxysteroid dehydrogenase. | ||
| S6675 | (R)-GNE-140 | (R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer. | ||
| S6689 | Merimepodib | Merimepodib (Merimempodib, MMPD, VI-21,497, VX-497) is a potent, specific, and reversible inosine monophosphate dehydrogenase(IMPDH) inhibitor with antiviral activity against hepatitis C virus (HCV) and a variety of DNA and RNA viruses in vitro.Merimepodib is an immunosuppressive agent. | ||
| S0209 | BVT 2733 | BVT 2733, a new small molecule, is a non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1). | ||
| S2055 | Gimeracil | Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair. | ||
| S0718 | AG-120 (racemic) | AG-120 (racemic), the racemic mixture of AG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. | ||
| S8382 | ML390 | ML390 is a human DHODH inhibitor with an IC50 of 0.56 μM and induces differentiation in acute myeloid leukemia. | ||
| S5800 | Alda 1 | Alda 1 is an ALDH2 agonist that activates catalysis for both wild-type ALDH2 (ALDH2*1) and ALDH2*2. | ||
| S7941 | NCT-501 | NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM. | ||
| S9617 | G6PDi-1 | G6PDi-1 is an effective inhibitor of glucose-6-phosphate dehydrogenase (G6PD). G6PDi-1 depletes NADPH and decreases inflammatory cytokine production. | ||
| S2296 | Enoxolone | Enoxolone (Glycyrrhetin) is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb liquorice. | ||
| S3565 | Brequinar Sodium | Brequinar Sodium (Bipenquinate, BRQ, DUP-785, NSC 368390) is a potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of ~20 nM and triggers differentiation in the ER-HoxA9, U937, and THP1 cells with ED50 of ~1 μM. | ||
| S3804 | Alpha-Mangostin | Alpha-mangostin is the main xanthone purified from mangosteen and has health promoting benefits including anti-bacterial, anti-inflammatory, anti-oxidant, anti-cancer and cardioprotective activities. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Alpha-mangostin is also an agonist of human STING. | ||
| S8590 | GSK 2837808A | GSK2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively. | ||
| S8530 | BAY 1436032 | BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants. | ||
| S2987 | 4-Methyl-2-oxovaleric acid | 4-Methyl-2-oxovaleric acid (Ketoleucine, 4-MOV, KIC, 4-Methyl-2-oxopentanoic acid, alpha-Ketoisocaproic acid, alpha-ketoisocaproate, 2-Oxoisohexanoate) is released by Astrocytes to neurons and can be reaminated by aminotransferase to leucine. 4-Methyl-2-oxovaleric acid reduces the rate of protein degradation in skeletal muscle. 4-Methyl-2-oxovaleric acid acts as an uncoupler of oxidative phosphorylation (OXPHOS) and as a metabolic inhibitor possibly through its inhibitory effect on alpha-ketoglutarate dehydrogenase (oxoglutarate dehydrogenase complex, OGDC) activity. | ||
| S3993 | Ethyl Vanillate | Ethyl vanillin (Bourbonal, Ethylprotal), a vanillin analog, is a flavouring agent and a fungicidal agent that exhibits strong antioxidant activity. Ethyl Vanillate inhibits 17β-HSD2 with an IC50 1.3 µM. | ||
| S6749 | ASP-9521 | ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5). | ||
| E0355 | CVT-10216 | CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 with an IC50 of 29 nM. | ||
| S5146 | 3-Methylpyrazole | 3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase. | ||
| E4704New | D34-919 | D34-919 is potent inhibitor of the ALDH1A3-PKM2 interaction, and prevents the ALDH1A3-mediated enhancement of PKM2 tetramerization. D34-919 mediated in vitro and in vivo treatment enhances and restores chemoradiotherapy-induced apoptosis and sensitivity in glioblastoma (GBM) cells. | ||
| S0522 | CM10 | CM10 is a potent and selective inhibitor of aldehyde dehydrogenase 1A family (ALDH1A) with IC50 of 1700 nM, 740 nM and 640 nM for ALDH1A1, ALDH1A2 and ALDH1A3, respectively. CM10 exhibits anti-cancer activity. | ||
| S0746 | hDHODH-IN-1 | hDHODH-IN-1 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with anti-inflammatory effect. | ||
| S0747 | DHODH-IN-11 | DHODH-IN-11 is a Leflunomide derivative and a weak inhibitor of dihydroorotate dehydrogenase (DHODH). | ||
| S4116 | Isovaleramide | Isovaleramide(3-Methylbutanamide) is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases. | ||
| S9776 | AG-636 | AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity. | ||
| S0764 | AKR1C1-IN-1 | AKR1C1-IN-1 is a potent and selective inhibitor of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) with Ki of 4 nM, 87 nM, 4.2 μM and 18.2 μM for AKR1C1, AKR1C2, AKR1C3 and AKR1C4, respectively. | ||
| S9645 | CBR-5884 | CBR-5884 is a selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and was selectively toxic to cancer cell lines with high serine biosynthetic activity. | ||
| E1078 | Emvododstat (PTC299) | Emvododstat(PTC299), a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells PTC299 inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM. | ||
| S2289 | Daidzin | Daidzin (Daidzoside, Daidzein 7-O-glucoside, Daidzein 7-glucoside), a natural organic compound in the class of phytochemicals known as isoflavones, is a potent and selective inhibitor of human mitochondrial aldehyde dehydrogenase and inhibits ALDH-I selectively (Ki=20 nM); at least 500 times less effective against ALDH-Ⅱ, the cytosolic isozyme (Ki=10 μM). | ||
| S6222 | Ethyl potassium malonate | Ethyl potassium malonate (Potassium 3-ethoxy-3-oxopropanoate) is used as a competitive inhibitor of the enzyme succinate dehydrogenase. It acts as a precursor to produce (trimethylsilyl)ethyl malonate, which is utilized to prepare beta-ketoesters by acylation and serves as an intermediate for the preparation of ethyl tert-butyl malonate. | ||
| E0788 | PfDHODH-IN-2 | PfDHODH-IN-2, a dihydrothiophenone derivative, is a potent Plasmodium falciparum dihydroorotate dehydrogenase (pfDHODH) inhibitor with an IC50 of 1.11 µM, acting as an antimalarial agent which can be used for the research of malaria. | ||
| S3652 | 3-Nitropropionic acid (3-NP) | 3-Nitropropionic acid (3-NP) is an irreversible inhibitor of mitochondrial respiratory Complex II succinate dehydrogenase, resulting in energy depletion through disruption of the electron transport chain. | ||
| S7994New | GSK864 | GSK864 is a cell-penetrant, potent, and selective inhibitor of isocitrate dehydrogenase 1 (IDH1) mutants, specifically targeting the R132C, R132H, and R132G variants with IC50 values of 8.8 nM, 15.2 nM, and 16.6 nM, respectively. | ||
| E1875New | BI-3231 | BI-3231 is the potent and selective chemical probe, which inhibits hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) with an IC50 of 1 nM and Ki of 0.7 nM in the enzymatic assay. It has the potential to treat NASH and other liver diseases. | ||
| S3574 | IDH-305 | IDH-305 (Compound 13) is an orally available, mutant-selective and brain-penetrant inhibitor of isocitrate dehydrogenase 1 (IDH1) that targets IDH1(R132) mutation with IC50 of 27 nM, 28 nM and 6.14 μM for IDH1R132H, IDH1R132C and IDH1WT, respectively. | ||
| S4805 | Carboxine | Carboxin (Carbathiin, Vitavax, Kisvax) is a systemic agricultural fungicide and seed protectant. Carboxin inhibits succinate dehydrogenaseactivity . | ||
| S8949 | Olutasidenib | Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively. | ||
| E1170 | R162 | R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties. | ||
| S8881 | DS-1001b (DS 1001) | DS-1001b is an oral selective inhibitor of mutant IDH1 R132X with potential antineoplastic activity and is designed to penetrate the blood-brain barrier. | ||
| S5425 | Phenylglyoxal hydrate | Phenylglyoxal (1-Phenylethanedione) is a potent inhibitor of mitochondrial aldehyde dehydrogenase. It reacts with arginine residues in purified Hageman factor (HF, Factor XII) and causes inhibition of its coagulant properties. | ||
| S1680 | Disulfiram | Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD). |
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| S2302 | Glycyrrhizin (NSC 167409) | Glycyrrhizin (NSC 167409, Glycyrrhizic Acid) is a direct HMGB1(high mobility group box 1) inhibitor that inhibits HMGB1-dependent inflammatory molecule expression and oxidative stress; modulates P38 and P-JNK but not p-ERK signalling; Also inhibits 11 beta-hydroxysteroid dehydrogenase and monoamine oxidase (MAO). |
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| S2776 | Devimistat (CPI-613) | Devimistat (CPI-613), a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. CPI-613 induces apoptosis in pancreatic cancer cells. Phase 2. | ||
| S4169 | Teriflunomide | Teriflunomide (A77 1726, HMR-1726) is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent. |
|
|
| S5097 | Methotrexate disodium | Methotrexate sodium, an analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis. | ||
| S2303 | Gossypol Acetate | Gossypol Acetate (Gossypol Acetic acid, Pogosin, AT101) is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes such as lactate dehydrogenase, NAD-linked enzymes. |
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|
| S8205 | Enasidenib (AG-221) | Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme. | ||
| S1247 | Leflunomide | Leflunomide is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR. |
|
|
| S2295 | Emodin | Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica). |
|
|
| S7185 | AGI-5198 | AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM. |
|
|
| S8206 | Ivosidenib (AG-120) | Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. |
|
|
| S7241 | AGI-6780 | AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM. |
|
|
| S8615 | DCA (Sodium dichloroacetate) | DCA (Sodium dichloroacetate), a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na+-K+-2Cl- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth. | ||
| S1501 | Mycophenolate mofetil | Mycophenolate mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. Mycophenolate Mofetil induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells. |
|
|
| S2487 | Mycophenolic acid | Mycophenolic acid (Mycophenolate, RS-61443) is a potent IMPDH inhibitor and the active metabolite of an immunosuppressive drug, used to prevent rejection in organ transplantation. | ||
| S1404 | Trilostane | Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome. |
|
|
| S9783 | 6AN (6-Aminonicotinamide) | 6AN (6-Aminonicotinamide) is an antimetabolite used to inhibit the NADPH-producing pentose phosphate pathway (PPP) in many cellular systems, making them more susceptible to oxidative stress. 6-Aminonicotinamide is a competitive inhibitor of NADP+-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) with Ki of 0.46 μM. | ||
| S8619 | NCT-503 | NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with the IC50 value of 2.5 μM. It is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs. | ||
| S8000 | Tenovin-1 | Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH). |
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| S6626 | Brequinar | Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro. | ||
| S4900 | Tenovin-6 | Tenovin-6 is a small molecule activator of p53 transcriptional activity and inhibits dihydroorotate dehydrogenase (DHODH). Tenovin-6 is also an inhibitor of SirT1 and SirT2. | ||
| S7900 | SW033291 | SW033291 is a selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) with IC50 and Ki of 1.5 nM and 0.1 nM, respectively. | ||
| S8405 | RRx-001 | RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. RRx-001 triggers apoptosis and exhibits anticancer activity.RRx-001 is also a downregulator of the CD47- SIRPα checkpoint pathway. | ||
| S6852 | Gossypol | Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells. | ||
| S9721 | Farudodstat | Farudodstat(LAS 186323,ASLAN003) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors. |
||
| S8847 | Orludodstat (BAY 2402234) | Orludodstat (BAY 2402234) is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM. | ||
| S4929 | Enasidenib(AG-221) Mesylate | Enasidenib (AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2). | ||
| S7262 | Vidofludimus | Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2. | ||
| S1717 | Fomepizole | Fomepizole (4-methylpyrazole, Antizol, Antizol-Vet) is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. | ||
| S8611 | Vorasidenib (AG-881) | Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2). | ||
| S2376 | Ammonium Glycyrrhizinate | Ammonium Glycyrrhizinate (AMGZ, Glycyram, Glycyrrhizin ammonium salt, Glycyrrhizic acid ammonium salt) is a unique product from Licorice root with a very high sweetness. Ammonium glycyrrhizinate is a direct inhibitor of HMGB1 with anti-inflammatory, anti-tumor, anti-diabetic activities. Ammonium Glycyrrhizinate inhibits growth and cytopathology of several unrelated DNA and RNA viruses. Ammonium Glycyrrhizinate also inhibits both hepatic delta 4-5-reductase and 11 beta-hydroxysteroid dehydrogenase. | ||
| S6675 | (R)-GNE-140 | (R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer. | ||
| S6689 | Merimepodib | Merimepodib (Merimempodib, MMPD, VI-21,497, VX-497) is a potent, specific, and reversible inosine monophosphate dehydrogenase(IMPDH) inhibitor with antiviral activity against hepatitis C virus (HCV) and a variety of DNA and RNA viruses in vitro.Merimepodib is an immunosuppressive agent. | ||
| S0209 | BVT 2733 | BVT 2733, a new small molecule, is a non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1). | ||
| S2055 | Gimeracil | Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair. | ||
| S0718 | AG-120 (racemic) | AG-120 (racemic), the racemic mixture of AG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. | ||
| S8382 | ML390 | ML390 is a human DHODH inhibitor with an IC50 of 0.56 μM and induces differentiation in acute myeloid leukemia. | ||
| S7941 | NCT-501 | NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM. | ||
| S9617 | G6PDi-1 | G6PDi-1 is an effective inhibitor of glucose-6-phosphate dehydrogenase (G6PD). G6PDi-1 depletes NADPH and decreases inflammatory cytokine production. | ||
| S2296 | Enoxolone | Enoxolone (Glycyrrhetin) is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb liquorice. | ||
| S3565 | Brequinar Sodium | Brequinar Sodium (Bipenquinate, BRQ, DUP-785, NSC 368390) is a potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of ~20 nM and triggers differentiation in the ER-HoxA9, U937, and THP1 cells with ED50 of ~1 μM. | ||
| S3804 | Alpha-Mangostin | Alpha-mangostin is the main xanthone purified from mangosteen and has health promoting benefits including anti-bacterial, anti-inflammatory, anti-oxidant, anti-cancer and cardioprotective activities. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Alpha-mangostin is also an agonist of human STING. | ||
| S8590 | GSK 2837808A | GSK2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively. | ||
| S8530 | BAY 1436032 | BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants. | ||
| S2987 | 4-Methyl-2-oxovaleric acid | 4-Methyl-2-oxovaleric acid (Ketoleucine, 4-MOV, KIC, 4-Methyl-2-oxopentanoic acid, alpha-Ketoisocaproic acid, alpha-ketoisocaproate, 2-Oxoisohexanoate) is released by Astrocytes to neurons and can be reaminated by aminotransferase to leucine. 4-Methyl-2-oxovaleric acid reduces the rate of protein degradation in skeletal muscle. 4-Methyl-2-oxovaleric acid acts as an uncoupler of oxidative phosphorylation (OXPHOS) and as a metabolic inhibitor possibly through its inhibitory effect on alpha-ketoglutarate dehydrogenase (oxoglutarate dehydrogenase complex, OGDC) activity. | ||
| S3993 | Ethyl Vanillate | Ethyl vanillin (Bourbonal, Ethylprotal), a vanillin analog, is a flavouring agent and a fungicidal agent that exhibits strong antioxidant activity. Ethyl Vanillate inhibits 17β-HSD2 with an IC50 1.3 µM. | ||
| S6749 | ASP-9521 | ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5). | ||
| E0355 | CVT-10216 | CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 with an IC50 of 29 nM. | ||
| S5146 | 3-Methylpyrazole | 3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase. | ||
| E4704New | D34-919 | D34-919 is potent inhibitor of the ALDH1A3-PKM2 interaction, and prevents the ALDH1A3-mediated enhancement of PKM2 tetramerization. D34-919 mediated in vitro and in vivo treatment enhances and restores chemoradiotherapy-induced apoptosis and sensitivity in glioblastoma (GBM) cells. | ||
| S0522 | CM10 | CM10 is a potent and selective inhibitor of aldehyde dehydrogenase 1A family (ALDH1A) with IC50 of 1700 nM, 740 nM and 640 nM for ALDH1A1, ALDH1A2 and ALDH1A3, respectively. CM10 exhibits anti-cancer activity. | ||
| S0746 | hDHODH-IN-1 | hDHODH-IN-1 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with anti-inflammatory effect. | ||
| S0747 | DHODH-IN-11 | DHODH-IN-11 is a Leflunomide derivative and a weak inhibitor of dihydroorotate dehydrogenase (DHODH). | ||
| S4116 | Isovaleramide | Isovaleramide(3-Methylbutanamide) is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases. | ||
| S9776 | AG-636 | AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity. | ||
| S0764 | AKR1C1-IN-1 | AKR1C1-IN-1 is a potent and selective inhibitor of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) with Ki of 4 nM, 87 nM, 4.2 μM and 18.2 μM for AKR1C1, AKR1C2, AKR1C3 and AKR1C4, respectively. | ||
| S9645 | CBR-5884 | CBR-5884 is a selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and was selectively toxic to cancer cell lines with high serine biosynthetic activity. | ||
| E1078 | Emvododstat (PTC299) | Emvododstat(PTC299), a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells PTC299 inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM. | ||
| S2289 | Daidzin | Daidzin (Daidzoside, Daidzein 7-O-glucoside, Daidzein 7-glucoside), a natural organic compound in the class of phytochemicals known as isoflavones, is a potent and selective inhibitor of human mitochondrial aldehyde dehydrogenase and inhibits ALDH-I selectively (Ki=20 nM); at least 500 times less effective against ALDH-Ⅱ, the cytosolic isozyme (Ki=10 μM). | ||
| S6222 | Ethyl potassium malonate | Ethyl potassium malonate (Potassium 3-ethoxy-3-oxopropanoate) is used as a competitive inhibitor of the enzyme succinate dehydrogenase. It acts as a precursor to produce (trimethylsilyl)ethyl malonate, which is utilized to prepare beta-ketoesters by acylation and serves as an intermediate for the preparation of ethyl tert-butyl malonate. | ||
| E0788 | PfDHODH-IN-2 | PfDHODH-IN-2, a dihydrothiophenone derivative, is a potent Plasmodium falciparum dihydroorotate dehydrogenase (pfDHODH) inhibitor with an IC50 of 1.11 µM, acting as an antimalarial agent which can be used for the research of malaria. | ||
| S3652 | 3-Nitropropionic acid (3-NP) | 3-Nitropropionic acid (3-NP) is an irreversible inhibitor of mitochondrial respiratory Complex II succinate dehydrogenase, resulting in energy depletion through disruption of the electron transport chain. | ||
| S7994New | GSK864 | GSK864 is a cell-penetrant, potent, and selective inhibitor of isocitrate dehydrogenase 1 (IDH1) mutants, specifically targeting the R132C, R132H, and R132G variants with IC50 values of 8.8 nM, 15.2 nM, and 16.6 nM, respectively. | ||
| E1875New | BI-3231 | BI-3231 is the potent and selective chemical probe, which inhibits hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) with an IC50 of 1 nM and Ki of 0.7 nM in the enzymatic assay. It has the potential to treat NASH and other liver diseases. | ||
| S3574 | IDH-305 | IDH-305 (Compound 13) is an orally available, mutant-selective and brain-penetrant inhibitor of isocitrate dehydrogenase 1 (IDH1) that targets IDH1(R132) mutation with IC50 of 27 nM, 28 nM and 6.14 μM for IDH1R132H, IDH1R132C and IDH1WT, respectively. | ||
| S4805 | Carboxine | Carboxin (Carbathiin, Vitavax, Kisvax) is a systemic agricultural fungicide and seed protectant. Carboxin inhibits succinate dehydrogenaseactivity . | ||
| S8949 | Olutasidenib | Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively. | ||
| E1170 | R162 | R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties. | ||
| S8881 | DS-1001b (DS 1001) | DS-1001b is an oral selective inhibitor of mutant IDH1 R132X with potential antineoplastic activity and is designed to penetrate the blood-brain barrier. | ||
| S5425 | Phenylglyoxal hydrate | Phenylglyoxal (1-Phenylethanedione) is a potent inhibitor of mitochondrial aldehyde dehydrogenase. It reacts with arginine residues in purified Hageman factor (HF, Factor XII) and causes inhibition of its coagulant properties. | ||
| S5800 | Alda 1 | Alda 1 is an ALDH2 agonist that activates catalysis for both wild-type ALDH2 (ALDH2*1) and ALDH2*2. | ||
| E4704New | D34-919 | D34-919 is potent inhibitor of the ALDH1A3-PKM2 interaction, and prevents the ALDH1A3-mediated enhancement of PKM2 tetramerization. D34-919 mediated in vitro and in vivo treatment enhances and restores chemoradiotherapy-induced apoptosis and sensitivity in glioblastoma (GBM) cells. | ||
| S7994New | GSK864 | GSK864 is a cell-penetrant, potent, and selective inhibitor of isocitrate dehydrogenase 1 (IDH1) mutants, specifically targeting the R132C, R132H, and R132G variants with IC50 values of 8.8 nM, 15.2 nM, and 16.6 nM, respectively. | ||
| E1875New | BI-3231 | BI-3231 is the potent and selective chemical probe, which inhibits hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) with an IC50 of 1 nM and Ki of 0.7 nM in the enzymatic assay. It has the potential to treat NASH and other liver diseases. |
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Tags: Dehydrogenase inhibition | Dehydrogenase activity | Dehydrogenase assay | Dehydrogenase reaction | Dehydrogenase enzyme activity | pyruvate dehydrogenase inhibition | pyruvate dehydrogenase activity | pyruvate dehydrogenase assay | pyruvate dehydrogenase phosphorylation | pyruvate dehydrogenase cancer | pyruvate dehydrogenase pathway | pyruvate dehydrogenase activation | dihydropyrimidine dehydrogenase activity | stearoyl-CoA desaturase pathway | Dehydrogenase inhibitor review
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