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シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1501 Mycophenolate Mofetil <1 mg/mL 86 mg/mL ''<1 mg/mL
S2776 Devimistat (CPI-613) <1 mg/mL 77 mg/mL '''77 mg/mL
S1247 Leflunomide <1 mg/mL 54 mg/mL ''54 mg/mL
S2487 Mycophenolic acid <1 mg/mL 64 mg/mL '5 mg/mL
S7185 AGI-5198 <1 mg/mL 24 mg/mL '14 mg/mL
S6852 Gossypol <1 mg/mL 100 mg/mL ''8 mg/mL
S8590 GSK 2837808A <1 mg/mL 100 mg/mL ''''<1 mg/mL
S9617 G6PDi-1 <1 mg/mL 57 mg/mL '''<1 mg/mL
S0718 AG-120 (racemic) <1 mg/mL 100 mg/mL ''100 mg/mL
S0209 BVT 2733 ˂1 mg/mL 86 mg/mL '3 mg/mL
S6689 Merimepodib <1 mg/mL 90 mg/mL '<1 mg/mL
S8949 Olutasidenib (FT-2102) <1 mg/mL 71 mg/mL <1 mg/mL
S6675 (R)-GNE-140 <1 mg/mL 100 mg/mL '<1 mg/mL
S8847 BAY 2402234 <1 mg/mL 100 mg/mL 33 mg/mL
S6749 ASP-9521 <1 mg/mL 66 mg/mL 66 mg/mL
S6626 Brequinar <1 mg/mL 37 mg/mL <1 mg/mL
S8881 DS-1001b (DS 1001) <1 mg/mL 14 mg/mL <1 mg/mL
S1680 Disulfiram <1 mg/mL 59 mg/mL '''''59 mg/mL
S1404 Trilostane <1 mg/mL 65 mg/mL '<1 mg/mL
S8000 Tenovin-1 <1 mg/mL 74 mg/mL '<1 mg/mL
S4169 Teriflunomide <1 mg/mL 32 mg/mL ',1 mg/mL
S2055 Gimeracil <1 mg/mL 29 mg/mL <1 mg/mL
S3993 Ethyl Vanillate -1 mg/mL 39 mg/mL -1 mg/mL
S8382 ML390 <1 mg/mL 81 mg/mL 60 mg/mL
S5097 Methotrexate disodium 99 mg/mL <1 mg/mL -1 mg/mL
S4116 Isovaleramide <1 mg/mL 20 mg/mL 20 mg/mL
S4900 Tenovin-6 98 mg/mL 98 mg/mL '<1 mg/mL
S7900 SW033291 <1 mg/mL 83 mg/mL 32 mg/mL
S2376 Ammonium Glycyrrhizinate 5 mg/mL 168 mg/mL '''<1 mg/mL
S7241 AGI-6780 <1 mg/mL 96 mg/mL 96 mg/mL
S7941 NCT-501 <1 mg/mL 32 mg/mL 25 mg/mL
S8405 RRx-001 <1 mg/mL 53 mg/mL '23 mg/mL
S2289 Daidzin <1 mg/mL 83 mg/mL 4 mg/mL
S7262 Vidofludimus <1 mg/mL 100 mg/mL ''''1 mg/mL
S2295 Emodin <1 mg/mL 54 mg/mL 2 mg/mL
S2296 Enoxolone <1 mg/mL 94 mg/mL <1 mg/mL
S2302 Glycyrrhizin (Glycyrrhizic Acid) <1 mg/mL 100 mg/mL 100 mg/mL
S2303 Gossypol Acetate <1 mg/mL 100 mg/mL 10 mg/mL
S3652 3-Nitropropionic acid 23 mg/mL 23 mg/mL 23 mg/mL
S1717 Fomepizole ' mg/mL
S8615 Sodium dichloroacetate (DCA) 30 mg/mL 30 mg/mL '''30 mg/mL
S8611 Vorasidenib (AG-881) <1 mg/mL 82 mg/mL 82 mg/mL
S8206 Ivosidenib (AG-120) <1 mg/mL 100 mg/mL 100 mg/mL
S4805 Carboxine -1 mg/mL 47 mg/mL '-1 mg/mL
S8619 NCT-503 <1 mg/mL 81 mg/mL 81 mg/mL
S3804 Alpha-Mangostin -1 mg/mL 82 mg/mL -1 mg/mL
S8205 Enasidenib (AG-221) <1 mg/mL 94 mg/mL 94 mg/mL
S5425 Phenylglyoxal hydrate -1 mg/mL 30 mg/mL -1 mg/mL
S8530 BAY 1436032 <1 mg/mL 98 mg/mL 98 mg/mL
S5800 Alda 1 <1 mg/mL 65 mg/mL 12 mg/mL

Dehydrogenase製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1501

Mycophenolate Mofetil

Mycophenolate Mofetil (RS61443) 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.

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.

S1247

Leflunomide

Leflunomide (HWA486) 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.

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.

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.

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.

S8590

GSK 2837808A

GSK 2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively.

S9617

G6PDi-1

G6PDi-1 is an effective inhibitor of glucose-6-phosphate dehydrogenase (G6PD). G6PDi-1 depletes NADPH and decreases inflammatory cytokine production.

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.

S0209

BVT 2733

BVT 2733, a new small molecule, is a non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

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.

S8949

Olutasidenib (FT-2102)

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.

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.

S8847

BAY 2402234

BAY 2402234 is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM.

S6749

ASP-9521

ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5).

S6626

Brequinar

Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.

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.

S1680

Disulfiram

Disulfiram (NSC 190940) 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.

S1404

Trilostane

Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.

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).

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.

S2055

Gimeracil

Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.

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.

S8382

ML390

ML390 is a human DHODH inhibitor that induces differentiation in acute myeloid leukemia.

S5097

Methotrexate disodium

Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.

S5146

3-Methylpyrazole

3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.

S4116

Isovaleramide

Isovaleramide is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases.

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 Kiapp of 1.5 nM and 0.1 nM, respectively.

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.

S7241

AGI-6780

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.

S7941

NCT-501

NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.

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.

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).

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.

S2295

Emodin

Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica).

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.

S2302

Glycyrrhizin (Glycyrrhizic Acid)

Glycyrrhizin (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).

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.

S3652

3-Nitropropionic acid

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.

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.

S8615

Sodium dichloroacetate (DCA)

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.

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).

S8206

Ivosidenib (AG-120)

Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.

S4805

Carboxine

Carboxin (Carbathiin, Vitavax, Kisvax) is a systemic agricultural fungicide and seed protectant.

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.

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.

S8205

Enasidenib (AG-221)

Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.

S5425

Phenylglyoxal hydrate

Phenylglyoxal 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.

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.

S5800

Alda 1

Alda 1 is an ALDH2 agonist that activates catalysis for both wild-type ALDH2 (ALDH2*1) and ALDH2*2.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1501

Mycophenolate Mofetil

Mycophenolate Mofetil (RS61443) 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.

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.

S1247

Leflunomide

Leflunomide (HWA486) 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.

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.

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.

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.

S8590

GSK 2837808A

GSK 2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively.

S9617

G6PDi-1

G6PDi-1 is an effective inhibitor of glucose-6-phosphate dehydrogenase (G6PD). G6PDi-1 depletes NADPH and decreases inflammatory cytokine production.

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.

S0209

BVT 2733

BVT 2733, a new small molecule, is a non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

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.

S8949

Olutasidenib (FT-2102)

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.

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.

S8847

BAY 2402234

BAY 2402234 is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM.

S6749

ASP-9521

ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5).

S6626

Brequinar

Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.

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.

S1680

Disulfiram

Disulfiram (NSC 190940) 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.

S1404

Trilostane

Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.

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).

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.

S2055

Gimeracil

Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.

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.

S8382

ML390

ML390 is a human DHODH inhibitor that induces differentiation in acute myeloid leukemia.

S5097

Methotrexate disodium

Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.

S5146

3-Methylpyrazole

3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.

S4116

Isovaleramide

Isovaleramide is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases.

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 Kiapp of 1.5 nM and 0.1 nM, respectively.

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.

S7241

AGI-6780

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.

S7941

NCT-501

NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.

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.

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).

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.

S2295

Emodin

Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica).

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.

S2302

Glycyrrhizin (Glycyrrhizic Acid)

Glycyrrhizin (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).

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.

S3652

3-Nitropropionic acid

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.

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.

S8615

Sodium dichloroacetate (DCA)

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.

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).

S8206

Ivosidenib (AG-120)

Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.

S4805

Carboxine

Carboxin (Carbathiin, Vitavax, Kisvax) is a systemic agricultural fungicide and seed protectant.

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.

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.

S8205

Enasidenib (AG-221)

Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.

S5425

Phenylglyoxal hydrate

Phenylglyoxal 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.

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.

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S5800

Alda 1

Alda 1 is an ALDH2 agonist that activates catalysis for both wild-type ALDH2 (ALDH2*1) and ALDH2*2.

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