|S1501||Mycophenolate Mofetil||<1 mg/mL||86 mg/mL||<1 mg/mL|
|S2776||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|
|S5425||Phenylglyoxal hydrate||-1 mg/mL||30 mg/mL||-1 mg/mL|
|S5097||Methotrexate disodium||99 mg/mL||<1 mg/mL||-1 mg/mL|
|S1158||MK-8245||<1 mg/mL||93 mg/mL||<1 mg/mL|
|S1680||Disulfiram||<1 mg/mL||59 mg/mL||59 mg/mL|
|S8076||PluriSIn #1 (NSC 14613)||<1 mg/mL||43 mg/mL||<1 mg/mL|
|S2376||Ammonium Glycyrrhizinate||5 mg/mL||168 mg/mL||<1 mg/mL|
|S2055||Gimeracil||<1 mg/mL||29 mg/mL||<1 mg/mL|
|S8382||ML390||<1 mg/mL||81 mg/mL||60 mg/mL|
|S4116||Isovaleramide||<1 mg/mL||20 mg/mL||20 mg/mL|
|S7900||SW033291||<1 mg/mL||83 mg/mL||32 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-Acetic acid||<1 mg/mL||100 mg/mL||10 mg/mL|
|S3652||3-Nitropropionic acid||23 mg/mL||23 mg/mL||23 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|
|S8619||NCT-503||<1 mg/mL||81 mg/mL||81 mg/mL|
|S8205||AG-221 (Enasidenib)||<1 mg/mL||94 mg/mL||94 mg/mL|
|S5800||Alda 1||<1 mg/mL||65 mg/mL||12 mg/mL|
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.
Natural killer cell activation is differentially modulated by treatment with CsA,Tac, Sir, or MMF. PBMC of three or four healthy donors were incubated for 4 days with or without 500 U/ml IL-2 in the presence CNI (CsA and Tac), mTORi (Sir), or mycophenolate (MMF) at a concentration of 10 µM, DMSO control solvent or medium.The percentage of all NK cells (CD3− /CD56+ ) and of the major NK cell subsets deﬁned as CD16+ /CD16− CD56dim and CD56bright were determined by ﬂow cytometry. Each data point indicates one donor, and the median values with standard deviations are depicted as black bars.
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. Phase 2.
Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent.
Peritoneal macrophages were pretreated for 1 h with the leﬂunomide (100 umol/L), followed by treatment with 10 ug/ml rTsP53 for 6 h. Western blot analysis of P-STAT6 and STAT6 expression was performed. Corresponding staining for b-actin was carried out to control for equal loading. *P < 0.05 versus control group, #P < 0.05 versus rTsP53 group.
Mycophenolic acid is a potent IMPDH inhibitor and the active metabolite of an immunosuppressive drug, used to prevent rejection in organ transplantation.
AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.
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.
Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.
MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. Phase 2.
Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.
The effect of drugs on sperm movement. Purified human sperm were incubated under capacitating conditions for 0, 15, 30, 60 or 120 min, and motility was measured in the presence of disulfirum. The standard deviation is shown as bars. Statistical differences by Student's t-test compared with control are annotated as “*” for p<0.05 or “**” for p<0.01.
PluriSIn #1 is an inhibitor of the stearoyl-coA desaturase 1 (SCD1), which is able to selectively eliminate hPSCs.
Ammonium Glycyrrhizinate inhibits growth and cytopathology of several unrelated DNA and RNA viruses.
Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.
ML390 is a human DHODH inhibitor that induces differentiation in acute myeloid leukemia.
3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.
Isovaleramide is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases.
SW033291 is a selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) with IC50 and Kiapp of 1.5 nM and 0.1 nM, respectively.
AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.
NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
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.
Daidzin, 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).
Vidofludimus is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Phase 2.
Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica).
Trypsin inhibition dose-response curves in the absence (black circles) and presence (red triangles) of detergent for (A) emodin.
Enoxolone is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb liquorice.
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).
Western blot analysis of TLR2 and CXCR4 after direct inhibition with glycyrrhizin.
Gossypol Acetate is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes such as lactate dehydrogenase, NAD-linked enzymes.
Weight gain of Spodoptera littoralis larvae on combined Cry proteins and gossypol. Weight gain (mg ± SE) of 2nd instar S. littoralis after feeding for one week on diet containing different concentrations of Cry proteins, gossypol, or a combination of both. Control = diet with added PBST; C1 = Cry1Ac 0.05 + Cry2Ab2 1.6 pmol/g; C3 = Cry1Ac 0.52 + Cry2Ab2 16.4 pmol/g; C4 = Cry1Ac 1.7 + Cry2Ab2 54.5 pmol/g; G3 = 1.3 μmol/g gossypol. Asterisks indicate significant difference to the control diet using a GLM with gamma distribution followed by Dunnett`s Test (n = 53-60). *** p ≤ 0.001.
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.
Fomepizole 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.
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 a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.
Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).
Gilteritinib(ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).
Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.
Alda 1 is an ALDH2 agonist that activates catalysis for both wild-type ALDH2 (ALDH2*1) and ALDH2*2.