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squalene synthase inhibitor
RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8??0.2 nM. -
FASN inhibitor
Denifanstat (TVB-2640) is a Fatty Acid Synthase (FASN) inhibitor extracted from patent WO2012122391A1, compound 152, has an IC50 of 0.052 μM and an EC50 of 0.072 μM.
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Cytochrome P450 inhibitor
Talarozole R enantiomer inhibits the metabolism of retinoic acid by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase. -
alpha-glucosidase I inhibitor
Celgosivir is an alpha-glucosidase I inhibitor for the potential treatment of HCV infection. -
PDE9 inhibitor
PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor that increased indicators of hippocampal synaptic plasticity and improved cognitive function in a variety of cognition models in both rats and mice. -
GA mitochondrial matrix inhibitor
Gamitrinib TPP is a GA mitochondrial matrix inhibitor. Gamitrinib TPP is offered as the hexafluorophosphate salt.
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Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor
Rilapladib is a selective Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor with an IC50 of 230 pM. -
ferroptosis inhibitor
Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.- Cheng Chen, .et al. , Neurochem Res, 2025, Mar 18;50(2):122 PMID: 40100474
- Yin-Yin Wang, .et al. , Bioorg Chem, 2025, May:158:108342 PMID: 40058224
- Filiz Bakar-Ates, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2024, Oct 11 PMID: 39392483
- Rushikesh Deshpande, .et al. , Int J Mol Sci, 2024, Jan 18;25(2):1157 PMID: 38256231
- Huan Yang, .et al. , Theriogenology, 2024, Feb:215:281-289 PMID: 38103405
- Filiz Bakar-Ates, .et al. , Toxicol In Vitro, 2024, Feb:94:105732 PMID: 37956772
- Binjie Yan, .et al. , Cell Death Discov, 2023, 9: 456 PMID: 38097554
- Panpan Tai, .et al. , J Transl Med, 2023, Nov 17;21(1):823 PMID: 37978379
- Chengzhu Song, .et al. , Food Funct, 2023, Jan 23;14(2):1087-1098 PMID: 36594456
- Erva Ozkan, .et al. , Life Sci, 2023, Jan 1;312:121222 PMID: 36442526
- Xueyan Zhang, .et al. , DNA Cell Biol, 2022, Aug;41(8):705-715 PMID: 35687364
- A Xavier, .et al. , Cell Rep, 2020, May 19;31(7):107667 PMID: 32433976
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Cathepsin B inhibitor
CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.- Tianming Qiu, .et al. , Cell Death Dis, 2018, Oct; 9(10): 946 PMID: 30237538
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MAO-B inhibitor
Safinamide is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration. -
SGK1 inhibitor
GSK 650394 is a glucocorticoid- and serum-regulated kinase 1 (SGK1) inhibitor which displays antiproliferative properties against the LNCaP prostate carcinoma cell line.- Elif HAZNEDAROGLU BENLIOGLU, .et al. , International Journal of Hematology and Oncology, 2023, 1(33): 37-44
- Qui-Dong Le, .et al. , Arab J Chem, 2022, 16(2):104462
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PDE3 inhibitor
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux. -
HO-1 inhibitor
Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is a competitive heme oxygenase-1 (HO-1) inhibitor, markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2.- Beixian Zhou, .et al. , MedComm, 2024, Apr 12;5(4):e531 PMID: 38617435
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15-LO inhibitor
PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis. -
HSP 70 inhibitor
VER 155008 is a small molecule, ATP-derivative inhibitor of HSP70 (IC50 = 500 nM).- Linglong Yin, .et al. , Oncogene, 2025, Jun;44(21):1567-1577 PMID: 40044984
- Hiroshi Katoh, .et al. , J Virol, 2017, Mar 15; 91(6): e02220-16 PMID: 28053100
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MAO Inhibitor
Bifemelane hydrochloride is an antidepressant MAO inhibitor. Reverses catalepsy induced by tetrabenazine in mice and increases locomotor activity in MPTP-treated marmosets. -
LSD1/BHC110 & MAO inhibitor
Tranylcypromine hydrochloride is a non-selective MAO-A/B inhibitor. -
Cytochrome P450 inhibitor
Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.- Vera-Chang MN, .et al. , Proc Natl Acad Sci U S A, 2018, Dec 10. pii: 201811695 PMID: 30530669
- Tea J, .et al. , J Exp Biol, 2018, Dec 10. pii: jeb.194894 PMID: 30530837
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cathepsin S inhibitor
Petesicatib is a cathepsin S inhibitor, used in research of immune diseases. -
Xanthine oxidase inhibitor
Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout. -
Cathepsin S inhibitor
Z-FL-COCHO (LY3000328) is a novel Cathepsin S inhibitor.
- Gil-Im Mun, .et al. , Biochim Biophys Acta Mol Basis Dis, 2024, Sep 25;1871(1):167523 PMID: 39332782
- Fu R, .et al. , Sci Rep, 2020, Jan 29;10(1):1455 PMID: 31996771
- Klinngam W, .et al. , Sci Rep, 2019, Jul 2;9(1):9559 PMID: 31267034
- Chen CY, .et al. , Clin Sci (Lond), 2018, Oct 29;132(20):2221-2239 PMID: 30287519
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hIDO2 inhibitor
GNF-PF-3777 (8-Nitrotryptanthrin) is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM. -
CYP17A1/androgen synthesis inhibitor
Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues. -
Cathepsin B inhibitor
CA-074 methyl ester is a cell-permeable analog of CA-074 that acts as an irreversible cathepsin B inhibitor. CA-074 methyl ester is reported to inhibit bone resorption in rodent models and shown to inhibit B16 melanoma cell invasion in vitro.- Qian Chu, .et al. , Food Chem Toxicol, 2021, Jan;147:111867 PMID: 33217525
- Ye Tao, .et al. , Chemosphere, 2020, Mar;242:124959 PMID: 31669990
- Ming Sun, .et al. , J Agric Food Chem, 2018, Nov 21;66(46):12376-12384 PMID: 30392375
- Xueyan Wu, .et al. , Food Chem Toxicol, 2017, Aug;106(Pt A):273-282 PMID: 28579546
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Carbonic anhydrase inhibitor
Benzenesulfonamide ia an inhibitor of carbonic anhydrases. -
PDE3 inhibitor
Cilostamide is a selective inhibitor of phosphodiesterase (PDE)3A and PDE3B with IC50 values of 27 and 50 nM, respectively. -
ACE inhibitor
Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM. -
PDE-KRAS inhibitor
Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling. -
HMG-CoA reductase inhibitor
Atorvastatin is an HMG-CoA reductase inhibitor (IC50 = 154 nM) that is effective in treating hypercholesterolemia and certain dyslipidemias.- Huang Y, .et al. , Mol Med Rep, 2016, Feb;13(2):1888-94 PMID: 26707502

