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O-GlcNAcase inhibitor
Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37,000-fold selectivity over human lysosomal-hexosaminidase.- Aaron K Olson, .et al. , BMC Mol Cell Biol, 2025, Jun 10;26(1):19 PMID: 40495125
- Kefan Wu, .et al. , Biomedicines, 2023, Apr 24;11(5):1259 PMID: 37238930
- Wei Zhong Zhu, .et al. , PLoS One, 2022, Oct 26;17(10):e0276285 PMID: 36288343
- Zhu WZ, .et al. , J Am Heart Assoc, 2019, Jun 4;8(11):e011260 PMID: 31131693
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3CLpro inhibitor
GC376 is a 3CLpro inhibitor (3C-like protease inhibitor).- Ai-Ai Chou, .et al. , Vet Q, 2024, Dec;44(1):1-13 PMID: 38712855
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MyD88 dimerization Inhibitor
ST 2825 is a MyD88 pharmacologic inhibitor.- Bernard Kan, .et al. , Nat Commun, 2018, 9: 4822 PMID: 30446641
- Shira Dishon, .et al. , Sci Rep, 2018, 8: 9476 PMID: 29930295
- Treprostinil is a stable analog of prostacyclin that is used clinically for the treatment of PPH.
- Bhat L, .et al. , Eur J Pharmacol, 2018, May 15;827:159-166 PMID: 29453947
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SE inhibitor
NB-598 is a potent competitive inhibitor of squalene epoxidase (SE). NB-598 suppresses triglyceride biosynthesis through the farnesol pathway.- Gia-Buu Tran, .et al. , Cancer Res, 2023, Apr 14;CAN-22-3450 PMID: 37057874
- Weber RA, .et al. , Mol Cell, 2020, Feb 6;77(3):645-655 PMID: 31983508
- Garcia-Bermudez J, .et al. , Nature, 2019, Feb 13 PMID: 30760928
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TPA/PMA inhibitor
Cyclosporin H is a TPA/PMA inhibitor and a selective inhibitor of formyl peptide receptors (Ki = 0.1 uM).- Jean-Philippe Auger, .et al. , Nature, 2024, May;629(8010):184-192 PMID: 38600378
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c-Fos inhibitor
T-5224 is a selective inhibitor of c-Fos/activator protein-1.- Mirei Fujita, .et al. , Biomolecules, 2026, 16(5), 755 PMID: 42194103
- Kamata Y, .et al. , J Dermatol Sci, 2018, Apr 23. pii: S0923-1811(18)30186-5 PMID: 29730173
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rRNA biogenesis inhibitor
Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis that is overexpressed in cancer cells; disruption of this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis may result in the inhibition of ribosome synthesis and tumor cell apoptosis.- Rocio Diaz Escarcega, .et al. , Cell Death Dis, 2026, Jun 18 PMID: 42310298
- Maria Sultan, .et al. , J Biomed Sci, 2025, Feb 5;32(1):15 PMID: 39905515
- Jing-Wei Liang, .et al. , Antioxidants (Basel), 2023, Dec 20;13(1):11 PMID: 38275631
- Maria Razzaq, .et al. , Arch Pharm Res, 2023, Jul;46(7):598-615 PMID: 37563335
- Janne J. M. van Schie, .et al. , Nat Commun, 2020, 11: 4287 PMID: 32855419
- Yue Sheng, .et al. , Blood, 2020, Aug 21 PMID: 32822452
- Hald øH, .et al. , Oncogene, 2018, Dec 12 PMID: 30542116
- Louise E. Kerry, .et al. , PLoS Negl Trop Dis, 2017, Mar; 11(3): e0005432 PMID: 28263991
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micromolar inhibitor
Zanamivir is a neuraminidase inhibitor used in the treatment and prophylaxis of influenza caused by influenza A virus and influenza B virus.- Yuuki Kurebayashi, .et al. , PLoS One, 2016, 11(5): e0156400 PMID: 27232333
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O-GlcNAcase inhibitor
Streptozotocin (Streptozocin, Zanosar, STZ)is used in medical research to produce an animal model for Type 1 diabetes, which directly inhibist the O-GlcNAcase activity of the enzyme NCOAT in vitro.- Zhen Liang, .et al. , Nat Metab, 2023, Jan;5(1):29-40 PMID: 36624157
- Alemayehu Toma, .et al. , J Exp Pharmacol, 2022, 14: 309-316 PMID: 36317069
- Andressa Braga, .et al. , Braz J Pharm Sci, 2022, 58: e19674
- Yuanyuan Du, .et al. , Nat Med, 2022, Feb;28(2):272-282 PMID: 35115708
- Karemah A. Alatawi, .et al. , Saudi Journal of Biological Sciences, 2021, 25 June PMID: 34354403
- D.H. Mhya, .et al. , Asian J Exp Biol Sci, 2019, 12 (2): 164-172
- Stanley I. R. Okoduwa, .et al. , J Diabetol, 2017, 8(3): 74-85
- Stanley I. R. Okoduwa, .et al. , Medicines (Basel), 2017, Dec; 4(4): 73 PMID: 29019956
- Stanley I. R. Okoduwa, .et al. , PLoS One, 2017, 12(1): e0170971 PMID: 28129400
- Stanley I. R. Okoduwa, .et al. , World J Diabetes, 2016, Dec 15; 7(20): 605-614 PMID: 28031778
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Hyaluronan (HA) synthesis inhibitor
4-Methylumbelliferone is a selective inhibitor of Hyaluronan (HA) synthesis which is thought to function as an inhibitor via the depletion of UDP-glucuronic acid, the common substrate for HA synthesis. -
Hydrogen peroxide inhibitor
Acetanilide is used as an inhibitor in hydrogen peroxide and is used to stabilize cellulose ester varnishes. -
DprE1 inhibitor
BTZ043 (BTZ038, BTZ044) inhibits decaprenylphosphoryl-β-d-ribose 2?-epimerase, which is an enzyme which produces the cell wall of the pathogenic bacterium Mycobacterium tuberculosis. -
Monoamine reuptake inhibitor
Diclofensine (Ro 8-4650) acts as a triple monoamine reuptake inhibitor, primarily inhibiting the reuptake of dopamine and noradrenaline. -
dipeptidase inhibitor
Cilastatin is a dipeptidase inhibitor that specifically inhibits DPEP1 (dehydrodipeptidase I), a renal membrane-bound glycoprotein involved in the hydrolytic metabolism of penem and carbapenem ??-lactam antibiotics. -
HPPD inhibitor
Nitrisinone is a competitive inhibitor that reversibly inhibits 4-Hydroxyphenylpyruvate oxidase (dioxygenase). -
triazole DAGL(α) inhibitor
DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100. -
enkephalin degrading enzymes inhibitor
Kelatorphan is a full inhibitor of enkephalin degrading enzymes. -
CDC7 kinase inhibitor
(R)-Simurosertib ((R)-TAK-931) is the (R)-enantiomer of Simurosertib, Simurosertib (TAK-931) is a selective cycle 7 (CDC7) kinase inhibitor, with an IC50<0.3 nM. -
SAMDC inhibitor
Sardomozide is an S-adenosylmethionine decarboxylase (SAMDC) inhibitor with an IC50 of 5 nM. -
polymerase inhibitor
ERDRP-0519 is an orally available inhibitor of polymerase that shows efficacy against a lethal morbillivirus infection in a large animal model. -
p18INK inhibitor
NSC23005 is a p18INK inhibitor. NSC23005 potently promotes hematopoietic stem cell (HSC) expansion (ED50 = 5.21 nM). -
inhibitor for GA perception
TSPC is an inhibitor for GA perception by in vitro and in planta evaluations. -
Eph family tyrosine kinase inhibitor
Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor. -
S-adenosylhomocysteine hydrolase inhibitor
3-Deazaadenosine (hydrochloride) is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 ?M; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity. -
inhibitor of glycogen synthase kinase 3
5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3). -
transcriptional inhibitor of G0/G1 switch 2
NS-3-008 hydrochloride is an orally active transcriptional inhibitor of G0/G1 switch 2 (G0s2) with an IC50 of 2.25 μM. NS-3-008 hydrochloride can be used for chronic kidney disease. -
Glycogen phosphorylase (GP) inhibitor
AVE5688 is an inhibitor of glycogen phosphorylase (GP), with IC50s of 430 nM and 915 nM and Kds of 170 nM and 530 nM for rabbit muscle glycogen phosphorylase (rmGPb and rmGPa, respectively); AVE5688 can be used for the research of type 2 diabetes. -
ECE inhibitor
(±)-WS75624B is an endothelin converting enzyme (ECE) inhibitor with an IC50 of 0.03 μg/mL. -
CNT2 Inhibitor
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2. -
squalene epoxidase inhibitor
FR194738 free base is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM. -
Neutrophil elastase inhibitor
Freselestat is a potent neutrophil elastase inhibitor. Freselestat reduces inflammatory mediators during simulated extracorporeal circulation. ONO-6818 significantly reduced interleukin 8 and C5b-9 production. ONO-6818 did not modulate changes of CD11b and L-selectin during recirculation. -
SCD1 inhibitor
stearoyl-CoA desaturase 1 (SCD1) inhibitor. Used to selectively eliminate undifferentiated human pluripotent stem cells (hPSCs) from culture; induces ER stress, attenuates protein synthesis and induces apoptosis in hPSCs. Prevents teratoma formation in immunocompromised mice. -
glycolate oxidase inhibitor
Glycolic acid oxidase inhibitor 1 is a glycolate oxidase inhibitor, extracted from patent EP0021228A1, in Table IV. -
AKR1C3 inhibitor
AKR1C3-IN-1 is a potent, highly selective inhibitor of AKR1C3, with an IC50 of 13 nM.

