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Tyrosinase inhibitor
Aloin (Barbaloin) is a yellow crystalline substance obtained from aloe and is reported to be a potent inhibitors of tyrosinase. -
Tyrosinase inhibitor
Arbutin is a glycosylated hydroquinone used in traditional Chinese medicine (TCM). Arbutin inhibits melanin formation due to its tyrosinase inhibitory activity.
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HIV Protease inhibitor
Atazanavir is an antiretroviral drug of the protease inhibitor (PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). -
HIV Protease inhibitor
Atazanavir is an antiretroviral drug of the protease inhibitor (PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). -
Thrombin inhibitor
BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate. It has shown antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action and predictable pharmacodynamic response.
- Tanaka M, .et al. , J Pharmacol Sci, 2016, Jul;131(3):162-71 PMID: 27426918
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Thrombin inhibitor
BIBR-1048 (Dabigatran etexilate) is an anticoagulant from the class of the direct thrombin inhibitors. -
HCV NS5A inhibitor
BMS-790052 is an NS5A inhibitor under investigation for the treatment of hepatitis C virus (HCV) infection.- TS Wahyuni, .et al. , Southeast Asian J Trop Med public health, 2020, 51(1)
- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
- Sato K, .et al. , Hepatol Res, 2018, Feb;48(3):E347-E353 PMID: 28834004
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Proteasome inhibitor
Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome- Tomoyuki Abe, .et al. , Eur J Pharmacol, 2022, Nov 15;935:175321 PMID: 36228744
- Yoshitaka Sato, .et al. , Cell Commun Signal, 2022, Jun 21;20(1):95 PMID: 35729616
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Shin-Ichi Makino, .et al. , J Am Soc Nephrol, 2021, Mar;32(3):597-613 PMID: 33510039
- Yusuke Yamashita, .et al. , Int J Mol Sci, 2020, Sep; 21(17): 6314 PMID: 32878237
- Nandini Verma, .et al. , Sci Adv, 2020, 6 : eaba8968
- A Hayano, .et al. , Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Hiroshi Fukamachi, .et al. , J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Y Sato, .et al. , J Virol, 2019, Jan 30. pii: JVI.01707-18 PMID: 30700607
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Wenhan Deng, .et al. , Transl Oncol, 2018, Oct; 11(5): 1147-1154 PMID: 30055346
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Hokyung K. Chung, .et al. , Nat Chem Biol, 2015, Sep; 11(9): 713-720 PMID: 26214256
- S Raz, .et al. , Cell Death Dis., 2014, 5(2): e1067 PMID: 24556682
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HCV NS3/4A protease inhibitor
Danoprevir is a potent inhibitor of the HCV NS3/4A serine protease.- Mahim Khan, .et al. , BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Inês GARCEZ PALHA, .et al. , Biol Open, 2018, Nov 7 PMID: 30404898
- Hui Shen, .et al. , PLoS One., 2013, 8(12): e82299 PMID: 24358168
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Gamma secretase inhibitor
DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively.- Kubra Telli, .et al. , Turkish Journal of Biochemistry, 2023, February 6
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
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Proteasome Inhibitor
MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM. -
Proteasome Inhibitor
Ixazomib Citrate (MLN9708) Analogue is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.
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serine protease inhibitor
Nafamostat is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma. - Pimecrolimus is a natural ascomycin macrolactam that binds to macrophilin-12 (FKBP-12) and inhibits calcineurin as well as prolyl isomerase (rotamase).
- Doxycycline Hydrochloride is a synthetic tetracycline derivative with similar antimicrobial activity.
- Racecadotril is a potent enkephalinase inhibitor which exhibits selective antisecretory activity.
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HIV Protease inhibitor
Ritonavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease.Ritonavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. -
Gamma-secretase inhibitor
RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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Gamma-secretase inhibitor
Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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DDP-4 inhibitor
Sitagliptin phosphate is an anti-diabetic (antihyperglycemic) drug of the dipeptidyl peptidase-4 (DPP-4) class. Inhibition of the enzyme DPP-4 is thought to increase Glucagon-like peptide-1 (GLP-1) which inhibits glucagon release , stimulates the insulin release and lowers blood glucose. -
protein tyrosine phosphatases inhibitor
Sodium orthovanadate is the chemical compound Na3VO4. It is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue. -
HCV NS3-4A protease inhibitor
Telaprevir (VX-950) is known as protease inhibitors that inhibits the hepatitis C virus NS3.4A serine protease.- Mahim Khan, .et al. , BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Adita Ayu Permanasari, .et al. , BMC Complement Med Ther, 2021, Oct 12;21(1):260 PMID: 34641875
- Che C Colpitts, .et al. , eLife, 2020, 9: e52237 PMID: 32539931
- TS Wahyuni, .et al. , Southeast Asian J Trop Med public health, 2020, 51(1)
- Stefan Bittmann, .et al. , J Regen Biol Med, 2020, 2(2):1-3
- Wahyuni TS, .et al. , J Basic Clin Physiol Pharmacol, 2019, Dec 14 PMID: 31837259
- Jacobs CL, .et al. , Nat Methods, 2018, Jul;15(7):523-526 PMID: 29967496
- Apriyanto DR, .et al. , Jpn J Infect Dis, 2016, May 20;69(3):213-20 PMID: 26255732
- Mizuki Yamamoto, .et al. , Antimicrob Agents Chemother, 2016, Nov; 60(11): 6532-6539 PMID: 27550352
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HCV Protease inhibitor
VX-222 is a small molecule non-nucleoside inhibitor of HCV NS5B polymerase that is being investigated for the treatment of hepatitis C virus infection.- Wataru Ito, .et al. , Antivir Chem Chemother, 2015, Dec; 24(5-6): 148-154 PMID: 27503576
- Hui Shen, .et al. , PLoS One., 2013, 8(12): e82299 PMID: 24358168
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Caspase-1/4 inhibitor
VX-765 is a novel Caspase-1 inhibitor,which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18.- Joseph Flores, .et al. , Cell Death Dis, 2022, Oct 11;13(10):864 PMID: 36220815
- Arjun Thapa, .et al. , Leukemia, 2021, 23 February
- Prenitha Mercy Ignatius Arokia Doss, .et al. , Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. , Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. , Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. , Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. , J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. , Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054
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Proteasome inhibitor
MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM).- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Vo Thi Anh Nguyet, .et al. , Biochim Biophys Acta Gen Subj, 2022, Sep 6;1866(12):130241 PMID: 36075516
- Jalila Chagraoui, .et al. , Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Eunsu Yoo, .et al. , BMC Cancer, 2020, Sep 14;20(1):881 PMID: 32928152
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Chi-Hung R Or, .et al. , Int J Mol Sci, 2020, Mar 5;21(5):1773 PMID: 32150830
- Ghosh S, .et al. , Biochemistry, 2020, Feb 18;59(6):780-789 PMID: 31977203
- Kondo H, .et al. , J Biol Chem, 2020, Feb 7;295(6):1658-1672 PMID: 31915251
- Ohigashi I, .et al. , Cell Rep, 2019, Nov 26;29(9):2901-2916 PMID: 31775054
- Paudel DB, .et al. , Virology, 2018, Nov;524:127-139 PMID: 30195250
- Ohkusu-Tsukada K, .et al. , Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
- Chi-Hung R. Or, .et al. , Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
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Caspase activator
PAC-1 is an activator of procaspase-3 induces apoptosis in cancer cells with EC50 of 2.08 μM.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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DPP-4 Inhibitor
Saxagliptin (BMS-477118) is a new dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 50 nM.- OHE El-Shoubashy, .et al. , JPC, 2020, 33, 59-70
- Sato T, .et al. , Sci Rep, 2019, Dec 2;9(1):18094 PMID: 31792328
- Chintan N. Koyani, .et al. , Front Physiol, 2018, 9: 1622 PMID: 30487758
- Koyani CN, .et al. , Biochem Pharmacol, 2016, Dec 1;145:64-80 PMID: 28859968
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Proteasome inhibitor
CEP-18770 is a novel orally active proteasome inhibitor with a favorable tumor selectivity profile for the treatment of MM and other malignancies responsive to proteasome inhibition. -
γ-secretase inhibitor
YO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent.- Weijun Zhang, .et al. , Stem Cell Rev Rep, 2023, Jan 7 PMID: 36609902
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Gamma secretase inhibitor
LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.
- Haiwen Yu, .et al. , Immunol Invest, 2023, Feb;52(2):241-255 PMID: 36562737
- Wojciech J Szlachcic, .et al. , iScience, 2022, Jul 15;25(7) PMID: 35756892
- Zhang ZH, .et al. , APMIS, 2019, Jul 5 PMID: 31274210
- Bo Pang, .et al. , Biosci Rep, 2018, Dec 21; 38(6): BSR20181922 PMID: 30473538
- Shuo Li, .et al. , Int Immunopharmacol, 2018, Oct;63:129-136 PMID: 30086535
- Jiang BC, .et al. , Viral Immunol, 2017, Sep;30(7):522-532 PMID: 28410452
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HIV Entry Inhibitor
BMS-806, also known as BMS-378806 , is a type of medicine called an entry inhibitor. Entry inhibitors work by blocking HIV from entering human cells. BMS-378806 (BMS-806) is a small molecule that blocks the binding of host-cell CD4 with viral gp120 protein and therefore inhibits the first steps of HIV-1 infection. -
DPP-4 Inhibitor
Linagliptin is a DPP-4 inhibitor, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). -
NAE Inhibitor
NAE inhibitor MLN4924 binds to and inhibits NAE, which may result in the inhibition of tumor cell proliferation and survival.- Blue-leaf A. Cordes, .et al. , Cancers (Basel), 2023, Mar; 15(6): 1846 PMID: 36980731
- Min Dong, .et al. , J Immunother Cancer, 2022, Oct;10(10):e005270 PMID: 36198437
- Corentin Mallet, .et al. , J Virol, 2021, Dec 22;JVI0142721 PMID: 34936483
- Nobuyuki Shimizu, .et al. , Commun Biol, 2021, Nov 11;4(1):1277 PMID: 34764413
- Jalila Chagraoui, .et al. , Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Stephan Riesenberg, .et al. , Nat Commun, 2018, 9: 2164 PMID: 29867139
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Richard J. Kraus, .et al. , PLoS Pathog, 2017, Jun; 13(6): e1006404 PMID: 28617871
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Cathepsin K Inhibitor
Odanacatib is an inhibitor of cathepsin K,an enzyme involved in bone resorption. -
Proteasome inhibitor
PR-171 (Carfilzomib) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin.- Andrew Thorne, .et al. , PLoS One, 2023, Jun 8;18(6):e0286783 PMID: 37289679
- Mahmood Barani, .et al. , J Drug Deliv Sci Technol, 2023, 81: 104268
- Ori Kalid, .et al. , Chem Biol Drug Des, 2022, Mar 24 PMID: 35322538
- Abbas Rahdar, .et al. , Journal of Molecular Liquids, 2022, 346: 118271
- Sadegh Zarei, .et al. , J Appl Biotechnol Rep, 2019, June;6(2):45-49
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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HCV replication Inhibitor
Anguizole is a small molecule inhibits HCV replication and alters NS4B's subcellular distribution.- Choi M, .et al. , Virus Genes., 2013, Dec;47(3):395-407 PMID: 23868571
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HCV Protease Inhibitor
Boceprevir is a protease inhibitor used as a treatment for hepatitis C genotype 1.- Ueda Y, .et al. , Virus Res, 2017, May 2;235:37-48 PMID: 28322919
- Shirasaki T, .et al. , Hepatology., 2014, 60(5):1519-30 PMID: 24962339
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NS5A inhibitor
BMS-790052 is an NS5A inhibitor under investigation for the treatment of hepatitis C virus (HCV) infection.- Shirasaki T, .et al. , Hepatology., 2014, 60(5):1519-30 PMID: 24962339
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HIV Protease Inhibitor
Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. Saquinavir inhibits both HIV-1 and HIV-2 proteases.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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gamma-secretase modulator
E 2012 is γ-secretase inhibitor.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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NAE Inhibitor
NAE inhibitor MLN4924 binds to and inhibits NAE, which may result in the inhibition of tumor cell proliferation and survival. -
HIV-1 protease inhibitor
Nelfinavir is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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HCV Nucleotide Inhibitor
PSI-7977 is a phosphoramidate prodrug of PSI-7851, a nucleoside analog that, when phosphorylated, inhibits the RNA-dependent RNA polymerase of hepatitis C virus (EC50 = 92 nM).- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467