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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. -
Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
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- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Yodita Asfaha, .et al. , Eur J Med Chem, 2024, 263: 115907
- 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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Aminopeptidase inhibitor
CHR-2797 (Tosedostat) is a novel metalloenzyme inhibitor that exerts antiproliferative effects against a range of tumor cell lines in vitro and in vivo and shows selectivity. -
HCV NS3/4A protease inhibitor
Danoprevir is a potent inhibitor of the HCV NS3/4A serine protease.- Deqiang Kong, .et al. , Nat Commun, 2024, Jun 8;15(1):4894 PMID: 38849338
- Xinyi Wang, .et al. , Nat Chem Biol, 2023, Oct 23 PMID: 37872400
- 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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reversible Protease inhibitor
Ubenimex, also known as NK 421 and Bestatin, is a CD13 inhibitor. Ubenimex attenuates acquired sorafenib resistance in renal cell carcinoma by inhibiting Akt signaling in a lipophagy associated mechanism. Ubenimex synergistically enhances the effects of anticancer drugs in hepatocellular carcinoma. Ubenimex inhibits cell proliferation, migration and invasion by inhibiting the expression of APN and inducing autophagic cell death in prostate cancer cells. -
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).- Nathan Bulangalire, .et al. , Biochimie, 2024, Apr 16:S0300-9084(24)00079-8 PMID: 38636798
- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
- Carolina N Franco, .et al. , Sci Adv, 2023, Sep 8;9(36):eadi2232 PMID: 37682999
- 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.- Ki-Young Kim, .et al. , Pharmaceutics, 2024, Jan 13;16(1):106 PMID: 38258116
- 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). -
γ-secretase inhibitor
Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. -
γ-secretase inhibitor
PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM . -
NAE Inhibitor
NAE inhibitor MLN4924 binds to and inhibits NAE, which may result in the inhibition of tumor cell proliferation and survival.- Takumi Ito, .et al. , Research Square, 2023, 2023
- 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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NS3 protease inhibitor
Asunaprevir is an inhibitor of the viral enzyme serine protease NS3.- Mahim Khan, .et al. , BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
- Kato N, .et al. , Arch Virol, 2019, Dec 12 PMID: 31832864
- Fay EJ, .et al. , J Virol, 2018, Fay EJ PMID: 30282710
- Bennie Lemmens, .et al. , Mol Cell, 2018, Jul 5; 71(1): 117-128.e3 PMID: 30008317
- Ueda Y, .et al. , Virus Res, 2017, May 2;235:37-48 PMID: 28322919
- Furihata T, .et al. , Int J Antimicrob Agents, 2015, Oct;46(4):381-8 PMID: 26163159
- Tomomi Furihata, .et al. , Antimicrob Agents Chemother, 2014, 58(8): 4555-4564 PMID: 24867984
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Serine protease inhibitor
BCX 1470 is serine protease inhibitor. BCX 1470 blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro. -
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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Polymerase inhibitor
Balapiravir (R1626, RG1626) is the prodrug of a nucleoside analogue inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase (R1479, RG1479). -
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