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Results for "

Direct Inhibitors

" in MedChemExpress (MCE) Product Catalog:

125

Inhibitors & Agonists

4

Screening Libraries

2

Fluorescent Dye

3

Peptides

7

Inhibitory Antibodies

11

Natural
Products

13

Isotope-Labeled Compounds

1

Click Chemistry

Cat. No. Product Name Target Research Areas
  • HY-D0939
    Direct Blue 1

    Chicago Sky Blue 6B

    		 Amyloid-β Neurological Disease
    Direct Blue 1 (Chicago Sky Blue 6B) is a counterstain for background autofluorescence in immunofluorescence histochemistry. Direct Blue 1, structurally related to glutamate, is a potent and competitive VGLUT inhibitor without affecting plasma membrane transporters. Direct Blue 1 is the first small molecule PrP ligand capable of inhibiting Aβ binding.
  • HY-B0375A
    Argatroban monohydrate
    3 Publications Verification

    MD-805 monohydrate; MCI-9038 monohydrate; Argipidine monohydrate

    		 Thrombin Cardiovascular Disease Cancer
    Argatroban (monohydrate) (MD-805 (monohydrate)) is a direct, selective thrombin inhibitor.
  • HY-10515
    BX-320

    		PDK-1 Cancer
    BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect.
  • HY-B0375
    Argatroban

    MD-805; MCI-9038; Argipidine

    		 Thrombin Cardiovascular Disease
    Argatroban (MD-805) is a direct, selective thrombin inhibitor.
  • HY-19628A
    OD36 hydrochloride

    		RIP kinase TGF-β Receptor Inflammation/Immunology
    OD36hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with KDs of 37 nM.
  • HY-19628
    OD36

    		RIP kinase TGF-β Receptor Inflammation/Immunology
    OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM.
  • HY-17378
    Dabigatran (ethyl ester)
    1 Publications Verification

    		 Thrombin Cardiovascular Disease
    Dabigatran ethyl ester is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity.
  • HY-146048
    Antitumor agent-57

    		Apoptosis Reactive Oxygen Species Cancer
    Antitumor agent-57 (Compound 3o) is an NQO1-directed antitumor agent. Antitumor agent-57 inhibits tumor cell growth, triggers ROS generation and induces cell apoptosis.
  • HY-12176AS
    Aliskiren-d6 hydrochloride

    CGP 60536-d6 Hydrochloride; CGP60536Bd6 Hydrochloride; SPP 100d6(Hydrochloride)

    		 Isotope-Labeled Compounds Renin Cardiovascular Disease Cancer
    Aliskiren-d6 (hydrochloride) is is deuterium labeled Aliskiren, which is a direct renin inhibitor.
  • HY-124859
    CeMMEC2

    		Epigenetic Reader Domain Cancer
    CeMMEC2 is a novel direct BRD4 inhibitor with an IC50 of 0.9 μM.
  • HY-141487
    CLP-3094
    1 Publications Verification

    		 Androgen Receptor Metabolic Disease Inflammation/Immunology
    CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
  • HY-103643
    Fumagillol

    (-)-Fumagillol

    		 Bacterial Infection
    Fumagillol is a direct precursor of fumagillin. Fumagillin, as an antimicrobial agent, is a potent and selective inhibitor of angiogenesis.
  • HY-D1270
    Direct Violet 1

    		SARS-CoV Infection
    Direct Violet 1, an azo dye, is a textile dye. Direct Violet 1 is also the protein-protein interaction (PPI) between the SARS-CoV-2 spike protein and ACE2 inhibitor with IC50s of 1.47-2.63 μM.
  • HY-B0375S
    Argatroban-d3

    		Isotope-Labeled Compounds Thrombin Cardiovascular Disease
    Argatroban-d3 is the deuterium labeled Argatroban. Argatroban (MD-805) is a direct, selective thrombin inhibitor.
  • HY-114511
    BMS-593214

    		Others Cardiovascular Disease
    BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT).
  • HY-P99843
    Datopotamab

    		ADC Antibody Cancer
    Datopotamab (CDP7657) is an antibody targeting to TROP2. Datopotamab can be used to synthesize Datopotamab deruxtecan (HY-141598), TROP2-directed antibody-drug conjugate (ADC). Datopotamab deruxtecan consists of DNA topoisomerase I inhibitor Deruxtecan (HY-13631E) and Datopotamab.
  • HY-10163AS
    Dabigatran-d4 hydrochloride

    BIBR-953-d4 hydrochloride

    		 Thrombin Cardiovascular Disease
    Dabigatran-d4 (hydrochloride) is deuterium labeled Dabigatran, which is a reversible and selective, direct thrombin inhibitor (DTI) with a Ki value of 4.5 nM.
  • HY-P1929
    Bivalirudin
    5+ Cited Publications

    		 Thrombin Cardiovascular Disease
    Bivalirudin, a peptide anticoagulant, is a direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.
  • HY-10217
    Thrombin Inhibitor 2

    		Thrombin Cardiovascular Disease
    Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2. Thrombin Inhibitor 2 has antithrombotic activity.
  • HY-103334
    MAFP

    Methyl Arachidonyl Fluorophosphonate

    		 Phospholipase Metabolic Disease Neurological Disease Cardiovascular Disease
    MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.
  • HY-U00422
    K-756

    		PARP Cancer
    K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively.
  • HY-128661
    IDH1 Inhibitor 2

    		Isocitrate Dehydrogenase (IDH) Metabolic Disease
    IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.
  • HY-12369
    GGTI-2133

    		ROS Kinase Inflammation/Immunology
    GGTI-2133 is a direct and selective inhibitor of geran ylgeranyltransferase (GGTase). GGTI-2133 has the potential for eosinophilic airway inflammation such as asthma research.
  • HY-10273
    Atecegatran metoxil

    AZD0837; Atecegatran fexenetil

    		 Thrombin Cardiovascular Disease
    Atecegatran metoxil is a oral anticoagulant, which inhibits thrombin factor II and is used in thromboembolic disorders. In vivo, Atecegatran metoxil is converted to AR-H067637, a selective and reversible direct thrombin inhibitor.
  • HY-12177S
    Aliskiren-d6 hemifumarate

    CGP 60536 d6 (hemifumarate); CGP60536B d6 (hemifumarate); SPP 100 d6 (hemifumarate)

    		 Renin Autophagy Cancer Cardiovascular Disease
    Aliskiren-d6 (hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM[1][2].
  • HY-153493A
    PF-04523655 sodium

    		Small Interfering RNA (siRNA) Metabolic Disease
    PF-04523655 sodium is a siRNA directed against RTP801 gene. RTP801 sodium is an inhibitor of the mammalian target of rampamycin complex 1 (mTORC1) and downstream transcription factor HIF-1.
  • HY-139032
    CM121

    		Aldehyde Dehydrogenase (ALDH) Others
    CM121 is an active site-directed reversible ALDH1A2 inhibitor (IC50=0.54 μM；Kd=1.1 μM) with a variety of hydrophobic interactions.
  • HY-109855
    CP-67015

    		Topoisomerase Antibiotic Bacterial Infection
    CP-67015, a quinolone antibiotic, is a potent topoisomerase II inhibitor. CP-67015 is a positive direct-acting mutagen in mammalian cells with both gene and chromosomal level effects.
  • HY-10274
    Dabigatran etexilate
    3 Publications Verification

    BIBR 1048

    		 Thrombin Cardiovascular Disease
    Dabigatran etexilate (BIBR 1048) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
  • HY-153493
    PF-04523655

    		Small Interfering RNA (siRNA) Metabolic Disease
    PF-04523655 is a siRNA directed against RTP801 gene. RTP801 is an inhibitor of the mammalian target of rampamycin complex 1 (mTORC1) and downstream transcription factor HIF-1.
  • HY-10274A
    Dabigatran etexilate mesylate
    3 Publications Verification

    BIBR 1048MS; Dabigatran etexilate methanesulfonate

    		 Thrombin Cardiovascular Disease
    Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
  • HY-102076
    0990CL

    		Others Others
    0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP.
  • HY-125989
    2-Methylthio-AMP
    1 Publications Verification

    2-MeSAMP; 2-Methylthioadenosine 5′-monophosphate; 2-Methylthioadenosine 5′-phosphate

    		 P2Y Receptor Cardiovascular Disease
    2-Methylthio-AMP (2-MeSAMP) is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP is an inhibitor of ADP-dependent platelet aggregation.
  • HY-50903
    Rivaroxaban
    10+ Cited Publications

    BAY 59-7939

    		 Factor Xa Cardiovascular Disease Cancer
    Rivaroxaban (BAY 59-7939) is a highly potent, selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
  • HY-10163
    Dabigatran
    4 Publications Verification

    BIBR 953; BIBR 953ZW

    		 Thrombin Cardiovascular Disease
    Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
  • HY-112373
    Aurora kinase inhibitor-3

    		Aurora Kinase Others
    Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket.
  • HY-126302
    DMT1 blocker 2

    		Others Metabolic Disease
    DMT1 blocker 2 is a direct inhibitor of divalent metal transporter 1 (DMT1), with an IC50 of 0.83 μM. DMT1 blocker 2 can block iron uptake by enterocytes in vivo.
  • HY-122482
    β-Rubromycin

    		HIV Reverse Transcriptase Antibiotic Inflammation/Immunology
    β-Rubromycin is a potent and selective inhibitor of human immunodeficiency virus-1 (HIV-1) RNA-directed DNA polymeras (reverse transcriptase). β-Rubromycin is a class of quinone antibacterials.
  • HY-115062
    MJ33 lithium salt

    		Phospholipase Metabolic Disease
    MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
  • HY-76948
    5-R-Rivaroxaban

    		Factor Xa Cardiovascular Disease
    5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
  • HY-125989B
    2-Methylthio-AMP diTEA

    2-MeSAMP diTEA; 2-Methylthioadenosine 5′-monophosphate diTEA; 2-Methylthioadenosine 5′-phosphate diTEA

    		 P2Y Receptor Cardiovascular Disease
    2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation.
  • HY-103666
    CY-09
    Maximum Cited Publications
    27 Publications Verification

    		 NOD-like Receptor (NLR) Inflammation/Immunology
    CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation.
  • HY-150691
    SARS 3CLpro-IN-1

    		SARS-CoV Cancer
    SARS 3CLpro-IN-1 (Compound 3b) is a SARS 3CL protease inhibitor with an IC50 value of 95 μM, as a specific stereo isomer of the octahydroisochromene scaffold, directs the P1 site imidazole.
  • HY-W025062
    Diethyl pyridine-2,4-dicarboxylate

    		Others Others
    Diethyl pyridine-2,4-dicarb is a potent prolyl 4-hydroxylase-directed proinhibitor. Diethyl pyridine-2,4-dicarb inhibits prolyl hydroxylation and procollagen processing in chick-embryo calvaria.
  • HY-50903S
    Rivaroxaban-d4
    1 Publications Verification

    BAY 59-7939-d4

    		 Factor Xa Cardiovascular Disease
    Rivaroxaban-d4 is a deuterium labeled Rivaroxaban. Rivaroxaban is a highly potent，selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM)[1][2].
  • HY-139031
    ALDH1A2-IN-1

    		Aldehyde Dehydrogenase (ALDH) Endocrinology
    ALDH1A2-IN-1 is an active site-directed reversible ALDH1A2 inhibitor (IC50=0.91 μM; Kd=0.26 μM) with several hydrophobic interactions.
  • HY-127105A
    Iptacopan hydrochloride
    3 Publications Verification

    LNP023 hydrochloride

    		 Complement System Metabolic Disease Inflammation/Immunology
    LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM.
  • HY-151931
    JA-ACC

    Jasmonyl-ACC

    		 Others Metabolic Disease
    JA-ACC (Jasmonyl-ACC) is a derivative of 1-aminocyclopropane-1-carboxylic acid (ACC). ACC is the direct precursor of the plant hormone ethylene. JA-ACC inhibits root growth in Arabidopsis and the inhibition is independent of jasmonic acid (JA) signaling.
  • HY-156395
    MN551

    		Others Cancer
    MN551 is a potent inhibitor of cysteine-directed electrophilic covalent that plays important roles in the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation.
  • HY-B1099
    Hycanthone
    2 Publications Verification

    		 DNA/RNA Synthesis Topoisomerase Parasite Infection
    Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
  • HY-10163S
    Dabigatran-d4

    BIBR 953-d4; BIBR 953ZW-d4

    		 Isotope-Labeled Compounds Thrombin Cardiovascular Disease
    Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
  • HY-102084
    LMT-28
    5+ Cited Publications

    		 Interleukin Related Inflammation/Immunology
    LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130.
  • HY-11005
    BX-912
    4 Publications Verification

    		 PDK-1 Apoptosis Cancer
    BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
  • HY-10163S1
    Dabigatran-d3

    BIBR 953-d3; BIBR 953ZW-d3

    		 Thrombin Cardiovascular Disease
    Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
  • HY-15724A
    Vercirnon sodium
    1 Publications Verification

    GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium

    		 CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-15724
    Vercirnon
    1 Publications Verification

    GSK-1605786; CCX282-B; Traficet-EN

    		 CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-18660
    Ciraparantag

    PER977

    		 Others Cardiovascular Disease
    Ciraparantag is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban.
  • HY-P99886
    Pexelizumab

    h5G1. 1-SC

    		 Complement System Apoptosis Neurological Disease Cardiovascular Disease
    Pexelizumab (h5G1. 1-SC) is a humanized scFv monoclonal antibody directed against the C5 complement component. Pexelizumab inhibits apoptosis and leukocyte infiltration. Pexelizumab can be used for the research of cerebral IR injury and myocardial infarction.
  • HY-119711
    NNGH

    		MMP Cancer
    NNGH is a stromelysin-1 (MMP-3) inhibitor. MMP-3 is both a direct transcriptional target and a necessary contributor of the Wnt/β-catenin signaling pathway. Matrix metalloproteinases (MMPs) play a well-defined role in later stages of tumor progression.
  • HY-N8188
    Dehydrojuncusol

    		HCV HCV Protease Infection
    Dehydrojuncusol, a potent HCV inhibitor, targets HCV NS5A and is able to inhibit RNA replication of replicons harboring resistance mutations to anti-NS5A direct-acting antivirals. Dehydrojuncusol significantly inhibits HCV infection when added after virus inoculation of HCV genotype 2a (EC50=1.35 µM).
  • HY-19826
    Isofistularin-3

    		DNA Methyltransferase ADC Cytotoxin Autophagy Apoptosis Cancer
    Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
  • HY-103180
    2'-MeCCPA

    		Adenosine Receptor Neurological Disease
    2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs).
  • HY-110019
    Indatraline hydrochloride

    Lu 19-005

    		 Serotonin Transporter Dopamine Transporter Neurological Disease
    Indatraline hydrochloride (Lu 19-005) is a non-selective monoamine transporter inhibitor that blocks the reuptake of neurotransmitters (dopamine, serotonin, and norepinephrine). Indatraline hydrochloride can be used for the research of antidepressive. Indatraline hydrochloride induces autophagy while simultaneously inhibiting cell proliferation. Indatraline hydrochloride may also serve to direct the development of new agents for autophagy-related diseases such as atherosclerosis or restenosis.
  • HY-10163S2
    Dabigatran-13C6

    BIBR 953-13C6; BIBR 953ZW-13C6

    		 Thrombin
    Dabigatran- 13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
  • HY-129944
    MJ33-OH

    		Phospholipase Inflammation/Immunology
    MJ33-OH is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
  • HY-129944A
    MJ33-OH lithium

    		Phospholipase Inflammation/Immunology
    MJ33-OH lithium is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
  • HY-18637
    LDN-57444
    10+ Cited Publications

    		 Deubiquitinase Apoptosis Neurological Disease
    LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
  • HY-P10108
    Hexokinase II VDAC binding domain peptide

    Hxk2VBD peptide

    		 Hexokinase Neurological Disease
    Hexokinase II VDAC binding domain peptide (Hxk2VBD peptide) is a cell-permeable hexokinase II VDAC binding domain. Hexokinase II VDAC binding domain peptide inhibits mitochondrial localization of hexokinase 2 (HXK2). Hexokinase II VDAC binding domain peptide inhibits neurotrophic factor-directed axon outgrowth.
  • HY-10163S3
    Dabigatran-13C,d3

    BIBR 953-13C,d3; BIBR 953ZW-13C,d3

    		 Isotope-Labeled Compounds Thrombin Cardiovascular Disease
    Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
  • HY-P99205
    Glembatumumab

    		ADC Antibody Cancer
    Glembatumumab is a fully human IgG2 monoclonal antibody directed against the extracellular structural domain of GPNMB expressed in human breast cancer and melanoma. Glembatumumab can be coupled to the microtubule inhibitor monomethyl auristatin E to form glembatumumab vedotin. Glembatumumab vedotin is an antibody-agent coupling (ADC) with antitumor activity.
  • HY-106228
    HLF1-11

    		Fungal Bacterial Glutathione Peroxidase Infection
    HLF1-11, a human lactoferrin-derived peptide, is a broad spectrum antimicrobial agent. HLF1-11 inhibits human MPO activity. HLF1-11 also directs GM-CSF-driven monocyte differentiation toward macrophages, and enhances immune responses.
  • HY-N7119
    Cimicifugoside

    		Others Inflammation/Immunology
    Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity. Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function.
  • HY-B0252
    Hydrochlorothiazide
    1 Publications Verification

    HCTZ

    		 TGF-beta/Smad Potassium Channel Metabolic Disease Cardiovascular Disease Cancer
    Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
  • HY-W058849
    MT 63-78

    		AMPK mTOR Apoptosis Cancer
    MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.
  • HY-117290
    BMS-962212

    		Factor Xa Cardiovascular Disease
    BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity.
  • HY-151111
    SPH3127

    		Renin Cardiovascular Disease
    SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research.
  • HY-143499
    hMAO-B-IN-3

    		Monoamine Oxidase Neurological Disease
    hMAO-B-IN-3 (Compound 15) is a potent inhibitor of hMAO-B with an IC50 of 47.4 nM. hMAO-B-IN-3 is playing favourable agent-like properties and a broad safety window. hMAO-B-IN-3 is thus a suitable candidate for lead optimization and the development of multitarget-directed ligands.
  • HY-115673
    LAS17
    1 Publications Verification

    		 Gutathione S-transferase Cancer
    LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione?S-Transferase Pi (GSTP1) . LAS17 inhibits GSTP1 activity with an IC50 of 0.5 μM. LAS17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-138280
    DTHIB
    1 Publications Verification

    		 HSP Cancer
    DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research.
  • HY-100923
    H-9 Dihydrochloride

    		PKA 5-HT Receptor EGFR Neurological Disease
    H-9 Dihydrochloride is a PKA (protein kinase) inhibitor. H-9 Dihydrochloride (10 μM) significantly reduces the excitatory response to 5-HT. H-9 Dihydrochloride also has a direct effect on pharyngeal activity. H-9 Dihydrochloride inhibits signal-transduction and cell growth in EGF (epidermal growth factor)-dependent epithelial cell lines.
  • HY-155557
    Anti-inflammatory agent 45

    		Apoptosis Cancer
    Anti-inflammatory agent 45 (compound 2v) is an anticancer agent with direct inhibitory effects on the growth of different blood cancers including leukemia, lymphoma and myeloma cell lines. Anti-inflammatory agent 45 induces apoptosis and inhibits NO production in HL60 leukemia cells (IC50=14.7 μM).
  • HY-N3931
    Gardneramine

    		Others Cardiovascular Disease
    Gardneramine is an orally active alkaloid that acts like papaverine. Gardneramine has peripheral vascular diastolic effect, direct inhibition on myocardium and central inhibition. Gardneramine showed antihypertensive, vasodilatation and atrial inhibition effects in rabbit, dog and guinea pig models, respectively. Gardneramine also inhibits the movement of smooth muscle organs such as the stomach and intestines.
  • HY-B0557
    Bisacodyl

    		Dopamine Transporter Opioid Receptor Metabolic Disease Cancer
    Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.
  • HY-149368
    SARS-CoV-2-IN-51

    		SARS-CoV Infection
    SARS-CoV-2-IN-51 (S-10) is a potent lead compound of Omicron fusion inhibitor. SARS-CoV-2-IN-51 inhibits Omicron and other variants with EC50s of 0.82-5.45 μM. SARS-CoV-2-IN-51 inhibits SARS-CoV-2 virus entry, by the direct interaction with S in the prefusion state.
  • HY-13295
    Vinpocetine
    5+ Cited Publications

    Ethyl apovincaminate

    		 Sodium Channel IKK Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease Cardiovascular Disease Cancer
    Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na + channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
  • HY-19840
    Voxilaprevir

    GS-9857

    		 HCV Protease Infection
    Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity. Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively. Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research.
  • HY-101499A
    GKT136901 hydrochloride

    		NADPH Oxidase Metabolic Disease Neurological Disease
    GKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 hydrochloride is also a selective and direct scavenger of peroxynitrite. GKT136901 hydrochloride can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 hydrochloride also has anti-inflammatory activity.
  • HY-122080
    Memoquin

    		Cholinesterase (ChE) Beta-secretase Amyloid-β Neurological Disease
    Memoquin is an anti-amyloid and anti-oxidant multi-target-directed ligand. Memoquin is an orally active inhibitor of BACE-1 and AChE with IC50 values of 108 and 1.55 nM, respectively. Memoquin is a cognitive enhancer that prevents the Aβ-induced neurotoxicity mediated by oxidative stress. Memoquin can be used for the research of Alzheimer’s disease (AD).
  • HY-127105
    Iptacopan
    3 Publications Verification

    LNP023

    		 Complement System Metabolic Disease Inflammation/Immunology
    Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G).
  • HY-101499
    GKT136901

    		NADPH Oxidase Metabolic Disease Inflammation/Immunology Neurological Disease
    GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 is also a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.
  • HY-W412264
    Pim-1/2 kinase inhibitor 1

    		Pim Cancer
    Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27 Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer.
  • HY-N0292
    Oleuropein
    1 Publications Verification

    		 Cytochrome P450 PPAR Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.
  • HY-10264B
    Edoxaban tosylate monohydrate
    4 Publications Verification

    DU-176b monohydrate

    		 Factor Xa Thrombin Cardiovascular Disease Cancer
    Edoxaban (DU-176b) monohydrate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Kis of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban monohydrate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban monohydrate can be used for preventing thromboembolic disease research.
  • HY-10264C
    Edoxaban hydrochloride

    DU-176 hydrochloride

    		 Factor Xa Thrombin Cardiovascular Disease
    Edoxaban (DU-176b) hydrochloride is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban hydrochloride exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban hydrochloride can be used for preventing thromboembolic disease research.
  • HY-116785
    BRD32048

    		DNA/RNA Synthesis Cancer
    BRD32048 is a direct binder of ETV1 with a KD of 17.1 μM. BRD32048 modulates both ETV1-mediated transcriptional activity and invasion of ETV1-driven cancer cells. BRD32048 inhibits ETV1 acetylation and promotes its degradation. BRD32048 acts as a top candidate ETV1 perturbagen.
  • HY-10264
    Edoxaban
    4 Publications Verification

    DU-176

    		 Factor Xa Thrombin Cardiovascular Disease Cancer
    Edoxaban (DU-176b) is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban can be used in preventing thromboembolic disease research.
  • HY-B0252S
    Hydrochlorothiazid-d2

    HCTZ-d2

    		 TGF-beta/Smad Potassium Channel Metabolic Disease Cardiovascular Disease
    Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
  • HY-125927
    8-Aminoadenosine

    8-NH2-Ado

    		 DNA/RNA Synthesis Akt mTOR Autophagy Apoptosis Cancer
    8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity.
  • HY-129056
    Melagatran

    		Thrombin Cardiovascular Disease
    Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion.
  • HY-10264A
    Edoxaban tosylate
    4 Publications Verification

    DU-176b

    		 Factor Xa Thrombin Cardiovascular Disease Cancer
    Edoxaban (DU-176b) tosylate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Kis of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban tosylate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban tosylate can be used for preventing thromboembolic disease research.
  • HY-107845
    SCR7 pyrazine
    5+ Cited Publications

    		 CRISPR/Cas9 DNA/RNA Synthesis Apoptosis Cancer
    SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity.
  • HY-N10177
    Peniterphenyl A

    		HSV Infection
    Peniterphenyl A is a natural product obtained from a deep-sea-derived Penicillium sp. Peniterphenyl A inhibits HSV-1/2 virus entry into cells and may block HSV-1/2 infection through direct interaction with virus envelope glycoprotein D to interfere with virus adsorption and membrane fusion. Peniterphenyl A is a promising lead compound against HSV-1/2.
  • HY-13295S
    Vinpocetine-d5

    		Sodium Channel IKK Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease Cardiovascular Disease Cancer
    Vinpocetine-d5 is the deuterium labeled Vinpocetine. Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders[1][2][3].
  • HY-B0252S2
    Hydrochlorothiazide-13C6

    HCTZ-13C6

    		 TGF-beta/Smad Potassium Channel
    Hydrochlorothiazide- 13C6 is the 13C labeled Hydrochlorothiazide[1]. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[2][3][4].
  • HY-100900
    ML364
    10+ Cited Publications

    		 Deubiquitinase Cancer
    ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP.
  • HY-B0252S1
    Hydrochlorothiazid-13C,d2

    HCTZ-13C,d2

    		 Isotope-Labeled Compounds TGF-beta/Smad Potassium Channel Metabolic Disease Cardiovascular Disease
    Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
  • HY-123349
    5α-Hydroxy-6-keto cholesterol

    		Drug Metabolite Cardiovascular Disease
    5α-Hydroxy-6-keto cholesterol is major metabolite of β-epoxide (5α,6β-epoxycholesterol) during direct exposure of intact cultured human bronchial epithelial cells (16-HBE) to ozone. 5α-Hydroxy-6-keto cholesterol inhibits cholesterol synthesis with an IC50 of 350 nM.
  • HY-125604
    WCK-4234

    		Bacterial Infection
    WCK-4234 is a potent β-lactamase inhibitor. WCK-4234 inhibits class A, C, and D β-lactamases activity. WCK-4234 lacks direct antibacterial activity. WCK-4234 potentiates imipenem and meropenem against Enterobacteriaceae with OXA-48/OXA-181 or KPC enzymes, or with combinations of impermeability and AmpC or ESBL activity. WCK-4234 distinctively overcomes resistance mediated by OXA-type carbapenemases.
  • HY-145827
    KIF18A-IN-4

    		Microtubule/Tubulin Cancer
    KIF18A-IN-4 is a moderately potent ATP and microtubule (MT) noncompetitive KIF18A inhibitor (IC50=6.16 μM). KIF18A-IN-4 has selectivity against a large panel of mitotic kinesins and kinases, and does not show any direct effects on tubulin assembly. KIF18A-IN-4 exhibits anti-tumor activity.
  • HY-124364
    RO6889678

    		HBV Cytochrome P450 Infection Metabolic Disease
    RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes. RO6889678 is metabolized by a combination of CYP3A4-mediated oxidation and UDP-glucuronosyltransferase UGT1A3- and UGT1A1-mediated direct glucuronidation.
  • HY-18649
    Galidesivir hydrochloride
    5+ Cited Publications

    BCX4430 hydrochloride; Immucillin-A hydrochloride

    		 DNA/RNA Synthesis SARS-CoV Filovirus Infection
    Galidesivir (BCX4430) hydrochloride, an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir hydrochloride is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir hydrochloride inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.
  • HY-19357
    E3330
    2 Publications Verification

    APX-3330

    		 DNA/RNA Synthesis NF-κB AP-1 HIF/HIF Prolyl-Hydroxylase VEGFR Reactive Oxygen Species Cancer Neurological Disease Cardiovascular Disease
    E3330 (APX-3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. E3330 is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. E3330 shows anticancer activities.
  • HY-125028
    Hck-IN-1

    		Src HIV Infection
    Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity.
  • HY-18649A
    Galidesivir
    5+ Cited Publications

    BCX4430; Immucillin-A

    		 DNA/RNA Synthesis SARS-CoV Filovirus Infection
    Galidesivir (BCX4430), an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.
  • HY-123823
    Nitroaspirin

    NCX 4016

    		 COX Apoptosis Cancer
    Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.
  • HY-18980
    Rottlerin
    4 Publications Verification

    Mallotoxin; NSC 56346; NSC 94525

    		 PKC Autophagy Apoptosis HIV RABV Infection Cancer
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.
  • HY-100034
    NSC 663284
    3 Publications Verification

    DA-3003-1

    		 Phosphatase Histone Methyltransferase Cancer
    NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM).
  • HY-12742
    SCR7

    		DNA/RNA Synthesis CRISPR/Cas9 Apoptosis Cancer
    SCR7 is an unstable form that can be autocyclized into a stable form SCR7 pyrazine. SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity.
  • HY-124295
    MPT0E028

    		HDAC Akt Apoptosis Cancer
    MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity.
  • HY-N1942
    5-O-Demethylnobiletin
    1 Publications Verification

    5-Demethylnobiletin

    		 Lipoxygenase Leukotriene Receptor Inflammation/Immunology Neurological Disease Cancer
    5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
  • HY-P9976
    Isatuximab
    1 Publications Verification

    		 Apoptosis Cancer
    Isatuximab is a monoclonal antibody targeting the transmembrane receptor and ectoenzyme CD38, a protein highly expressed on hematological malignant cells, including those in multiple myeloma (MM). Isatuximab has antitumor activity via multiple biological mechanisms, including antibody-dependent cellular-mediated cytotoxicity, complement-dependent cytotoxicity, antibody-dependent cellular phagocytosis, and direct induction of apoptosis without crosslinking. Isatuximab also directly inhibits CD38 ectoenzyme activity, which is implicated in many cellular functions.
  • HY-145931
    CC214-2

    		mTOR Autophagy Cancer
    CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo.
  • HY-117693
    Mirin

    		ATM/ATR Cancer
    Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells.
  • HY-P99361
    Enavatuzumab

    PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)

    		 TNF Receptor Cancer
    Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
  • HY-N5072
    Desmethylglycitein

    4',6,7-Trihydroxyisoflavone

    		 CDK PI3K PKC Cancer
    Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.