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specific inhibition

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81

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3

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114672

    Phosphodiesterase (PDE) Cardiovascular Disease
    MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE .
    MBCQ
  • HY-137817

    DNA/RNA Synthesis Metabolic Disease
    BCH001, a quinoline derivative, is a specific PAPD5 inhibitor. BCH001 restores telomerase activity and telomere length in dyskeratosis congenita (DC) induced pluripotent stem cells. BCH001 shows no inhibition of poly(A)-specific ribonuclease (PARN) or several other canonical and non-canonical polynucleotide polymerases. BCH001 is used to regulate aging .
    BCH001
  • HY-P10146

    Caspase Cancer
    Ac-LETD-CHO is a caspases 8 inhibitor. Ac-LETD-CHO has specific inhibition to casp-8 with an IC50 value of 6.71 nM. Ac-LETD-CHO can be used for the research of anticancer .
    Ac-LETD-CHO
  • HY-W014134

    p-Amidinophenylmethylsulfonylfluoride hydrochloride

    Others Others
    p-APMSF is an irreversible inhibitor of serinase. p-APMSF has substrate specificity for positively charged side chains of amino acids, lysine, or arginine. p-APMSF can be used to study the irreversible inhibition of trypsin and thrombin .
    p-APMSF hydrochloride
  • HY-139852

    Phosphatase Cancer
    PLAP-IN-1 is a potent (IC50 = 32 nM) and selective PLAP inhibitor, with no detectable inhibition of tissue non-specific alkaline phosphatase (TNAP) activity.
    PLAP-IN-1
  • HY-116850

    EG626; Phthalazinol; SC-32840

    Phosphodiesterase (PDE) Neurological Disease
    Oxagrelate is a specific inhibitor of cyclic adenosine monophosphate phosphodiesterase and exhibits concentration-dependent inhibition of collagen- and ADP-induced platelet aggregation in vitro .
    Oxagrelate
  • HY-149859

    HDAC Neurological Disease
    HDAC-IN-58 is a HDAC inhibitor. HDAC-IN-58 has HDAC6-specific inhibition activity with an IC50 value of 2.06 nM. HDAC-IN-58 can be used for the research of chronic diseases, including neurodegenerative and psychiatric conditions .
    HDAC-IN-58
  • HY-101370

    Others Metabolic Disease
    2-Methylthio-ATP tetrasodium is a non-specific P2-receptor agonist. 2-Methylthio-ATP tetrasodium causes noncompetitive inhibition of ADP-induced human platelet aggregation .
    2-Methylthio-ATP tetrasodium
  • HY-13714

    AG 337 free base

    Others Others
    Nolatrexed (AG 337 free base) is a compound with antifolate activity, high oral bioavailability, and major toxicity at inhibitory doses is gastrointestinal reactions. It can be safely taken orally at specific doses for inhibition, with effects on platelets and neutrophils.
    Nolatrexed
  • HY-160481

    Tau Protein MicroRNA Neurological Disease
    MG-1102 is first-in-class dual binder of monomeric tau and pre-miRNA-146a. MG-1102 shows specific inhibition of miRNA146a with IC50s of 0.21 mM and 0.36 mM specific inhibition of doublelabeled pre-miRNA146a and mono-labeled pre-miRNA146a, respectively. MG-1102 interacts with tau monomers with a Kd of 3.21 mM by surface plasmon resonance (SPR). MG-1102 is a potential multi-target-directed ligands (MTDLs) for Alzheimer’s disease (AD) .
    MG-1102
  • HY-117746

    Others Infection
    KSK120 is a potent inhibitor of drug-resistant infections with specific activity against Chlamydia trachomatis (C. trachomatis). KSK120 inhibits the developmental cycle of C. trachomatis, thereby reducing the infectivity of progeny bacteria. KSK120 targets the glucose-6-phosphate (G-6P) metabolic pathway of C. trachomatis, showing its potential application in antimicrobial inhibition. The mechanism of KSK120 may involve inhibition of the transcriptional machinery, which provides new ideas for the development of specific drugs against C. trachomatis infection .
    KSK120
  • HY-P5881

    PKC Cardiovascular Disease
    PKCα (C2-4) inhibitor peptide is a PKCα specific inhibitor peptide that blocks the inhibition of IKr by the α1A adrenoreceptor agonist A-61603 (HY-101366) .
    PKCα (C2-4) inhibitor peptide
  • HY-15320
    NBI-74330
    4 Publications Verification

    CXCR Inflammation/Immunology Endocrinology
    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of ( 125I)CXCL10 and ( 125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
    NBI-74330
  • HY-15802
    WZ4003
    5 Publications Verification

    AMPK Cancer
    WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1 (ARK5)/NUAK2, without significant inhibition on other 139 kinases.
    WZ4003
  • HY-145721A

    GED-0301 sodium

    TGF-beta/Smad Inflammation/Immunology
    Mongersen sodium is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen sodium restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen sodium can attenuate Crohn's disease-like experimental colitis in mice .
    Mongersen sodium
  • HY-50937
    ST 2825
    Maximum Cited Publications
    67 Publications Verification

    MyD88 Inflammation/Immunology
    ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity .
    ST 2825
  • HY-155338

    YAP Cancer
    SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity .
    SWTX-143
  • HY-145721

    GED-0301

    TGF-beta/Smad Inflammation/Immunology
    Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice .
    Mongersen
  • HY-121328

    S-2852F

    Parasite Infection Neurological Disease
    Empenthrin (S-2852F) is a synthetic pyrethroid. Empenthrin can be used in insecticides. Empenthrin shows a clear species-specificity in the inhibitory effect on the Pentobarbital (PTB)-metabolizing enzyme(s). Empenthrin prolongs PTB induced-sleeping time in mice through an inhibition of the PTB-metabolizing enzyme(s) in the liver, an effect that does not occur in rats. Empenthrin shows a clear species-specificity in the inhibitory effect on the PTB-metabolizing enzyme(s) .
    Empenthrin
  • HY-P9915
    Daratumumab
    1 Publications Verification

    Anti-Human CD38, Human Antibody

    CD38 ADC Antibody Inflammation/Immunology Cancer
    Daratumumab (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab has anti-multiple myeloma (MM) effect. Daratumumab impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
    Daratumumab
  • HY-15838
    ID-8
    4 Publications Verification

    DYRK Cancer
    ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs .
    ID-8
  • HY-133118
    6RK73
    2 Publications Verification

    Deubiquitinase Cancer
    6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer .
    6RK73
  • HY-101122

    SGLT Metabolic Disease
    LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract .
    LX2761
  • HY-P9915A
    Daratumumab (PBS)
    1 Publications Verification

    Anti-Human CD38, Human Antibody (PBS)

    ADC Antibody CD38 Cancer
    Daratumumab (PBS) (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab (PBS) has anti-multiple myeloma (MM) effect. Daratumumab (PBS) impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
    Daratumumab (PBS)
  • HY-156034

    NLRP3-IN-19

    NOD-like Receptor (NLR) Inflammation/Immunology
    JT001 (NLRP3-IN-19) is a potent, specific and orally active inhibitor of NLRP3. JT001 can inhibit NLRP3 inflammasome assembly, resulting in the inhibition of cytokine release and the prevention of pyroptosis. JT001 can be used for the research of nonalcoholic steatohepatitis and liver fibrosis .
    JT001
  • HY-156034A

    NLRP3-IN-19 sodium

    NOD-like Receptor (NLR) Inflammation/Immunology
    JT001 (NLRP3-IN-19) sodium is a potent, specific and orally active inhibitor of NLRP3. JT001 sodium can inhibit NLRP3 inflammasome assembly, resulting in the inhibition of cytokine release and the prevention of pyroptosis. JT001 sodium can be used for the research of nonalcoholic steatohepatitis and liver fibrosis .
    JT001 sodium
  • HY-128348

    RIP kinase Inflammation/Immunology Cancer
    PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis .
    PK68
  • HY-125693

    Fungal Infection Neurological Disease
    L685818 is a specific immunophilin ligand. L685818 was neuroregenerative and non-neuroprotective in primary brain cultures. L685818 protects dopaminergic neurons from toxic inhibition of MPP+ and 6-OHDA, reduces tyrosine hydroxylase (TH) loss, and promotes neuronal process regeneration. L685818 is also an antifungal reagent for Cryptococcus neoformans .
    L685818
  • HY-168094

    PARP Cancer
    PARP1-IN-30 (Compound 3) is a specific and potent PARP1 inhibitor with cytotoxicity. PARP1-IN-30 allows precise inhibition of PARP1 in tumor cells with breast cancer 1 protein (BRCA1) or BRCA2 deficiencies. PARP1-IN-30 is promising for research of cancers .
    PARP1-IN-30
  • HY-15798

    VSV TAM Receptor Cardiovascular Disease
    UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC50s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research .
    UNC2881
  • HY-18754

    p38 MAPK Autophagy Endocrinology
    FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo .
    FR 167653 free base
  • HY-100421
    CPI-455
    5+ Cited Publications

    Histone Demethylase Cancer
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
    CPI-455
  • HY-P1597
    Malantide
    1 Publications Verification

    PKA PKC Cancer
    Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a Km of 16 μM .
    Malantide
  • HY-18754A

    FR 167653 sulfate

    p38 MAPK Autophagy Endocrinology
    FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo .
    FR 167653
  • HY-116788
    Lipofermata
    2 Publications Verification

    Bacterial Infection
    Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM .
    Lipofermata
  • HY-108645

    p38 MAPK Autophagy Inflammation/Immunology
    AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity .
    AL 8697
  • HY-100421A

    Histone Demethylase Cancer
    CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
    CPI-455 hydrochloride
  • HY-141677B

    Histone Demethylase Cancer
    INCB059872 tosylate is a potent, selective and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, enhancing H3K4 methylation, thereby increasing the expression of tumor suppressor genes. INCB059872 inhibition also promotes H3K9 methylation, thereby reducing the transcription of tumor-promoting genes .
    INCB059872 tosylate
  • HY-P1597A

    PKA PKC Cancer
    Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM .
    Malantide TFA
  • HY-129388A

    CC-90011; LSD1-IN-7

    Histone Demethylase Cancer
    Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
    Pulrodemstat
  • HY-120072
    PF-3450074
    3 Publications Verification

    PF-74

    HIV Infection
    PF-3450074 (PF-74) is a specifical inhibitor of?HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle . CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
    PF-3450074
  • HY-121998

    Aurora Kinase Others
    Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
    Binucleine 2
  • HY-118041

    Others Cancer
    PMPMEase-IN-1 is an allylated methylated protein methylesterase inhibitor with the property of inhibiting PMPMEase activity. PMPMEase-IN-1 may provide a useful strategy for cancer inhibition by enhancing its affinity for polyisoprenyl derivatives. PMPMEase-IN-1 showed the potential to have an effective concentration (EC50) value in causing degeneration of human neuroblastoma SH-SY5Y cells. Specific inhibition of PMPMEase-IN-1 may help regulate the metabolism of polyisoprenyl proteins and thus maintain normal cell survival. Further development and application of PMPMEase-IN-1 may open up new avenues for inhibiting degenerative diseases and cancer .
    PMPMEase-IN-1
  • HY-129388B
    Pulrodemstat benzenesulfonate
    2 Publications Verification

    CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate

    Histone Demethylase Cancer
    CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
    Pulrodemstat benzenesulfonate
  • HY-105056

    Ro 16-6028

    GABA Receptor Neurological Disease
    Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
    Bretazenil
  • HY-N0822
    Shikonin
    30+ Cited Publications

    C.I. 75535; Isoarnebin 4

    Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV AIM2 Cancer
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .
    Shikonin
  • HY-108350

    Epigenetic Reader Domain Cancer
    MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation .
    MI-2-2
  • HY-129388

    CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate

    Histone Demethylase Cancer
    CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
    Pulrodemstat Methylbenzenesulfonate
  • HY-115570
    GW406108X
    1 Publications Verification

    GW108X

    Kinesin ULK Autophagy Cancer
    GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK .
    GW406108X
  • HY-138215

    ERK Cancer
    ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and ERK5, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo .
    ADTL-EI1712

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