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Results for "

domain

" in MCE Product Catalog:

311

Inhibitors & Agonists

3

Screening Libraries

2

Dye Reagents

1

Biochemical Assay Reagents

47

Peptides

7

Inhibitory Antibodies

13

Natural
Products

293

Recombinant Proteins

11

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-P9802
    Anti-Spike-RBD Single Domain mAb

    SARS-CoV-2 (2019-nCoV) Single-domain Antibodies; Humanized Single domain Antibody

    SARS-CoV Infection
    Anti-Spike-RBD Single Domain mAb is a CHO cell derived Alpaca monoclonal VHH-huFc antibody, specifically binds to SARS-CoV-2 RBD with high affinity.
  • HY-138283
    MR837

    Histone Methyltransferase Cancer
    MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain).
  • HY-141539
    SETDB1-TTD-IN-1

    Histone Methyltransferase Cancer
    SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD), with a Kd of 88 nM. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD.
  • HY-117570
    KSC-34

    Others Neurological Disease
    KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family.
  • HY-13956
    Pioglitazone

    U 72107

    PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  • HY-15098
    Apoptozole

    Apoptosis Activator VII

    HSP Apoptosis Cancer
    Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
  • HY-13956S
    Pioglitazone-d4

    U 72107-d4

    PPAR Ferroptosis Cancer Metabolic Disease
    Pioglitazone D4 (U 72107 D4) is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  • HY-141799
    Dimethyl-F-OICR-9429-COOH

    Ligands for Target Protein for PROTAC Cancer
    Dimethyl-F-OICR-9429-COOH a ligand for WD40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1 intermediate 19. Dimethyl-F-OICR-9429-COOH can be used in the synthesis of PROTACs.
  • HY-125399
    PSMA-11

    HBED-CC-PSMA

    Others Cancer
    PSMA-11 is a positron emission tomography (PET) tracer. PSMA-11 detects prostate cancer relapses and metastases by binding to the extracellular domain of prostate-specific membrane antigen (PSMA).
  • HY-18377
    Bioymifi

    DR5 Activator

    TNF Receptor Apoptosis Cancer
    Bioymifi (DR5 Activator), a potent TRAIL receptor DR5 activator, binds to the extracellular domain (ECD) of DR5 with a Kd of 1.2 μM. Bioymifi can act as a single agent to induce DR5 clustering and aggregation, leading to apoptosis.
  • HY-141798
    OICR-9429-N-C2-NH2

    Ligands for Target Protein for PROTAC Cancer
    OICR-9429-N-C2-NH2 is a ligand for Wd40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1, intermediate 2. OICR-9429-N-C2-NH2 can be used in the synthesis of PROTACs.
  • HY-116501
    VPC-14449

    Androgen Receptor Cancer
    VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer.
  • HY-131346
    HIF-PHD-IN-1

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia.
  • HY-123875A
    Ralaniten triacetate

    EPI-506

    Androgen Receptor Cancer
    Ralaniten triacetate (EPI-506), the pro-drug of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7.
  • HY-145932
    DMA-135 hydrochloride

    Enterovirus Infection
    DMA-135 hydrochloride inhibits enterovirus 71 (EV71) IRES-dependent translation and replication. DMA-135 hydrochloride binds to enterovirus 71 (EV71) SLII domain with moderately high affinity (KD= 520 nM). DMA-135 hydrochloride has no significant toxicity in cell-based studies.
  • HY-129527
    GNE-9278

    iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.
  • HY-102068
    Clathrin-IN-1

    HIV Infection
    Clathrin-IN-1 is a selective clathrin-mediated endocytosis (CME) inhibitor. Clathrin-IN-1 selectively inhibits amphiphysin association of clathrin terminal domain (TD) with an IC50 value of 12 μM. Clathrin-IN-1 acutely interferes with receptor-mediated endocytosis, entry of HIV, and synaptic vesicle recycling.
  • HY-110013
    Terreic acid

    Btk Antibiotic Infection Inflammation/Immunology
    Terreic acid, a quinone epoxide antibiotic, acts as an effective Btk inhibitor. Terreic acid blocks the interaction between PKC and the pleckstrin homology domain of Btk. Terreic acid inhibits the binding of GST-BtkPH to PKC in lysates of HMC-1 human mast cells with an IC50 of approximately 100 μM.
  • HY-N2521
    Tetramethylcurcumin

    FLLL31

    STAT Apoptosis Cancer Inflammation/Immunology
    Tetramethylcurcumin (FLLL31), derived from curcumin, specifically suppresses the phosphorylation of STAT3 by binding selectively to Janus kinase 2 and the STAT3 Src homology-2 domain. Tetramethylcurcumin exhibits anti-inflammatory and anti-cancer effects.
  • HY-109070
    Ralaniten

    EPI-002

    Androgen Receptor Cancer
    Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC).
  • HY-100348
    EPI-001

    Androgen Receptor PPAR Apoptosis Cancer
    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
  • HY-125837
    MS31

    Epigenetic Reader Domain Cancer
    MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells.
  • HY-125837A
    MS31 trihydrochloride

    Epigenetic Reader Domain Cancer
    MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells.
  • HY-103076
    EZ-482

    Others Neurological Disease
    EZ-482, a novel ligand of apolipoprotein (apoE), binds to sites on apoE in the C-terminal domain with Kds of 5-10 μM for apoE3 and apoE4. EZ-482 binds to apoE4 by a unique N-terminal allosteric effect. EZ482 has the potential for Alzheimer’s diseas.
  • HY-124308
    PS315

    PKC Cancer
    PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity.
  • HY-126666
    PNU-159682 carboxylic acid

    ADC Cytotoxin Cancer Inflammation/Immunology
    PNU-159682 carboxylic acid (compound 53) is a potent ADCs cytotoxin and encodes a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. PNU-159682 carboxylic acid has protein fold and diverse functions, such as cell adhesion, cell-cell signalling, glycoprotein turnover, and roles in inflammation and immune response.
  • HY-107506
    Ro 67-4853

    mGluR Neurological Disease
    Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.
  • HY-P3279
    EPQpYEEIPIYL

    Src Cancer
    EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains.
  • HY-P1377
    Caffeic acid-pYEEIE

    Src Inflammation/Immunology
    Caffeic acid-pYEEIE, a non-phosphopeptide inhibitor, exhibits potent binding affinity for the GST-Lck-SH2 domain.
  • HY-P1377A
    Caffeic acid-pYEEIE TFA

    Src Inflammation/Immunology
    Caffeic acid-pYEEIE TFA, a non-phosphopeptide inhibitor, exhibits potent binding affinity for the GST-Lck-SH2 domain.
  • HY-P1755
    p53 (17-26)

    MDM-2/p53 Cancer
    p53 (17-26) is amino acids 17 to 26 fragment of p53. p53 (17-26) is mdm-2-binding domain.
  • HY-104068
    Naphthol AS-E

    Histone Acetyltransferase Epigenetic Reader Domain Cancer
    Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 µM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 µM. Naphthol AS-E can be used for cancer research.
  • HY-P1985A
    Notch 1 TFA

    Notch Cancer Cardiovascular Disease
    Notch 1 TFA (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types.
  • HY-132203
    Necrostatin-34

    RIP kinase Cancer Inflammation/Immunology
    Necrostatin-34 (Nec-34), a RIPK1 kinase inhibitor, stabilizes RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain.
  • HY-13638
    GDC-0152

    IAP Cancer
    GDC-0152 is a potent IAPs inhibitor, and binds to the BIR3 domains of XIAP, cIAP1, cIAP2 and the BIR domain of ML-IAP with Ki values of 28 nM, 17 nM, 43 nM and 14 nM, respectively.
  • HY-124500
    AC-4-130

    STAT Cancer
    AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML).
  • HY-23999
    BI-0115

    Others Cardiovascular Disease
    BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain.
  • HY-145416
    G247

    Bacterial Infection
    G247 is a specific MsbA inhibitor. G247 acts as a transmembrane domains (TMDs) wedge, symmetrically increasing nucleotide-binding domains (NBDs) separation and preventing conformational transition of MsbA. G247 suppresses ATPase activity by increasing inter-NBD distance.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-146957
    ZIKV-IN-1

    Virus Protease Cancer
    ZIKV-IN-1 is a potent zika virus inhibitor with an EC50 of 2.8 µM and EC90 of 6.8 µM. ZIKV-IN-1 shows anti-ZIKV activity with low cytotoxicity. ZIKV-IN-1 shows a strong affinity to ZIKV RdRp domain.
  • HY-145103
    UNC6934

    Histone Methyltransferase Cancer
    UNC6934, a chemical probe targeting the PWWP domain, alters NSD2 nucleolar localization.
  • HY-125292
    NV03

    Histone Methyltransferase Ligands for E3 Ligase Cancer
    NV03 is a potent and selective antagonist of UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)- H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 has anticancer activity.
  • HY-136546
    Stafia-1

    STAT Cancer
    Stafia-1 is a potent STAT5a inhibitor (K i=10.9 μM, IC50=22.2 μM). Stafia-1 displays high selectivity over STAT5b and other STAT family members.
  • HY-52101A
    FMK

    Ribosomal S6 Kinase (RSK) Cancer
    FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
  • HY-18685
    CPDA

    Phosphatase Metabolic Disease
    CPDA is a novel potent SH2 domain-containing inositol phosphatase 2 (SHIP2) inhibitor.
  • HY-112904
    XRK3F2

    Autophagy Others
    XRK3F2 is an inhibitor of p62 (Sequestosome-1)-ZZ/ domain.
  • HY-15827
    NSC 405020

    MMP Cancer
    NSC 405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM and does not inhibit the catalytic activity of MT1-MMP or MMP-2.
  • HY-101084
    NSC 228155

    EGFR Histone Acetyltransferase Epigenetic Reader Domain Cancer
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
  • HY-111549
    Bragsin1

    Others Cancer
    Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
  • HY-100337
    WWL70

    MAGL Neurological Disease
    WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM.
  • HY-112861
    Gln-AMS

    Aminoacyl-tRNA Synthetase Bacterial Infection
    Gln-AMS is an aminoacyl-tRNA synthetases (AARS) inhibitor, which binds the A-domain within the NRPS enzymes.
  • HY-114208
    BI-9321

    Histone Methyltransferase Cancer
    BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
  • HY-114208A
    BI-9321 trihydrochloride

    Histone Methyltransferase Cancer
    BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
  • HY-P0300
    Bak BH3

    Bcl-2 Family Cancer
    Bak BH3 is derived from the BH3 domain of Bak, can antagonize the function of Bcl-xL in cells.
  • HY-114157
    DO-264

    MAGL Neurological Disease
    DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM.
  • HY-145409
    SR-0813

    Epigenetic Reader Domain Cancer
    SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia.
  • HY-112292A
    GW806742X hydrochloride

    Mixed Lineage Kinase VEGFR Cancer
    GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis.
  • HY-112292
    GW806742X

    Mixed Lineage Kinase VEGFR Others
    GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X has activity against VEGFR2 (IC50=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis.
  • HY-124952
    iKIX1

    Fungal Infection
    iKIX1 is an antifungal agent and resensitizes drug-resistant C. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC50 and Ki values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection.
  • HY-136300
    PHD-1-IN-1

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Cardiovascular Disease
    PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe 2+ ion and induces the formation of an “Arg367-out” pocket.
  • HY-107985
    FT671

    Deubiquitinase Cancer
    FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.
  • HY-138067
    SSAA09E2

    SARS-CoV Inflammation/Immunology
    SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .
  • HY-112647
    Stafib-1

    STAT Cancer
    Stafib-1 is the first selective inhibitor of the STAT5b SH2 domain, with a Ki of 44 nM and an IC50 of 154 nM.
  • HY-119254
    BAY-850

    Epigenetic Reader Domain Metabolic Disease
    BAY-850 is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC50 of 166 nM.
  • HY-P1562
    PUMA BH3

    Bcl-2 Family Cancer
    PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-138779
    ICCB-19 hydrochloride

    Autophagy RIP kinase Apoptosis Inflammation/Immunology
    ICCB-19 hydrochloride is a TRADD (TNFRSF1A associated via death domain) inhibitor. ICCB-19 hydrochloride binds with N-terminal domain of TRADD (TRADD-N), disrupting its binding to both TRADD-C and TRAF2. ICCB-19 hydrochloride is indirect inhibitor of RIPK1 kinase activity. ICCB-19 hydrochloride effectively induces autophagy and the degradation of long-lived proteins.
  • HY-123348
    Sampatrilat

    UK-81252

    Angiotensin-converting Enzyme (ACE) Neprilysin Inflammation/Immunology Cardiovascular Disease
    Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase (NEP). Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation.
  • HY-16510A
    UNC926 hydrochloride

    Epigenetic Reader Domain Cancer
    UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC50 of 3.9 μM.
  • HY-16510
    UNC926

    Epigenetic Reader Domain Cancer
    UNC926 is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC50 of 3.9 μM.
  • HY-101524
    TC13172

    Mixed Lineage Kinase Cancer
    TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells.
  • HY-145562
    Deucrictibant

    Bradykinin Receptor Others
    Deucrictibant is a potent bradykinin receptor antagonist. Bradykinin receptors are cell surface, G-protein coupled receptors of the seven-transmembrane domained family.
  • HY-110287
    Apcin

    APC Cancer
    Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis.
  • HY-117287
    Deucravacitinib

    BMS-986165

    JAK Interleukin Related IFNAR Inflammation/Immunology
    Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways.
  • HY-112798
    PH-002

    Others Neurological Disease
    PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that could rescue impairments of mitochondrial motility and neurite outgrowth.
  • HY-W018931
    DDR Inhibitor

    Discoidin Domain Receptor Cancer
    DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
  • HY-12134
    Poloxin

    Polo-like Kinase (PLK) Cancer
    Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.
  • HY-N7177
    Hydroxytanshinone IIA

    Drug Metabolite VEGFR Cancer
    Hydroxytanshinone IIA is a hydroxylated metabolite of Tanshinone IIA. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.
  • HY-16046
    Rimiducid

    AP1903

    FKBP Apoptosis Cancer
    Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.
  • HY-101628
    VEGFR-2-IN-9

    KDR-in-4

    VEGFR Cardiovascular Disease
    VEGFR-2-IN-9 (KDR-in-4) is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC50 of 7 nM.
  • HY-115867
    GSK852

    Epigenetic Reader Domain Cancer
    GSK852 is a highly potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor (pIC50 = 7.9).
  • HY-111381
    BI-3812

    Bcl-2 Family Cancer
    BI-3812 is potent and efficacious BCL6 inhibitor, inhibiting the BTB domain of BCL6, with an IC50 of ≤3 nM; BI-3812 has antitumor activity.
  • HY-120215
    KT203

    MAGL Metabolic Disease
    KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
  • HY-19776
    3α-Aminocholestane

    Phosphatase Cancer
    3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
  • HY-120177
    KT182

    MAGL Others
    KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
  • HY-112862
    Arg-AMS

    Aminoacyl-tRNA Synthetase Others
    Arg-AMS is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes.
  • HY-100015
    Mivebresib

    ABBV-075

    Epigenetic Reader Domain Apoptosis Cancer
    Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.
  • HY-U00447
    PK11000

    MDM-2/p53 DNA Alkylator/Crosslinker Cancer
    PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 by covalent cysteine modification, without compromising DNA binding.
  • HY-B0795
    MHY1485

    mTOR Autophagy Cancer
    MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
  • HY-P2565
    Pepinh-TRIF TFA

    Toll-like Receptor (TLR) Inflammation/Immunology
    Pepinh-TRIF (TFA) is a 30 aa peptide that blocks TIR-domain-containing adapter-inducing interferon-β (TRIF) signaling by interfering with TLR-TRIF interaction.
  • HY-16663
    ITX3

    Others Others
    ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 uM; inhibits TrioN-stimulated RhoG exchange in vitro.
  • HY-P1562A
    PUMA BH3 TFA

    Bcl-2 Family Cancer
    PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-128352
    SMYD3-IN-1

    Histone Methyltransferase Cancer
    SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM.
  • HY-110286
    6-Hydroxy-DOPA

    DNA/RNA Synthesis Cancer
    6-Hydroxy-DOPA is a selective and effective allosteric inhibitor of the RAD52 ssDNA binding domain. 6-Hydroxy-DOPA can be used for the research of cancer.
  • HY-115604
    Pitstop 2

    Apoptosis Cancer
    Pitstop 2 is a clathrin inhibitor which inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin. Pitstop 2 has the potential for anti-cancer research.
  • HY-N0135
    Tanshinone IIA

    Dan Shen ketone

    VEGFR Cardiovascular Disease Cancer
    Tanshinone IIA (Tan IIA) is one of the main compositions in the root of red-rooted salvia. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.
  • HY-100695
    DDR-TRK-1

    Discoidin Domain Receptor Cancer
    DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.
  • HY-119165
    GSM-1

    γ-secretase Neurological Disease
    GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).
  • HY-17513
    Amicarbazone

    BAY314666; BAY-MKH 3586

    Others Others
    Amicarbazone(BAY-MKH3586; BAY314666) is a potent inhibitor of photosynthetic electron transport via binding to the Qb domain of photosystem II (PSII); herbicide with a broad spectrum of weed control.
  • HY-12063
    PHT-427

    Akt Apoptosis Cancer
    PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
  • HY-D1398
    LtIA-F

    Others Neurological Disease
    LtIA-F, a novel fluorescent analogue of LtIA, provides a wealth of pharmacological tools to explore the structure–function relationship, distribution, and ligand binding domain of the α3β2 nAChR subtype.
  • HY-122234
    VPC-18005

    Others Cancer
    VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity.
  • HY-122816
    HLY78

    Wnt Cancer Neurological Disease
    HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction.
  • HY-129121
    ML-​226

    MAGL Neurological Disease
    ML226 is a potent α/β hydrolase domain-containing protein 11 (ABHD11) inhibitor in vitro and in situ with IC50s of 15 and 0.68 nM, respectively.
  • HY-100691
    NOD-IN-1

    NOD-like Receptor (NLR) Inflammation/Immunology
    NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2, with IC50 of 5.74 μM and 6.45 μM, respectively.
  • HY-136242
    UT-34

    Androgen Receptor Cancer Endocrinology
    UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy.
  • HY-U00444
    7rh

    DDR1-IN-2

    Discoidin Domain Receptor Inflammation/Immunology
    7rh (DDR1-IN-2) is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.
  • HY-19730
    Olmutinib

    HM61713, BI 1482694

    EGFR Cancer
    Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC.
  • HY-18749
    SC79

    Akt Cancer Inflammation/Immunology Neurological Disease
    SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.
  • HY-106723
    AMP-PCP

    HSP Cancer
    AMP-PCP is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP binding favors the formation of the active homodimer of Hsp90.
  • HY-15649
    UNC1215

    Histone Methyltransferase Apoptosis Cancer
    UNC1215 is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a Kd value of 120 nM and an IC50 of 40 nM. UNC1215 has the potential to treat malignant brain tumor.
  • HY-P99040
    Onvatilimab

    JNJ-61610588

    PD-1/PD-L1 Cancer
    Onvatilimab (JNJ-61610588) is a human IgG1κ anti-VISTA (V-domain Ig Suppressor of T-cell Activation) monoclonal antibody. Onvatilimab has an anti-tumor activity.
  • HY-P1586
    HIV-1 Rev (34-50)

    HIV-1 rev Protein (34-50)

    HIV Infection
    HIV-1 Rev (34-50) is a 17-aa peptide derived from the Rev-responsive element (RRE)-binding domains of Rev in HIV-1, with anti-HIV-1 activity.
  • HY-135232
    MMP-9-IN-1

    MMP Cancer
    MMP-9-IN-1 is a specific matrix metalloproteinase-9 (MMP-9) inhibitor, which selectively target the hemopexin (PEX) domain of MMP-9, but not other MMPs.
  • HY-18937
    WEHI-345

    RIP kinase Cancer
    WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.
  • HY-50898
    Lapatinib

    GW572016; GW2016

    EGFR Autophagy Ferroptosis Cancer
    Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
  • HY-106723A
    AMP-PCP disodium

    HSP Cancer
    AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90.
  • HY-15839
    UNC 669

    Epigenetic Reader Domain Cancer
    UNC 669, a ligand for a methyl-lysine binding domain, is a potent L3MBTL1 (IC50=4.2 uM) and L3MBTL3 (3.1 uM) inhibitor.
  • HY-120097
    R-10015

    LIM Kinase (LIMK) Reverse Transcriptase Infection
    R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1.
  • HY-107985A
    (R)-FT671

    Others Others
    (R)-FT671 is the R-isomer of FT671. FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.
  • HY-136257
    CMP98

    PROTACs Others
    CMP98, a PROTAC, is unable to induce degradation of VHL. CMP98 can be used as a negative control compound for CM11. CMP98 consists of two von Hippel-Lindau ligands on their active domain.
  • HY-N0170
    Indole-3-carbinol

    I3C; 3-Indolemethanol

    NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite Cancer
    Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
  • HY-50898B
    Lapatinib ditosylate

    GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate

    EGFR Autophagy Ferroptosis Cancer
    Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
  • HY-50898A
    Lapatinib ditosylate

    GW572016 ditosylate; GW2016 ditosylate

    EGFR Autophagy Ferroptosis Cancer
    Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
  • HY-N5024
    Gambogenic acid

    Histone Methyltransferase Cancer
    Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination.
  • HY-P1847
    IKKγ NBD Inhibitory Peptide

    NF-κB Cancer
    IKKγ NBD Inhibitory Peptide is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation.
  • HY-15989A
    SM-164 Hydrochloride

    IAP Apoptosis Cancer
    SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
  • HY-110346
    AZD5582 dihydrochloride

    IAP Apoptosis Cancer
    AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
  • HY-12600
    AZD5582

    IAP Apoptosis Cancer
    AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
  • HY-143886
    AD011

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    AD011 is a dual inhibitor of cACE/NEP. AD011 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD011 has the potential for providing the potent antihypertensive and cardioprotective benefits.
  • HY-143888
    AD013

    Angiotensin-converting Enzyme (ACE) Others
    AD013 is a dual inhibitor of cACE/NEP. AD013 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD013 has the potential for providing the potent antihypertensive and cardioprotective benefits.
  • HY-15989
    SM-164

    IAP Apoptosis Cancer
    SM-164 is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
  • HY-143887
    AD012

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    AD012 is a dual inhibitor of cACE/NEP. AD012 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD012 has the potential for providing the potent antihypertensive and cardioprotective benefits.
  • HY-109143
    Elsubrutinib

    ABBV-105

    Btk Inflammation/Immunology
    Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease.
  • HY-124711
    TBOPP

    Others Cancer
    TBOPP is a selective inhibitor of DOCK1 with an IC50 of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (Kd of 7.1 μM), has anti-tumor activity for broader types of tumors.
  • HY-W011400
    TLR1

    MyD88 Inflammation/Immunology
    TLR1 (compound 4a) is a low molecular weight, cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic. TLR1 inhibits IL-1 receptor-mediated responses.
  • HY-119039
    RU-301

    TAM Receptor Cancer
    RU-301 is a pan-TAM receptor inhibitor, exerts pan-TAM inhibitory activity by binding at the interface between Gas6 and the Ig1 domain of the respective TAMs with Kd and IC50 values of 12 μM and 10 μM, respectively.
  • HY-114173
    DDR1-IN-4

    Discoidin Domain Receptor Inflammation/Immunology
    DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.
  • HY-P1847A
    IKKγ NBD Inhibitory Peptide TFA

    NF-κB Inflammation/Immunology
    IKKγ NBD Inhibitory Peptide TFA is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation.
  • HY-12693
    R(+)-IAA-94

    R(+)-Methylindazone

    Chloride Channel Others
    R(+)-IAA-94 (R(+)-Methylindazone) is a potent indanyloxyacetic acid blocker of epithelial chloride channels. R(+)-IAA-94 inhibits Nef-sdAb19 (single-domain antibody) interaction and binds to negative factor (Nef).
  • HY-12345
    ML365

    Potassium Channel Cardiovascular Disease
    ML365 is a selective two-pore domain potassium channel KCNK3/TASK1 inhibitor, with an IC50 of 4 nM. ML365 acts as a pharmacological tool that can be used to examine the specific roles of TASK1 channels.
  • HY-141430
    AS-85

    Histone Methyltransferase Cancer
    AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 µM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78 µM.
  • HY-15369
    FPA-124

    Akt Apoptosis Cancer
    FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis.
  • HY-104021
    GSK840

    GSK'840

    RIP kinase Inflammation/Immunology
    GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.
  • HY-101457
    JZP-430

    MAGL Metabolic Disease
    JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).
  • HY-111547
    M1001

    HIF/HIF Prolyl-Hydroxylase Cancer
    M1001 is a weak agonist of HIF-2α, directly binds to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 enhances the stabilities of HIF-2α-ARNT complex.
  • HY-10528
    Tasquinimod

    ABR-215050

    HDAC Cancer
    Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.
  • HY-120210
    XY018

    ROR Cancer Inflammation/Immunology
    XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).
  • HY-10799
    EG00229

    Complement System Cancer
    EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2.
  • HY-P9807
    Anti-SARS-CoV-2 Spike mAb (CR3022)

    SARS-CR3022; SARS-CoV-2 Antibody-CR3022

    SARS-CoV Infection Inflammation/Immunology
    Anti-SARS-CoV-2 Spike mAb (CR3022) is a a CHO cell derived human monoclonal IgG1 antibody. It binds to both S1 domain of SARS-CoV/SARS-CoV-2 Spike protein.
  • HY-108697
    PT2399

    HIF/HIF Prolyl-Hydroxylase Cancer
    PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.
  • HY-141796
    MS67

    Histone Methyltransferase PROTACs Cancer
    MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.
  • HY-103666
    CY-09

    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-125402
    GSK-843

    GSK'843

    RIP kinase Inflammation/Immunology
    GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM.
  • HY-126316
    Zapalog

    FKBP Others
    Zapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis.
  • HY-100112
    WEHI-345 analog

    Others Others
    WEHI-345 analog is the analog of WEHI-345. WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.
  • HY-128760
    COH34

    Others Cancer
    COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors.
  • HY-139831
    Galectin-8-IN-1

    Others Cancer
    Galectin-8-IN-1 is a selective ligand for the galectin-8 N-terminal domain (galectin-8N), with a Kd of 48 μM and 15-fold selectivity over galectin-3 and even better selectivity over the other mammalian galectins.
  • HY-134849
    PAPD5-IN-1

    DNA/RNA Synthesis Neurological Disease
    PAPD5-IN-1 is a PAP associated domain containing 5 (PAPD5) inhibitor, extracted from patent WO2019084271A1. PAPD5-IN-1 can be used for aging-related degenerative disorders and other diseases research.
  • HY-110392
    CMP8

    Estrogen Receptor/ERR Cancer
    CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively.
  • HY-112800
    cyt-PTPε Inhibitor-1

    Phosphatase Metabolic Disease
    cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.
  • HY-115467
    MitoBloCK-10

    Others Metabolic Disease
    MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70.
  • HY-125378
    SBP-0636457

    SBI-0636457; SB1-0636457

    IAP Cancer
    SBP-0636457 (SB1-0636457) is a SMAC mimetic, and as an IAP antagonist. SBP-0636457 binds to the BIR-domains of the IAP proteins, with a Ki of 0.27 μM. SBP-0636457 can be used for the research of solid tumors and hematologic cancers.
  • HY-P1933A
    [pSer2, pSer5, pSer7]-CTD TFA

    CDK Cancer
    [pSer2, pSer5, pSer7]-CTD (TFA), a substrate for CDK7 (cyclin dependent protein kinase), is a phosphorylated polypeptide at ser2, ser5 and ser7 sites of RNA polymerase II carboxy-terminal domain (CTD).
  • HY-18686
    AS1949490

    Phosphatase Metabolic Disease
    AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes.
  • HY-109176
    Giredestrant

    GDC-9545

    Estrogen Receptor/ERR Cancer
    Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
  • HY-129602
    SD-36

    PROTACs STAT Apoptosis Cancer
    SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-115531
    UNC-2170

    Others Cancer
    UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC50=29 µM; Kd=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB).
  • HY-114311
    FGFR1/DDR2 inhibitor 1

    FGFR Discoidin Domain Receptor Cancer
    FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.
  • HY-P0295
    Gly-Arg-Gly-Asp-Ser

    Integrin Others
    Gly-Arg-Gly-Asp-Ser is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM
  • HY-111350
    FT827

    Deubiquitinase Cancer
    FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 µM). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 µM.
  • HY-P1566
    MPG, HIV related

    HIV Infection
    MPG, HIV related is 27-aa peptide, derived from both the nuclear localisation sequence of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41 and is a potent delivery agent for the generalised delivery of nucleic acids and of oligonucleotides into cultured cells.
  • HY-121725
    MM-206

    STAT Cancer
    MM-206, a STAT3 activity inhibitor, potently inhibits the STAT3 SH2 domain-phosphopeptide interaction with IC50 of 1.2 μM. MM-206 demonstrates dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines.
  • HY-135903
    Giredestrant tartrate

    GDC-9545 tartrate

    Estrogen Receptor/ERR Cancer
    Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity.
  • HY-136179
    ZAP-180013

    Tyrosinase Inflammation/Immunology
    ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).
  • HY-P9920
    Ramucirumab

    VEGFR Cancer
    Ramucirumab is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D.
  • HY-123847
    KPT-6566

    Others Cancer
    KPT-6566, a potent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain. Anti-cancer activity.
  • HY-P0175A
    740 Y-P TFA

    740YPDGFR TFA; PDGFR 740Y-P TFA

    PI3K Autophagy Cancer
    740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
  • HY-13818
    Stattic

    STAT Apoptosis Cancer Inflammation/Immunology
    Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727). Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice.
  • HY-132232
    GSK097

    Epigenetic Reader Domain Cancer
    GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media.
  • HY-146728
    STAT3-IN-10

    STAT Apoptosis Cancer
    STAT3-IN-10 (A11) is a STAT3 inhibitor with an IC50 value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, inhibits tumor cell growth and induces apoptosis in cancer cells.
  • HY-126242S
    Tyk2-IN-7

    JAK Inflammation/Immunology
    Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 (Compound 48) provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 (Compound 48) provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model.
  • HY-P2499
    BAD (103-127) (human), FAM-labeled

    Bcl-2 Family Cancer
    BAD (103-127) (human), FAM-labeled is a FAM-labeled human BAD (103-127) (HY-P2468). BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL.
  • HY-100530B
    Sp-cAMPS

    PKA Phosphodiesterase (PDE) Neurological Disease
    Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM.
  • HY-100530C
    Sp-cAMPS sodium salt

    PKA Phosphodiesterase (PDE) Neurological Disease
    Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.
  • HY-108486
    Herbimycin A

    Bacterial Antibiotic Infection
    Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
  • HY-13956S2
    Pioglitazone-d4 N-Oxide

    PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone-d4 N-Oxide is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  • HY-N0135S
    Tanshinone IIA-d6

    Dan Shen ketone-d6

    VEGFR Cardiovascular Disease Cancer
    Tanshinone IIA-d6 (Dan Shen ketone-d6) is the deuterium labeled Tanshinone IIA. Tanshinone IIA (Tan IIA) is one of the main compositions in the root of red-rooted salvia. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.
  • HY-135401
    VU6015929

    Discoidin Domain Receptor Inflammation/Immunology
    VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production.
  • HY-N6769
    Radicicol

    Monorden

    HSP Bacterial Antibiotic Infection
    Radicicol is an inhibitor of Hsp90 with an IC50 value of 1 μM. Radicicol binds to the ATPase domain of Hsp90 and prevents maturation of Hsp90 clients, leading to proteasomal degradation. Radicicol is an antifungal antibiotic with antimalarial activity, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB.
  • HY-P0295A
    Gly-Arg-Gly-Asp-Ser TFA

    Integrin Inflammation/Immunology
    Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM.
  • HY-P0316
    TP508

    Thrombin NO Synthase Cardiovascular Disease
    TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 activates endothelial cells and stem cells to revascularize and regenerate tissues.
  • HY-100869
    MM-589

    Histone Methyltransferase Cancer
    MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
  • HY-126428
    ZL0580

    HIV Epigenetic Reader Domain Infection Inflammation/Immunology
    ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter.
  • HY-113649
    AKB-6899

    HIF/HIF Prolyl-Hydroxylase Cancer
    AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects.
  • HY-103661
    BI-6C9

    Mitochondrial Metabolism Apoptosis Neurological Disease
    BI-6C9 is a highly specific BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from mitochondrial apoptosis inducing factor (AIF) release and caspase-independent cell death in neurons.
  • HY-B1322A
    Amodiaquine

    Amodiaquin

    Parasite Histone Methyltransferase Infection Inflammation/Immunology Neurological Disease
    Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
  • HY-124699
    MMSET-IN-1

    Others Cancer
    MMSET-IN-1 is a multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) inhibitor against SETD2 and MMSET with IC50s of 0.49 and 3.3 μM, respectively. MMSET-IN-1 has a Kd of 1.6 μM for MMSET.
  • HY-50898S1
    Lapatinib-d7 dihydrochloride

    GW572016-d7 dihydrochloride; GW2016-d7 dihydrochloride

    EGFR Autophagy Ferroptosis Cancer
    Lapatinib-d7 (GW572016-d7) dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
  • HY-100573
    Necrosulfonamide

    Mixed Lineage Kinase Cancer
    Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis.
  • HY-124838
    EG1

    Others Cancer
    EG1, a specific Pax2 inhibitor, directly binds the paired domain of Pax2 (Kd=1.35-1.5 μM) and inhibits Pax2-DNA interactions. EG1 can inhibit embryonic kidney development, a process directly dependent on Pax2 activity.
  • HY-110204
    Heclin

    E1/E2/E3 Enzyme Others
    Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits several HECT ligases in tissue culture cells (IC50s=6.8, 6.3, and 6.9 μM for Smurf2, Nedd4, and WWP1 HECT ligase domains, respectively).
  • HY-139397
    TJ-M2010-5

    MyD88 Cardiovascular Disease
    TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI).
  • HY-P2468
    BAD (103-127) (human)

    Bcl-2 Family Cancer
    BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL. BAD (103-127) (human) is reported to have almost 800-fold higher affinity for Bcl-XL than the 16-mer peptide.
  • HY-127111
    NDI-091143

    ATP Citrate Lyase Cancer
    NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate.
  • HY-P9968
    Nimotuzumab

    EGFR Cancer
    Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a KD of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor drug, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC).
  • HY-111550
    Bragsin2

    Others Cancer
    Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC50 of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells.
  • HY-P3343A
    hFSH-β-(33-53) (TFA)

    Estrogen Receptor/ERR Cancer
    hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells.
  • HY-P0316A
    TP508 TFA

    Thrombin NO Synthase Cardiovascular Disease
    TP508 TFA is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 TFA activates endothelial cells and stem cells to revascularize and regenerate tissues.
  • HY-13968
    JW 55

    PARP Cancer
    JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively.
  • HY-P0175
    740 Y-P

    740YPDGFR; PDGFR 740Y-P

    PI3K Autophagy Cancer
    740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
  • HY-100624
    Ryuvidine

    CDK Others Cancer
    Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20 in vitro. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM and is cytotoxic against a range of human cancer cells.
  • HY-100869A
    MM-589 TFA

    Histone Methyltransferase Cancer
    MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
  • HY-50898BS
    Lapatinib-d7 ditosylate

    EGFR Autophagy Ferroptosis Cancer
    Lapatinib-d7 (GW572016-d7) ditosylate is the deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
  • HY-136555
    GSK717

    NOD-like Receptor (NLR) Inflammation/Immunology
    GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.
  • HY-124066
    RU-302

    TAM Receptor Cancer
    RU-302 is a pan TAM inhibitor that blocks the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain. RU-302 effectively blocks Gas6-inducible Axl receptor activation with a low micromolar IC50in cell assays, and suppresses lung cancer tumor growth.
  • HY-P2264
    KYL peptide

    Ephrin Receptor Inflammation/Immunology
    KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor. KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses.
  • HY-B1322
    Amodiaquine dihydrochloride dihydrate

    Amodiaquin dihydrochloride dihydrate

    Parasite Histone Methyltransferase Infection Inflammation/Immunology Neurological Disease
    Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
  • HY-124418
    SBI-477

    Others Metabolic Disease
    SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
  • HY-108705
    BI-3802

    Bcl-2 Family Cancer
    BI-3802 is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor activity.
  • HY-14422
    SR1078

    ROR Cancer
    SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription.
  • HY-133669
    DDR1-IN-5

    Discoidin Domain Receptor Cancer
    DDR1-IN-5 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 7.36 nM. DDR1-IN-5 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 4.1 nM. DDR1-IN-5 has anti-cancer activity.
  • HY-115739
    RTIL 13

    Ras Cancer Neurological Disease
    RTIL 13 is a potent inhibitor of dynamin GTPase, with an IC50 of 2.3 µM for dynamin I GTPase. RTIL 13 also targets pleckstrin homology lipid binding domain. RTIL 13 can inhibit receptor-mediated and synaptic vesicle endocytosis, with IC50s of 9.3 μM and 7.1 μM, respectively.
  • HY-112937
    GNE-6640

    Deubiquitinase Cancer
    GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.
  • HY-12283
    Rostafuroxin

    PST 2238

    Na+/K+ ATPase RSV Cardiovascular Disease
    Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na +,K +-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity.
  • HY-B1322B
    Amodiaquine dihydrochloride

    Amodiaquin dihydrochloride

    Parasite Histone Methyltransferase Infection Inflammation/Immunology Neurological Disease
    Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
  • HY-133670
    DDR1-IN-6

    Discoidin Domain Receptor Cancer
    DDR1-IN-6 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 9.72 nM. DDR1-IN-6 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 9.7 nM. DDR1-IN-6 has anti-cancer activity.
  • HY-110258
    ML334

    LH601A

    Keap1-Nrf2 Cancer
    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
  • HY-13956S1
    Pioglitazone-d4 (alkyl)

    PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  • HY-124314
    LEI-106

    MAGL Metabolic Disease
    LEI-106 is a potent, dual sn-1-Diacylglycerol lipase α (DAGL-α)/ABHD6 inhibitor with an IC50 of 18 nM for DAGL-α and a Ki of 0.8 μM for ABHD6. LEI-106 inhibits the hydrolysis of [ 14C]-sn-1-oleoyl-2-arachidonoyl-glycerol, the natural substrate of DAGL-α, with a Ki of 0.7 μM.
  • HY-100573S
    Necrosulfonamide-d4

    Mixed Lineage Kinase Cancer
    Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide. Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis.
  • HY-139782
    SKLB325

    Histone Demethylase Cancer
    SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .
  • HY-117833
    PXS-4681A

    Monoamine Oxidase Inflammation/Immunology
    PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects.
  • HY-111745
    Tyk2-IN-5

    JAK Inflammation/Immunology
    Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model.
  • HY-138280
    DTHIB

    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-P9806
    Anti-MERS-D12 mAb

    MERS-D12; MERS Antibody-D12

    SARS-CoV Infection
    Anti-MERS-D12 mAb (MERS-D12; MERS Antibody-D12) is a human monoclonal IgG1. Anti-MERS-D12 mAb binds directly to the DPP4 interacting region of the MERS-CoV Spike receptor binding domain (RBD) and effect neutralization by directly blocking receptor binding.
  • HY-128590
    PHT-7.3

    Ras Cancer
    PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity.
  • HY-112090
    ABBV-744

    Epigenetic Reader Domain HIV Cancer Infection Inflammation/Immunology
    ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with drug-like properties enable the investigation of its antitumor efficacy and tolerability.
  • HY-101451
    PBIT

    Histone Demethylase Cancer
    PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively.
  • HY-B1322AS
    Amodiaquine-d10

    Parasite Histone Methyltransferase Infection Inflammation/Immunology Neurological Disease
    Amodiaquine-d10 is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
  • HY-122611
    CSRM617

    Androgen Receptor Apoptosis Cancer
    CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
  • HY-129603
    SI-109

    STAT Ligands for Target Protein for PROTAC Cancer
    SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.
  • HY-111254
    GQ-16

    PPAR Metabolic Disease
    GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a Ki of 160 nM. GQ-16 is an effective inhibitor of Cdk5-mediated phosphorylation of PPARγ. GQ-16 is a partial agonist of PPARγ with reduced adipogenic actions. GQ-16 promotes insulin Sensitization without weight gain.
  • HY-126020
    Bractoppin

    DNA/RNA Synthesis RAD51 Cancer
    Bractoppin is a potent and selective drug-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response.
  • HY-14392
    5,6-Dichlorobenzimidazole riboside

    DRB

    CDK Cancer
    5,6-Dichlorobenzimidazole riboside is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. 5,6-Dichlorobenzimidazole riboside trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.
  • HY-N2587
    Irigenin

    Integrin Cancer
    Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells.
  • HY-122198
    ML367

    Others Cancer
    ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
  • HY-112338
    C188

    CPD188

    STAT Cancer
    C188 is a STAT3 inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC50= 0.7 μM).
  • HY-15147
    XAV-939

    β-catenin PARP Cancer
    XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively).
  • HY-101872A
    GSK-872 hydrochloride

    RIP kinase Inflammation/Immunology
    GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
  • HY-112804
    SGC-iMLLT

    Epigenetic Reader Domain Cancer
    SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with Kds of 0.129 and 0.077 μM, respectively.
  • HY-B0563
    Ropivacaine

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is used for the research of neuropathic pain management.
  • HY-114855
    BT2

    Bcl-2 Family Metabolic Disease
    BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM.
  • HY-B0563B
    Ropivacaine hydrochloride

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is widely used for neuropathic pain management in vivo.
  • HY-122746
    E67-2

    Histone Methyltransferase Cancer
    E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase.
  • HY-123905
    LIN28 inhibitor LI71

    MicroRNA Cancer
    LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells.
  • HY-N0460
    1-Caffeoylquinic acid

    NF-κB Cancer
    1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with Ki of 0.002 μM and binding energy of 1.50 Kcal/mol. 1-Caffeoylquinic acid has anti-oxidative stress ability. 1-Caffeoylquinic acid inhibits PD-1/PD-L1 interact.
  • HY-139979
    USP5-IN-1

    Deubiquitinase Cancer
    USP5-IN-1 (compound 64), a potent deubiquitinase USP5 inhibitor, binds to the USP5 ZnF-UBD with a KD of 2.8 μM. USP5-IN-1 is selective over nine proteins containing structurally similar ZnF-UBD domains. USP5-IN-1 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate.
  • HY-101872
    GSK-872

    RIP kinase Inflammation/Immunology
    GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
  • HY-80002
    BMX-IN-1

    BMX kinase inhibitor

    Btk BMX Kinase Cancer
    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
  • HY-N6712
    Thiolutin

    Acetopyrrothin

    Bacterial Antibiotic Infection Metabolic Disease
    Thiolutin (Acetopyrrothin) is a disulfide-containing antibiotic and anti-angiogenic compound produced by Streptomyces. Thiolutin inhibits the JAMM metalloproteases Csn5, Associated-molecule-with-the-SH3-Domain-of-STAM (AMSH) and Brcc36. Thiolutin is a potent and selective inhibitor of endothelial cell adhesion accompanied by rapid induction of Heat-shock protein beta-1 (Hsp27) phosphorylation.
  • HY-131031
    KCC-07

    DNA Alkylator/Crosslinker Cancer
    KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
  • HY-50845
    Avagacestat

    BMS-708163

    γ-secretase Notch Cancer
    Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.
  • HY-10235
    Telaprevir

    VX-950

    HCV Protease HCV SARS-CoV Infection
    Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide. Telaprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-110077
    API-1

    Akt Apoptosis Cancer
    API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL).
  • HY-110100
    CPYPP

    Others Inflammation/Immunology
    CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 DHR-2 for Rac1 in a dose-dependent manner with an IC50 of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9.
  • HY-100237
    SZL P1-41

    E1/E2/E3 Enzyme Apoptosis Cancer
    SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.
  • HY-B0563A
    Ropivacaine hydrochloride monohydrate

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo.
  • HY-B0563C
    Ropivacaine mesylate

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane.
  • HY-103463
    SA57

    FAAH MAGL Neurological Disease
    SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases.
  • HY-124761
    Poloppin

    Polo-like Kinase (PLK) Autophagy Cancer
    Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.
  • HY-131948
    3-Chlorodiphenylamine

    Potassium Channel Cardiovascular Disease
    3-Chlorodiphenylamine is a high affinity Ca 2+ sensitizer of cardiac muscle. 3-Chlorodiphenylamine is based on diphenylamine and binds to the isolated N-domain of cardiac troponin C (cTnC) (Kd=6 µM). 3-Chlorodiphenylamine is an excellent starting scaffold for the development of more potent Ca 2+-sensitizing compounds due to its small size, and can be used for systolic heart failure research.
  • HY-100671
    L002

    Histone Acetyltransferase STAT Cancer Inflammation/Immunology
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
  • HY-117977
    FCPR03

    Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects.
  • HY-132205
    DS45500853

    Estrogen Receptor/ERR Metabolic Disease
    DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).
  • HY-107390A
    AX-024 hydrochloride

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-124675
    MYCMI-6

    NSC354961

    c-Myc Apoptosis Cancer
    MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis.
  • HY-103565
    AMN082

    mGluR Neurological Disease
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-110088
    SCH529074

    MDM-2/p53 Cancer
    SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC).
  • HY-112610
    CF53

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
  • HY-117727
    Leriglitazone

    Hydroxypioglitazone

    PPAR Metabolic Disease
    Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM,induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM.
  • HY-P1200
    Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH

    Src Cancer
    Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is an inhibitor for src SH3-SH2:phosphoprotein interactions.
  • HY-119906
    Conglobatin

    FW-04-806

    HSP Apoptosis Cancer
    Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo.
  • HY-144120
    αGalCer-RBD

    SARS-CoV Infection
    αGalCer-RBD is a self-adjuvanting lipoprotein conjugate. αGalCer-RBD induces potent immunity against SARS-CoV-2 and its variants of concern. αGalCer-RBD conjugate induces RBD-specific, cytokine-producing T cell development. αGalCer-RBD has great potential to be an effective COVID-19 vaccine candidate. α-Galactosylceramide (αGalCer) is a potent invariant natural killer T cell (iNKT) agonist. RBD: receptor-binding domain
  • HY-143201
    DS20362725

    Estrogen Receptor/ERR Metabolic Disease
    DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).
  • HY-107390
    AX-024

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-120758
    SEL24-B489

    Pim FLT3 Apoptosis Cancer
    SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively.
  • HY-133512
    NCGC00249987

    Phosphatase Cancer
    NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC50s of 3 μM and 6.9 μM for Eya2 ED and MBP-Eya2 FL. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells.
  • HY-N2025
    Oroxin A

    PPAR Glucosidase Metabolic Disease
    Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
  • HY-141551
    GNE-274

    Estrogen Receptor/ERR Cancer
    GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research.
  • HY-105231
    Bryostatin 1

    PKC HIV Cancer Infection Inflammation/Immunology Neurological Disease
    Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.
  • HY-P1200A
    Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA

    Src Cancer
    Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA is an inhibitor for src SH3-SH2:phosphoprotein interactions.
  • HY-P1746A
    Protein Kinase C (19-31) (TFA)

    PKC (19-31) (TFA)

    PKC Inflammation/Immunology
    Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) TFA is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
  • HY-133121
    WDR5-IN-1

    Histone Methyltransferase Apoptosis Cancer
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
  • HY-103565A
    AMN082 free base

    mGluR Neurological Disease
    AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-P1746
    Protein Kinase C (19-31)

    PKC (19-31)

    PKC Inflammation/Immunology
    Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
  • HY-12725
    ML324

    Histone Demethylase HSV CMV Cancer
    ML324 is a potent JMJD2 demethylase inhibitor with antiviral activity. ML324 also exhibits inhibition for the histone demethylase KDM4B, with an IC50 of 4.9 μM. ML324 has potent anti-viral activity against both herpes simplex virus (HSV) and human cytomegalovirus (hCMV) infection via inhibition viral IE gene expression.
  • HY-10235S
    Telaprevir-d4

    VX-950-d4

    HCV Protease HCV SARS-CoV Infection
    Telaprevir-d4 (VX-950-d4) is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide. Telaprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-132301
    MCT4-IN-1

    Monocarboxylate Transporter Cancer
    MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research.
  • HY-133551
    WF-47-JS03

    RET Cancer
    WF-47-JS03 is a potent and selective RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration.
  • HY-145479
    PROTAC AR-V7 degrader-1

    PROTACs Androgen Receptor Cancer
    PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM.
  • HY-10108
    LY294002

    PI3K Casein Kinase DNA-PK Apoptosis Autophagy Cancer Infection
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator.
  • HY-100034
    NSC 663284

    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-19744
    T6167923

    MyD88 Inflammation/Immunology
    T6167923 is a potent and selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with an 50 of 2.7  μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
  • HY-135985
    DCLK1-IN-1

    Others Cancer
    DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC).
  • HY-145685
    RECQL5-IN-1

    Others Cancer
    RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer.
  • HY-101508
    GNA002

    Histone Methyltransferase Cancer
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
  • HY-112626
    CDK12-IN-2

    CDK Cancer
    CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12.
  • HY-116716
    PIN1 inhibitor API-1

    MicroRNA Cancer
    PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.
  • HY-103693
    NAZ2329

    Phosphatase Cancer
    NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
  • HY-P0117
    Tat-NR2B9c

    Tat-NR2Bct; NA-1

    iGluR NO Synthase Neurological Disease
    Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.
  • HY-P0117A
    Tat-NR2B9c TFA

    Tat-NR2Bct TFA; NA-1 TFA

    iGluR NO Synthase Neurological Disease
    Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.