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AIN

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111

Inhibitors & Agonists

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Inhibitory Antibodies

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Isotope-Labeled Compounds

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Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114153C

    c-Fms Neurological Disease
    PLX5622 in AIN-76A Diet (1200 ppm) contains 1200 mg of PLX5622 (HY-114153) per Kg of AIN-76 diet and it can be used for microglia clearance. PLX5622 in AIN-76A Diet (1200 ppm) is ideal choose for microglia function research in healthy/diseased states. PLX5622 in AIN-76A Diet (1200 ppm) has been verified by MedChemExpress (MCE).The color of PLX5622 in AIN-76A Diet (1200 ppm) provided by MCE is blue. Meanwhile, MCE will provide an equal amount of PLX5622-Free AIN-76A Diet (no added pigments) as a complimentary offering, which is used for the control group.
    PLX5622 in AIN-76A Diet (1200 ppm)
  • HY-P9927
    Secukinumab
    5+ Cited Publications

    AIN457

    Interleukin Related Inflammation/Immunology Cancer
    Secukinumab (AIN457) is a high affinity, human monoclonal antibody targeted against interleukin (IL)-17A. Secukinumab is the first-in-class anti-IL-17 agent used for the research of plaque psoriasis, ankylosing spondylitis and psoriatic arthritis .
    Secukinumab
  • HY-144433
    DNMT3A-IN-1
    2 Publications Verification

    DNA Methyltransferase Infection
    DNMT3A-IN-1 (compound 1) is an effective and selective DNMT3A inhibitor. DNMT3A-IN-1 exhibits inhibitory activity against DNMT3A, with KI values ranging from 9.16 to 18.85 μM (AdoMet) and 11.37 to 23.34 μM (poly dI-dC). DNMT3A-IN-1 can induce apoptosis in acute myeloid leukemia (AML) cell lines (Apoptosis) .
    DNMT3A-IN-1
  • HY-147066

    DYRK Cancer
    Dyrk1A-IN-4 is a potent and orally active Dyrk1A inhibitor. Dyrk1A-IN-4 exhibits IC50s against DYRK1A and DYRK2 of 2 nM and 6 nM. Dyrk1A-IN-4 exhibits the inhibition of the DYRK1A pSer520 autophosphorylation in U2OS cells with an IC50 of 28 nM. Dyrk1A-IN-4 can be used for the studies of ovarian adenocarcinoma, neuroblastoma and cervical squamous cell carcinoma .
    Dyrk1A-IN-4
  • HY-176842

    Eukaryotic Initiation Factor (eIF) Cancer
    eIF4A-IN-1 (Compound 79) is an eIF4A inhibitor that inhibits protein translation. eIF4A-IN-1 canb be used in gastric cancer research .
    eIF4A-IN-1
  • HY-148447

    Eukaryotic Initiation Factor (eIF) Cancer
    eIF4A-IN-3, Silvestrol (HY-13251) analogue, is an eIF4A inhibitor. eIF4A-IN-3 blocks protein translation initiation by interfering with eIF4F complex assembly, preferentially inhibiting translation of mRNAs with long, highly structured 5'-untranslated regions. eIF4A-IN-3 inhibits proliferation of human breast cancer cells. eIF4A-IN-3 has moderate apical to basolateral permeability in intestinal cell monolayers and a low efflux ratio .
    eIF4A-IN-3
  • HY-172997

    iGluR Neurological Disease
    GluN1/3A-IN-1 (Compound GM-10) is a GluN1/GluN3A NMDA receptor inhibitor. GluN1/3A-IN-1 exhibits potent inhibitory activity against GluN1/GluN3A (IC50: 0.98 µM). GluN1/3A-IN-1 exerts its inhibitory effect by targeting the pre-M1 region and forming hydrogen bond interactions with key residues. GluN1/3A-IN-1 can be used to study GluN1/GluN3A-related neurological diseases .
    GluN1/3A-IN-1
  • HY-D1474

    Wnt Cancer
    WNT7A-IN-1 sodium (1365-0109), a WNT7A inhibitor, disrupts the protein-protein interaction between WNT7A and its receptor FZD5, resulting in the upregulation of MHC-I expression. WNT7A-IN-1 sodium significantly increases the expression of MHC-I and p-p65,while concurrently reducing the expression of active β-catenin . WNT7A-IN-1 sodium (compound F) is also a photographic sensitizer in the green spectral region .
    WNT7A-IN-1 sodium
  • HY-146221
    Dyrk1A-IN-5
    1 Publications Verification

    DYRK Neurological Disease
    Dyrk1A-IN-5 (Compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. yrk1A-IN-5 exhibits significant selectivity for DYRK1B (IC50 = 600 nM) and CLK1 (IC50 = 500 nM), but shows almost no inhibition of DYRK2 (IC50 > 10 μM). Dyrk1A-IN-5 can be used for Down syndrome research .
    Dyrk1A-IN-5
  • HY-141890
    BAZ1A-IN-1
    1 Publications Verification

    Epigenetic Reader Domain Cancer
    BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A .
    BAZ1A-IN-1
  • HY-176844

    ADC Payload Drug Intermediate Cancer
    eIF4A-IN-1 intermediate (Compound 71E) is an intermediate of Eukaryotic translation initiation factor 4A (eIF4A) inhibitor. eIF4A-IN-1 intermediate can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs) .
    eIF4A-IN-1 intermediate
  • HY-170411

    Wnt Cancer
    WNT7A-IN-1 (1365-0109), a WNT7A inhibitor, disrupts the protein-protein interaction between WNT7A and its receptor FZD5, resulting in the upregulation of MHC-I expression. WNT7A-IN-1 significantly increases the expression of MHC-I and p-p65,while concurrently reducing the expression of active β-catenin. WNT7A-IN-1 (compound F) is also a photographic sensitizer in the green spectral region .
    WNT7A-IN-1
  • HY-170788

    Phosphodiesterase (PDE) Metabolic Disease
    PDE7A-IN-1 is an orally active and selective PDE7A inhibitor with an IC50 of 0.0037 μM against PDE7A. PDE7A-IN-1 shows excellent isozyme selectivity over PDE7B. PDE7A-IN-1 elevates intracellular cAMP levels, suppresses ECR5 enhancer activity and reduces sclerostin expression. PDE7A-IN-1 significantly increases bone mineral density in rats. PDE7A-IN-1 can be used for the study of osteoporosis .
    PDE7A-IN-1
  • HY-162937

    Kinesin Microtubule/Tubulin Cancer
    KIF18A-IN-13 (Compound 16) is an effective and orally active inhibitor of KIF18A with anticancer activity in vivo. KIF18A-IN-13 can be utilized for research in ovarian cancer .
    KIF18A-IN-13
  • HY-164220

    Phosphatase Bacterial Infection
    PPM1A-IN-1 (Compound IV-4) is an inhibitor for PP2C Ser/Thr phosphatase protein phosphatase Mg2+/Mn2+-dependent 1A. PPM1A-IN-1 exhibits antibacterial activity against Mycobacterium tuberculosis .
    PPM1A-IN-1
  • HY-W969907

    GSK-3 Others
    GSK3a-IN-38 is a groundbreaking small molecule that effectively inhibits GSK-3a activity.
    GSK3-IN-7
  • HY-175442

    iGluR Neurological Disease
    GluN1/3A-IN-2 (Compound DD-1) is a selective GluN1/GluN3A NMDA receptor inhibitor with an IC50 of 1.26  μM for GluN1/GluN3A NMDA receptor. GluN1/3A-IN-2 can be used for neurological and psychiatric disorders research .
    GluN1/3A-IN-2
  • HY-147060

    DYRK Neurological Disease
    Dyrk1A-IN-3 (Compound 8b), a highly selective dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease .
    Dyrk1A-IN-3
  • HY-44062

    Histone Methyltransferase Inflammation/Immunology Cancer
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer .
    G9a-IN-1
  • HY-145802

    Kinesin Microtubule/Tubulin Cancer
    KIF18A-IN-2 is a potent KIF18A inhibitor (IC50=28 nM). KIF18A-IN-2 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-2 can be used for researching cancer .
    KIF18A-IN-2
  • HY-162994

    Histone Acetyltransferase Cancer
    KAT6A-IN-1 is a KAT6A inhibitor with an IC50 of <10 μM. KAT6A-IN-1 can be used for the research of cancer .
    KAT6A-IN-1
  • HY-176402

    DYRK NO Synthase Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Dyrk1A-IN-13 (Compound 1) is a DYRK1A inhibitor (IC50: 41 nM). Dyrk1A-IN-13 reduces LPS-induced NO production and has antioxidant and anti-inflammatory activities. Dyrk1A-IN-13 can be used in the research of Alzheimer's disease, cancer and diabetes .
    Dyrk1A-IN-13
  • HY-157478

    Casein Kinase Infection
    CSNK2A-IN-1 (compound 7C) is a selective CSNK2A inhibitor. CSNK2A-IN-1 has antiviral activity and improved selectivity over PIM3 .
    CSNK2A-IN-1
  • HY-W231513

    MASTL Ser/Thr Protease Aurora Kinase Cancer
    MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis .
    MASTL/Aurora A-IN-1
  • HY-145803

    Kinesin Microtubule/Tubulin Cancer
    KIF18A-IN-3 is a potent KIF18A inhibitor (IC50=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer .
    KIF18A-IN-3
  • HY-176843

    Eukaryotic Initiation Factor (eIF) ADC Payload Cancer
    eIF4A-IN-2 (Compound 93) is an Eukaryotic translation initiation factor 4A (eIF4A) inhibitor. eIF4A-IN-2 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs) .
    eIF4A-IN-2
  • HY-146201

    Phosphodiesterase (PDE) 5-HT Receptor Neurological Disease
    PDE4B/7A-IN-1 is a dual PDE4B/PDE7A inhibitor. PDE4B/7A-IN-1 shows IC50 values of 69.0 μM for PDE4B and 57.0 μM for PDE7A, as well as Ki values of 539 nM for 5-HT1A and 328 nM for 5-HT7. PDE4B/7A-IN-1 shows favorable membrane permeability. PDE4B/7A-IN-1 can be used for the study of cognitive impairment and depression .
    PDE4B/7A-IN-1
  • HY-139830

    DYRK Neurological Disease
    Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers.
    Dyrk1A-IN-1
  • HY-178511

    Kinesin Cancer
    KIF18A-IN-17 (Example 37A) is a KIF18A inhibitor with racemic form with an IC50 of 48 nM. KIF18A-IN-17 exhibits anti-proliferative activity against HT29 cells. KIF18A-IN-17 can be used for the study of cancers such as breast cancer and ovarian cancer .
    KIF18A-IN-17
  • HY-178378

    Histone Methyltransferase GLP Receptor Reactive Oxygen Species (ROS) Autophagy Apoptosis Cancer
    G9a-IN-4 is a G9a inhibitor with high selectivity (IC50 = 32 nM). G9a-IN-4 shows high selectivity against the other tested lysine/arginine methyltransferases. G9a-IN-4 exhibits high enzymatic activity against G9a and more potent antiproliferative effects against all tested cancer cells. G9a-IN-4 significantly suppresses the H3K9me2 level. G9a-IN-4 triggers autophagy by inducing the production of ROS, thus leading to cell apoptosis and cell cycle arrest at G0/G1 in CT26 colon cells. G9a-IN-4 can be used for the study of colon cancer .
    G9a-IN-4
  • HY-175834

    Topoisomerase Reactive Oxygen Species (ROS) Apoptosis Microtubule/Tubulin Cancer
    DNA/TOP2A-IN-1 is an inhibitor of DNA and TOP2A. DNA/TOP2A-IN-1 selectively binds to TOP2A, not TOP2B, and interacts with DNA and TOP2A to form a stable DM1-TOP2A-DNA ternary complex. DNA/TOP2A-IN-1 induces DNA damage, increases reactive oxygen species (ROS) and triggers apoptosis in triple-negative breast cancer (TNBC) cells. DNA/TOP2A-IN-1 disrupts microtubule distribution and induces cell cycle arrest. DNA/TOP2A-IN-1 shows strong antiproliferative activity and inhibits cell migration. DNA/TOP2A-IN-1 inhibits tumor growth and can be used for TNBC research .
    DNA/TOP2A-IN-1
  • HY-162010

    Methionine Adenosyltransferase (MAT) Cancer
    MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile. MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors research .
    MAT2A-IN-13
  • HY-178343

    Aurora Kinase Apoptosis Cancer
    Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
    Aurora A-IN-5
  • HY-158386

    IRE1 Cancer
    IRE1a-IN-1 (Compound 10) is an IRE1α inhibitor, with an IC50 of less than 100 nM for XBP1 mRNA. IRE1a-IN-1 can be used for the research of cancer .
    IRE1a-IN-1
  • HY-158159

    Interleukin Related Inflammation/Immunology Cancer
    IL17A-IN-1 (compound 72) is an orally active Interleukin 17A inhibitor. IL17A-IN-1 can be used in the study of inflammatory and autoimmune diseases (plaque psoriasis, psoriatic arthritis, and ankylosing spondylitis, etc.), as well as cancer .
    IL17A-IN-1
  • HY-168265

    DYRK Neurological Disease Cancer
    Dyrk1A-IN-11 (compound 166) is a potent dual-specificity tyrosine phosphorylation- regulated 1A (DYRK1A) inhibitor with an EC50 value of 0.0021 µM. Dyrk1A-IN-11 inhibits the Phospho-Tau (Thr212) with an EC50 value of 0.0361 µM .
    Dyrk1A-IN-11
  • HY-142660

    Phosphodiesterase (PDE) Neurological Disease
    PDE2A-IN-1 is a phosphodiesterase 2A (PDE2A) inhibitor with an IC50 value of 1.3 nM.
    PDE2A-IN-1
  • HY-170500

    Methionine Adenosyltransferase (MAT) Cancer
    MAT2A-IN-17 is a potent MAT2A inhibitor with an IC50 < 100 nM. MAT2A-IN-17 can be used in the study of cancer .
    MAT2A-IN-17
  • HY-170503

    Methionine Adenosyltransferase (MAT) Cancer
    MAT2A-IN-20 (Compound A49) is an inhibitor for methionine adenosyltransferase 2A (MAT2A) with an IC50 ≤50 nM. MAT2A-IN-20 inhibits human UGT1A1 with an IC50 of 28.45 μM. MAT2A-IN-20 exhibits antitumor in mouse models .
    MAT2A-IN-20
  • HY-158237

    Phosphodiesterase (PDE) Neurological Disease
    PDE10A-IN-3 (Compound 8a) is an inhibitor of phosphodiesterase 10A (PDE10A). PDE10A-IN-3 can be used in schizophrenia research .
    PDE10A-IN-3
  • HY-170905S

    Methionine Adenosyltransferase (MAT) Isotope-Labeled Compounds Cancer
    MAT2A-IN-22 (Compound 29-1) is a BBB-penetrable and orally active MAT2A inhibitor with an IC50 of 4 nM. MAT2A-IN-22 shows selectivity and inhibitory activity against MTAP-deficient cancer cell lines. MAT2A-IN-22 has anti-tumor effects .
    MAT2A-IN-22
  • HY-158757

    Kinesin Microtubule/Tubulin Cancer
    KIF18A-IN-12 (compound 9) is a KIF18A inhibitor, with an IC50 value of 45.54 nM. KIF18A-IN-12 can be used in cancer research .
    KIF18A-IN-12
  • HY-149915

    Methionine Adenosyltransferase (MAT) Cancer
    MAT2A-IN-10 (Compound 28) is an orally active MAT2A inhibitor with an IC50 of 26 nM. MAT2A-IN-10 can be used for the research of cancer .
    MAT2A-IN-10
  • HY-170940

    DYRK Enterovirus Infection
    Dyrk1A-IN-12 (compound S43) is a Dyrk (Dual specificity tyrosine phosphorylation regulated kinase 1A inhibitor. Dyrk1A-IN-12 inhibits Dyrk1A with a IC50 of 95 nM. Dyrk1A-IN-12 shows anti-EV-A71 activity with an EC50 of 4.4 μM, CC50 of 12.8 μM and SI of 2.9. Dyrk1A-IN-12 shows potent inhibition against herpes simplex virus (HSV) .
    Dyrk1A-IN-12
  • HY-158212

    DYRK Neurological Disease
    Dyrk1A-IN-8 (compound 4C) is a potent inhibitor of Dyrk1A , with the IC50 of 209 nM. Dyrk1A-IN-8 plays an important role in neurodegenerative diseases .
    Dyrk1A-IN-8
  • HY-131973

    Phosphodiesterase (PDE) Cardiovascular Disease Metabolic Disease
    PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research .
    PDE10A-IN-2 hydrochloride
  • HY-179113

    Interleukin Related Inflammation/Immunology
    IL-17A-IN-5 (Compound 9) is an orally active IL-17A inhibitor. IL-17A-IN-5 demonstrates a clear dose-dependent inhibition of arthritis .
    IL-17A-IN-5
  • HY-170832

    Epigenetic Reader Domain Potassium Channel Cancer
    Menin–KMT2A-IN-1 (Compound 20) is the inhibitor for menin–KMT2A that binds to menin with an IC50 of 8 nM, and inhibits the interaction between menin and lysine methyltransferase 2A (KMT2A). Menin–KMT2A-IN-1 inhibits hERG with an IC50 of 65 μM. Menin–KMT2A-IN-1 inhibits cell MV4-11 with an IC50 of 74 nM. Menin–KMT2A-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mouse with an orally bioavailability of 74% .
    Menin–KMT2A-IN-1
  • HY-145827

    Kinesin Microtubule/Tubulin Cancer
    KIF18A-IN-4 is a moderately potent ATP and microtubule (MT) noncompetitive KIF18A inhibitor (IC50=6.16 μM). KIF18A-IN-4 has selectivity against a large panel of mitotic kinesins and kinases, and does not show any direct effects on tubulin assembly. KIF18A-IN-4 exhibits anti-tumor activity .
    KIF18A-IN-4
  • HY-161787

    Histone Methyltransferase Others
    G9a-IN-2 (Compound 7i) is an inhibitor for histone methyltransferases G9a with IC50 of 0.024 μM. G9a-IN-2 reduces H3K9me2 levels and induces the mRNA expression of γ-globin mRNA. G9a-IN-2 shows the potential in ameliorating sickle cell disease (SCD) .
    G9a-IN-2

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