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123

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13459

    Smo Cancer
    PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
    PF-5274857
  • HY-130243

    ROR Inflammation/Immunology
    RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo .
    RORγt Inverse agonist 6
  • HY-121802
    Dynarrestin
    2 Publications Verification

    Hedgehog Cancer
    Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-dependent processes in cells without affecting ATP hydrolysis and interfering with ciliogenesis. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells .
    Dynarrestin
  • HY-154313

    Clospirazine

    Ras Cancer
    Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .
    Spiclomazine
  • HY-D1459

    Fluorescent Dye Metabolic Disease
    BODIPY 665/676 is a lipophilic radical-sensitive fluorescent probe that can be used to study radical-driven lipid autoxidation .
    BODIPY 665/676
  • HY-13459A

    Smo Cancer
    PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
    PF-5274857 hydrochloride
  • HY-149880

    c-Met/HGFR Cancer
    c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    c-Met-IN-18
  • HY-163620

    FGFR Apoptosis Cancer
    LHQ490 is a selective FGFR2 inhibitor, with an IC50 of 5.2 nM. LHQ490 efficiently inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 1.4 nM. LHQ490 inhibits FGFR2-driven cancer cell proliferation and induces apoptosis of FGFR2-driven cancer cells .
    LHQ490
  • HY-145843

    c-Myc Cancer
    c-Myc inhibitor 5 (DA3) is a fluorescent, long chain-bridged bispurine that selectively targets the c-MYC G-quadruplex (KD of 16 μM). c-Myc inhibitor 5 shows inhibition on c-MYC expression rather than other G4-driven oncogenes .
    c-Myc inhibitor 5
  • HY-112378

    FLT3 Cancer
    D-65476 is an inhibitor of type Ⅲ receptor tyrosine kinase (Flt3). In the absence of IL-3, D-65476 inhibits the proliferation of TEL-Flt3 transfected BA/F3 cells (IC50= 0.2 μM), which can be used in the study of Flt3-driven leukemia .
    D-65476
  • HY-116785

    DNA/RNA Synthesis Cancer
    BRD32048 is a direct binder of ETV1 with a KD of 17.1 μM. BRD32048 modulates both ETV1-mediated transcriptional activity and invasion of ETV1-driven cancer cells. BRD32048 inhibits ETV1 acetylation and promotes its degradation. BRD32048 acts as a top candidate ETV1 perturbagen .
    BRD32048
  • HY-124826

    NSC 109268

    β-catenin Cancer
    BC21 (NSC 109268) is a β-catenin/Tcf4 inhibitor with an IC50 of 5 μM. BC21 effectively inhibits the binding of β-catenin to Tcf4-derived peptides and suppresses β-catenin/Tcf4-driven reporter gene activity. BC21 can be utilized in cancer research .
    BC21
  • HY-100849

    JAK Inflammation/Immunology
    JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM). JAK3i forms a covalent bond with a cysteine in JAK3, but not the closely related kinase domains in JAK1, JAK2, or TYK2. JAK3i abolishes IL-2-driven T-cell proliferation in vivo and has the potential for  autoimmune disease research .
    JAK 3i
  • HY-12284

    Prostaglandin Receptor Inflammation/Immunology
    NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats .
    NVP-QAV680
  • HY-112929
    DT-061
    10+ Cited Publications

    Phosphatase Cancer
    DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis .
    DT-061
  • HY-141896

    RET Cancer
    RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
    RET-IN-7
  • HY-124267

    SOMG-833

    c-Met/HGFR Cancer
    Zgwatinib (SOMG-833) is a potent, selective, and ATP-competitive c-MET inhibitor, with an IC50 of 0.93 nM against c-MET, over 10,000-fold more potent compared with 19 tyrosine kinases (including c-MET family members and highly homologous kinases). Zgwatinib potently inhibits c-MET-driven cell proliferation. Zgwatinib as a potential candidate agent for c-MET-driven human cancers research .
    Zgwatinib
  • HY-115866

    COX Cancer
    COX-2-IN-6 (compound 10) is an orally active, gut-restricted and selective cyclooxygenase-2 (COX-2) inhibitor for colorectal Chemoprevention of cancer. COX-2-IN-6 selectively targets COX-2 with an IC50 of 0.84 μM and a Ki of 69 nM. COX-2-IN-6 also inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM .
    COX-2-IN-6
  • HY-134978A
    (+)SHIN2
    2 Publications Verification

    SHMT Cancer
    (+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, whose target can be traced with 13C-serine. (+)SHIN2 increases survival in NOTCH1-driven mouse primary acute lymphoblastic leukemia (T-ALL) in vivo with a synergistic effect with Methotrexate (HY-14519) . (+)SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (+)SHIN2
  • HY-108417

    STAT JAK Bcr-Abl Cancer
    Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors .
    Debio 0617B
  • HY-125102

    IGF-1R Cancer
    AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
    AZ12253801
  • HY-151335

    HSP Cancer
    KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research .
    KU-177
  • HY-N9362

    Antibiotic Infection
    Emodinanthrone, an anthraquinone, is a sprecursor of Emodin (HY-14393) with antibiotic activity. Emodinanthrone inhibits respiration-driven solute transport at micromolar concentrations in membrane vesicles of Escherichia coli .
    Emodinanthrone
  • HY-122878

    HSP Cancer
    HS-131, a near infrared dye tethered Hsp90 inhibitor, is able to detect oncogene-driven breast cancers, including multiple different molecular subtypes of human breast cancers .
    HS-131
  • HY-131953

    Androgen Receptor Cancer
    Androgen receptor-IN-3 (Compound 22) is an androgen receptor inhibitor. Androgen receptor-IN-3 inhibits AR-driven transcriptional activity in LNCaP cells, with an IC50 of 5.04 μM .
    Androgen receptor-IN-3
  • HY-P3277

    Ras Cancer
    KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .
    KRpep-2d
  • HY-P3277A

    Ras Cancer
    KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .
    KRpep-2d TFA
  • HY-151881

    Ras Cancer
    SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer .
    SOS1-IN-15
  • HY-107730

    Neuropeptide Y Receptor Neurological Disease
    NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor .
    NPY5RA-972
  • HY-161682

    GPR84 Neurological Disease
    GPR84 antagonist 9 (compound 320) is an orally active GPR84 antagonist with the IC50 of 0.012 μM. GPR84 antagonist 9 can be used for study of inflammatory-driven pain diseases .
    GPR84 antagonist 9
  • HY-169153

    MAP3K Inflammation/Immunology
    Cot inhibitor-3 (Compound 33) is a potent and selective cancer osaka thyroid (COT) kinase inhibitor, with an IC50 of 4 nM. Cot inhibitor-3 can be used to prevent inflammation-driven lameness .
    Cot inhibitor-3
  • HY-19350
    BML-210
    2 Publications Verification

    HDAC Apoptosis Cancer
    BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice .
    BML-210
  • HY-157083

    YAP Cancer
    mCMY020 is a covalent inhibitor of TEAD. mCMY020 effectively reduces YAP (Yes-associated protein)-driven transcription and selectively slows the proliferation of Hippo-deficient cancer cells. mCMY020 can be used in cancer research .
    mCMY020
  • HY-131968

    JAK Cytochrome P450 Inflammation/Immunology
    BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium .
    BMS-986202
  • HY-19706
    ARS-853
    4 Publications Verification

    Ras Apoptosis Cancer
    ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .
    ARS-853
  • HY-124674A
    CCT365623 hydrochloride
    1 Publications Verification

    Monoamine Oxidase EGFR Akt TGF-beta/Smad Cancer
    CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties .
    CCT365623 hydrochloride
  • HY-136270
    Gartisertib
    2 Publications Verification

    VX-803; M4344; ATR inhibitor 2

    ATM/ATR Cancer
    Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
    Gartisertib
  • HY-P2471

    Calmodulin Neurological Disease
    Neurogranin (48-76), mouse is a peptide corresponding to residues 48-76 of Neurogranin. Neurogranin, a calmodulin-binding protein, is exclusively expressed in the post-synapse, and mediates NMDAR driven synaptic plasticity by regulating the calcium-calmodulin (Ca 2+-CaM) pathway .
    Neurogranin (48-76), mouse
  • HY-136579
    ASN007
    4 Publications Verification

    ERK-IN-3

    ERK Cancer
    ASN007 (ERK-IN-3) is a potent and orally active inhibitor of ERK. ASN007 inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 can be used for the research of cancers driven by RAS mutations .
    ASN007
  • HY-136579A

    ERK-IN-3 benzenesulfonate

    ERK Cancer
    ASN007 (ERK-IN-3) benzenesulfonate is a potent and orally active inhibitor of ERK. ASN007 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 benzenesulfonate can be used for the research of cancers driven by RAS mutations .
    ASN007 benzenesulfonate
  • HY-139361
    Sulfopin
    2 Publications Verification

    PIN1-3

    PIN1 Cancer
    Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors .
    Sulfopin
  • HY-13323
    CX-5461
    Maximum Cited Publications
    42 Publications Verification

    DNA/RNA Synthesis Cancer
    CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
    CX-5461
  • HY-P99217

    AMG 102

    c-Met/HGFR Cancer
    Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
    Rilotumumab
  • HY-W423595

    EGFR Cancer
    BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .
    BEBT-109
  • HY-14460

    FLAP Inflammation/Immunology
    AM679 is a potent, selective 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 2 nM in a human FLAP membrane binding assay. AM679 markedly reduces the respiratory syncytial virus-driven ocular pathology as well as the synthesis of cysteinyl leukotrienes (CysLTs) in the eye .
    AM679
  • HY-P99450

    IPH 5401; Anti-C5aR1 mAb

    Complement System Inflammation/Immunology Cancer
    Avdoralimab (IPH 5401) is a fully human IgGκ monoclonal antibody that targets the complement C5a receptor 1 (C5aR1) that prevents its binding to C5a. Avdoralimab can be used for complement-driven inflammatory diseases and solid tumours research .
    Avdoralimab
  • HY-163299

    Ras Apoptosis Cancer
    pan-KRAS-IN-5 (compound 15a) is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 induces cell cycle arrest and promptes apoptosis in KRAS-driven cancer cells .
    pan-KRAS-IN-5
  • HY-U00461

    Ketohexokinase inhibitor 1

    Ketohexokinase Metabolic Disease
    PF-06835919 (Ketohexokinase inhibitor 1) is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66 nM for KHK-C and KHK-A, respectively. PF-06835919 can be used for the study of metabolic disorders driven by the overconsumption of Fructose (HY-N0395) .
    PF-06835919
  • HY-106228

    Fungal Bacterial Glutathione Peroxidase Infection
    HLF1-11, a human lactoferrin-derived peptide, is a broad spectrum antimicrobial agent. HLF1-11 inhibits human MPO activity. HLF1-11 also directs GM-CSF-driven monocyte differentiation toward macrophages, and enhances immune responses .
    HLF1-11
  • HY-164513

    Ras Phosphodiesterase (PDE) Cancer
    NHTD is a KRAS-PDEδ inhibitor. NHTD targets the prenyl-binding pocket of PDEδ, altering the cellular localization of KRAS, thereby inhibiting the proliferation of KRAS-mutant cancer cells and inducing apoptosis. NHTD can be used for research on KRAS-driven non-small cell lung cancer (NSCLC) .
    NHTD

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