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ATP-binding domains

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50867
    Lestaurtinib
    4 Publications Verification

    CEP-701; KT-5555

    JAK FLT3 Trk Receptor Apoptosis STAT Cancer
    Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .
    Lestaurtinib
  • HY-103666
    CY-09
    Maximum Cited Publications
    50 Publications Verification

    NOD-like Receptor (NLR) Inflammation/Immunology
    CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation .
    CY-09
  • HY-17537
    APY29
    10+ Cited Publications

    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 .
    APY29
  • HY-80002
    BMX-IN-1
    5+ Cited Publications

    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.
    BMX-IN-1
  • HY-122616

    Trk Receptor Neurological Disease
    PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .
    PF-06273340
  • HY-120097

    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 .
    R-10015
  • HY-114977

    DNA/RNA Synthesis Apoptosis Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    Avenanthramide A is an orally active phytoalexin that targets the RNA helicase DDX3 with a KD of 8.8 μM. Avenanthramide A induces mitochondrial swelling and increased ROS production, and triggers apoptosis in CRC cells. Avenanthramide A inhibits smooth muscle cell proliferation and enhances nitric oxide production. Avenanthramide A can be used in research on colorectal cancer and atherosclerosis .
    Avenanthramide A
  • HY-145425

    IRE1 Apoptosis FGFR Inflammation/Immunology
    PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of Xbp1 mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1α-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1α signaling pathway in diseases such as pulmonary fibrosis .
    PAIR2
  • HY-177936

    NEDD8-activating Enzyme Cancer
    NAE-IN-3 (compound 1) is a potent, selective and non-covalent competitive NEDD8-activating enzyme (NAE) inhibitor (IC50 = 0.8 μM). NAE-IN-3 inhibits NAE by blocking the ATP-binding domain. NAE-IN-3 exhibits selectivity over analogous E1 enzymes UAE and SAE. NAE-IN-3 can be used for cancer research .
    NAE-IN-3
  • HY-P11053

    HSP Cancer
    A17 peptide is a Hsp70-targeting peptide. A17 peptide binds to the ATP-binding domains of Hsp70. A17 peptide specifically inhibits the chaperone activity, thereby increasing the cells' sensitivity to apoptosis induced by chemotherapeutic agents, such as Cisplatin (HY-17394). A17 peptide can be used for anticancer chemotherapy research, such multiple myeloma .
    A17 peptide
  • HY-122735

    Ser/Thr Kinase Bacterial Infection
    Inh2-B1 is a Ser/Thr protein kinase (STK1) inhibitor. Inh2-B1 specifically inhibits STK1 activity by directly binding to its ATP-binding catalytic domain. Inh2-B1 down-regulates cell wall hydrolase genes and disrupts the biofilm formation of Methicillin-resistant Staphylococcus aureus (MRSA) clearly .
    Inh2-B1
  • HY-W286614

    Ribosomal S6 Kinase (RSK) Inflammation/Immunology Cancer
    RSK2-IN-4 (Compound 10) is a RSK2 inhibitor, with an inhibition rate of 13.73% on RSK2 activity at 10 μM. RSK2-IN-4 binds to the ATP-binding site of RSK2 in the NTKD (N-terminal kinase domain), with the electron-donating group at the 4-position of the phenyl ring being the key determinant for its inhibitory activity .
    RSK2-IN-4
  • HY-155975

    PI3K Inflammation/Immunology
    PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC50: 0.8 nM, Kd: 84.8 nM). PI3Kδ-IN-14 binds to the ATP-binding site of the kinase domain of PI3Kδ. PI3Kδ-IN-14 has anti-inflammatory activity by inhibiting the PI3K/AKT pathway. PI3Kδ-IN-14 ameliorates acute lung injury (ALI) .
    PI3Kδ-IN-14
  • HY-182936

    Bacterial DNA/RNA Synthesis Infection
    Antibacterial agent 338 (Compound 65) is an antibacterial agent and GyrB inhibitor, with an IC50 of 12.60 nM against GyrB from E. coli. Antibacterial agent 338 binds to the ATP-binding domain of E. coli GyrB, thereby inhibiting the ATPase activity of GyrB. Antibacterial agent 338 exhibits broad-spectrum antibacterial activity against multidrug-resistant Gram-negative bacteria. Antibacterial agent 338 reduces bacterial load in a neutropenic mouse thigh infection model. Antibacterial agent 338 can be used for the research of Acinetobacter baumannii infection .
    Antibacterial agent 338
  • HY-123925

    RIP kinase IAP NOD-like Receptor (NLR) Inflammation/Immunology
    CSLP43 is a selective RIPK2 and XIAP inhibitor with an IC50 of 19.9 nM against human RIPK2. CSLP43 binds to the ATP-binding pocket of RIPK2 and disrupts the interaction between RIPK2 and the BIR2 domain of XIAP or cIAP1. CSLP43 inhibits RIPK2 ubiquitination, NOD1-dependent inflammatory signaling pathways, NOD2-dependent inflammatory signaling pathways, as well as NF-κB activation associated with NOD agonists. CSLP43 is selective for the NOD1/NOD2 signaling pathway and does not inhibit the kinase activity of RIPK1 or RIPK3. CSLP43 is applicable to research related to Crohn's disease, Blau syndrome, early-onset sarcoidosis and early-onset inflammatory bowel disease .
    CSLP43
  • HY-103666R

    Reference Standards NOD-like Receptor (NLR) Inflammation/Immunology
    CY-09 (Standard) is the analytical standard of CY-09 (HY-103666). This product is intended for research and analytical applications. 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 .
    CY-09 (Standard)
  • HY-112783

    JAK Inflammation/Immunology
    TYK2 ligand 4 (Compound 2) is a TYK2 ligand. TYK2 ligand 4 binds to both the kinase domain and pseudokinase domain, and induces an inactive conformation of the kinase domain, thereby preventing ATP binding. TYK2 ligand 4 serves as a tool compound for the development of Deucravacitinib (HY-117287) .
    TYK2 ligand 4
  • HY-183373

    EGFR PARP Cancer
    EGFR/PARP-1-IN-1 is a dual EGFR and PARP-1 inhibitor with IC50 values of 64 nM and 12 nM, respectively. EGFR/PARP-1-IN-1 binds to the ATP-binding pocket of EGFR and interacts with the catalytic domain of PARP-1, inhibiting kinase and enzymatic activity via hydrogen bond formation with key residues in both targets. EGFR/PARP-1-IN-1 induces apoptosis through the endogenous mitochondrial pathway, arrests the cell cycle at the G2 phase, and inhibits cell proliferation. EGFR/PARP-1-IN-1 can be used for research on triple-negative breast cancer .
    EGFR/PARP-1-IN-1
  • HY-10654

    Ephrin Receptor Cancer
    EphB4-IN-2 (compound 66) is a tyrosine kinase inhibitor with an IC50 value of 1.6 nM against human EphB4, and exhibits selectivity toward kinases bearing threonine gatekeeper residues. EphB4-IN-2 also has high ligand efficiency .
    EphB4-IN-2
  • HY-182073

    EGFR Apoptosis Cancer
    EGFR-IN-207 (Compound 5h) is an epidermal growth factor receptor (EGFR) kinase inhibitor with an IC50 of 0.21 μM. EGFR-IN-207 induces cell cycle arrest at the Sub-G1 phase and promotes Apoptosis. EGFR-IN-207 exhibits anticancer activity against lung cancer. EGFR-IN-207 shows extremely low toxicity in non-cancerous cell lines. EGFR-IN-207 can be used in lung cancer-related research .
    EGFR-IN-207
  • HY-182306

    VEGFR Cardiovascular Disease
    VEGFR-2 ligand-1, Sorafenib (HY-10201) derivative, is a vascular endothelial growth factor receptor 2 (VEGFR2) ligand. VEGFR-2 ligand-1 binds to the ATP-binding pocket of VEGFR2, forms hydrophobic contacts and hydrogen bonds with key binding-site residues. VEGFR-2 ligand-1 can be used for the research angiogenesis-related pathologies .
    VEGFR-2 ligand-2

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