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ATP binding site

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15463
    Imatinib
    Maximum Cited Publications
    120 Publications Verification

    STI571; CGP-57148B

    		 Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
    Imatinib
  • HY-101562
    Inavolisib
    5+ Cited Publications

    GDC-0077; RG6114

    		 PI3K Apoptosis Cancer
    Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
    Inavolisib
  • HY-128933
    AMP-PNP tetralithium
    3 Publications Verification

    Adenylyl-imidodiphosphate tetralithium

    		 Potassium Channel Metabolic Disease
    AMP-PNP (Adenylyl-imidodiphosphate) tetralithium is a non-hydrolyzable ATP analog. AMP-PNP tetralithium binds to ATP binding sites competely but is not hydrolyzed by enzymes, providing stable experimental conditions for studying ATP-dependent processes. AMP-PNP tetralithium can also be used to study enzyme activity, kinase regulation, DNA/RNA metabolism, ion channel function, and protein complex assembly .
    AMP-PNP tetralithium
  • HY-119976
    Boscalid
    1 Publications Verification

    		 Environmental Pollutants Apoptosis Fungal Mitochondrial Metabolism Succinate Dehydrogenase Infection
    Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis .
    Boscalid
  • HY-130777A
    AMP-PNP lithium hydrate
    3 Publications Verification

    Adenylyl imidodiphosphate lithium hydrate

    		 Drug Derivative Metabolic Disease
    AMP-PNP (Adenylyl imidodiphosphate) lithium hydrate is a non-hydrolyzable ATP analog. AMP-PNP lithium hydrate binds to ATP binding sites competely but is not hydrolyzed by enzymes, providing stable experimental conditions for studying ATP-dependent processes. AMP-PNP lithium hydrate can also be used to study enzyme activity, kinase regulation, DNA/RNA metabolism, ion channel function, and protein complex assembly .
    AMP-PNP lithium hydrate
  • HY-112299
    Zipalertinib
    3 Publications Verification

    TAS6417; CLN-081

    		 EGFR Apoptosis Cancer
    Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM .
    Zipalertinib
  • HY-N2524
    Camelliaside A

    		EGFR Cancer
    Camelliaside A is a phytochemical and also a HER2 ligand. Camelliaside A shows no inhibitory effect on mycelial growth of Rhizoctonia solani, indicating no antifungal activity against this pathogen. Camelliaside A is applicable to breast cancer-related research .
    Camelliaside A
  • HY-101513
    eIF4A3-IN-1
    4 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Neurological Disease Cancer
    eIF4A3-IN-1 is a selective eIF4A3 inhibitor (IC50: 0.26 μM; Kd: 0.043 μM) with cellular nonsense-mediated RNA decay (NMD) inhibitory activity. eIF4A3-IN-1 can specifically bind to the non-ATP binding site of eIF4A3. eIF4A3-IN-1 has anti-tumor and analgesic activities .
    eIF4A3-IN-1
  • HY-Y0095
    Isethionic acid (80% in water)

    2-Hydroxyethanesulfonic acid

    		 Environmental Pollutants Mitochondrial Metabolism Parasite Metabolic Disease
    Isethionic acid is a calcium binder and anionic detergent that enhances mitochondrial calcium binding capacity by competitively binding to calcium binding sites on the outer mitochondrial membrane. Isethionic acid can inhibit calcium-activated mitochondrial respiration. Isethionic acid inhibits barnacle (Balanus amphitrite) larvae with LC50s of 23 μg/mL (24 h) and 17 μg/mL (48 h), respectively. Isethionic acid can inhibit the attachment of barnacle larvae (complete inhibition at 10 μg/mL) and regulate mitochondrial calcium transport, and can enhance ATP-dependent calcium uptake at high calcium concentrations. Isethionic acid can be used to study the mechanism of mitochondrial calcium metabolism.
    Isethionic acid (80% in water)
  • HY-100848
    TX1-85-1
    2 Publications Verification

    		 EGFR Cancer
    TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling .
    TX1-85-1
  • HY-175606
    EVT0185

    		ATP Citrate Lyase Cancer
    EVT0185 is an orally active ATP citrate lyase (ACLY) inhibitor. EVT0185 is converted to a CoA thioester in the liver by SLC27A2 and interacts with the CoA-binding site of ACLY. EVT0185-CoA inhibits ACLY activity with an IC50 of 2.5 μM. EVT0185 can phenocopy the immune and antitumour effects of genetic ACLY deletion. EVT0185 can increase tumour-infiltrating B cells and chemokine CXCL13 levels. EVT0185 can be used for the research of cancer, such as hepatocellular carcinoma (HCC) .
    EVT0185
  • HY-159520
    Ofirnoflastum

    Ofirnoflast; HT-6184

    		 NEKs NOD-like Receptor (NLR) Caspase Apoptosis Pyroptosis NF-κB Cardiovascular Disease Inflammation/Immunology Cancer
    Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia .
    Ofirnoflastum
  • HY-10261B
    (E/Z)-Afatinib

    (E/Z)-BIBW 2992

    		 EGFR Apoptosis c-Met/HGFR Akt p38 MAPK Autophagy Others Cancer
    (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells .
    (E/Z)-Afatinib
  • HY-106005
    MMV390048
    3 Publications Verification

    		 Parasite PI4K Infection
    MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent .
    MMV390048
  • HY-173432
    LIBX-A401

    		ACSL Family Ferroptosis Neurological Disease Cancer
    LIBX-A401 is a selective long-chain acyl-CoA synthetase 4 (ACSL4) inhibitor with a human IC50 values of 0.38 μM and a Kd of 0.72 μM. LIBX-A401 binds to ACSL4 in an ATP-dependent manner, stabilizes the C-terminal domain, alters the fatty acid gate region, and interacts with residues A329 and Q302 within the fatty acid binding site. LIBX-A401 exhibits anti-ferroptosis properties in cells. LIBX-A401 can be used for the researches of cancer and parkinson's disease .
    LIBX-A401
  • HY-17547
    NMS-E973
    2 Publications Verification

    		 HSP Cancer
    NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy .
    NMS-E973
  • HY-12062
    PD318088
    1 Publications Verification

    		 MEK Cancer
    PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research .
    PD318088
  • HY-D1078
    5(6)-Carboxy-2',7'-dichlorofluorescein diacetate

    		Fluorescent Dye Reactive Oxygen Species (ROS) P-glycoprotein Others
    5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is a fluorescein-based reactive oxygen species (ROS) probe and also a MRP2 substrate. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate serves as a substrate for intracellular esterases, which cleave its acetate groups to generate a fluorescent product capable of detecting intracellular ROS. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is ATP-dependent and is transported via a single MRP2 binding site; it competes with LTC4 for MRP2 binding sites and inhibits MRP2-mediated LTC4 transport (Ex/Em = 496/525 nm) .
    5(6)-Carboxy-2',7'-dichlorofluorescein diacetate
  • HY-107779
    BI-882370

    		Raf Cancer
    BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases .
    BI-882370
  • HY-P10856
    CPI1

    		P-glycoprotein Cancer
    CPI1 is a multidrug resistance protein 1 (MRP1) inhibitor with a Ki value of 100 nM. CPI1 binds to the same substrate-binding site as leukotriene C4, stabilizes MRP1 in an apo-like inward-facing conformation, blocks the conformational changes required for ATP hydrolysis and substrate transport, and inhibits the ATPase activity of human and bovine MRP1. CPI1 serves as a tool for investigating the substrate transport mechanism of MRP1. CPI1 is applicable to research related to cancer multidrug resistance .
    CPI1
  • HY-110079
    TNP

    		IPK Superfamily Cancer
    TNP is a competitive, reversible inhibitor of IP6K1 and IP3K, with IC50s of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP competitively binds to the ATP binding site of IP6K, inhibits the generation of 5-IP7, and thus relieves the inhibition of 5-IP7 on the AKT signaling pathway. TNP can enhance insulin sensitivity and promote thermogenesis in adipose tissue. TNP cannot effectively pass through the blood-brain barrier and is mainly used in the study of obesity, type 2 diabetes, and metabolic syndrome. However, TNP also inhibits CYP3A4 and may need further optimization[1][2][3].
    TNP
  • HY-157508
    VCP Activator 1
    2 Publications Verification

    		 p97 Others
    VCP Activator 1 is a VCP activator that dose-dependently stimulates VCP ATPase activity. VCP Activator 1 binds an allosteric pocket near the C-terminus. In addition, VCP Activator 1 binding site can also be occupied by a phenylalanine residue in the VCP C-terminal tail .
    VCP Activator 1
  • HY-111930
    5-Iodo-indirubin-3'-monoxime

    		GSK-3 CDK Cancer
    5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively .
    5-Iodo-indirubin-3'-monoxime
  • HY-12679
    PF-06658607

    		Btk Cancer
    PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry .
    PF-06658607
  • HY-156685
    EDI048

    		PI4K Parasite Infection Metabolic Disease Cancer
    EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children .
    EDI048
  • HY-164393
    ON044580

    		JAK Bcr-Abl Apoptosis Cancer
    ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
    ON044580
  • HY-160519
    Targocil-II

    		Bacterial Antibiotic Infection
    Targocil-II (Compound 2) is an ABC transporter inhibitor with a IC50 value of 137 nM. Targocil-II prevents ATP hydrolysis by binding to allosteric sites of the TM domain. Targocil-II has (antibacterial) activity .
    Targocil-II
  • HY-100214
    EAI001

    		EGFR Cancer
    EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFR L858R/T790M. EAI001 can be used for research of cancer .
    EAI001
  • HY-N9279
    Dehydromonocrotaline

    Monocrotaline pyrrole; MCTP; 3,8-Didehydromonocrotaline

    		 Endogenous Metabolite Cardiovascular Disease Cancer
    Dehydromonocrotaline is a mitochondrial respiratory chain complex I NADH oxidase inhibitor, with a IC50 of 62.06 μM and a Ki of 8.1 μM in rats. Dehydromonocrotaline exerts non-competitive inhibitory effects by modifying cysteine thiol groups on complex I, and does not bind to the NADH-binding site. Dehydromonocrotaline dissipates mitochondrial membrane potential and reduces ATP levels. Dehydromonocrotaline can be used in studies related to hepatotoxicity, pulmonary hypertension and liver tumors .
    Dehydromonocrotaline
  • HY-173162
    GPV0057

    		P-glycoprotein Potassium Channel Cardiovascular Disease Cancer
    GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .
    GPV0057
  • HY-145425
    PAIR2

    		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-155941
    5-Hydroxydecanoic acid

    		Potassium Channel Neurological Disease
    5-Hydroxydecanoic acid (5-HD） is a KATP channel antagonist，which has the effect of blocking the K KATP channel only during ischaemia by competing with the ATP binding site and does not affect pancreatic KATP channels .
    5-Hydroxydecanoic acid
  • HY-115749
    D-Luciferin 6′-methyl ether

    6′-Methoxyluciferin

    		 Fluorescent Dye Others
    D-Luciferin 6′-methyl ether (6′-Methoxyluciferin; compound 19a) is a potent luciferase from the North American firefly Photinus pyralis (PpyLuc) inhibitor with an IC50 of 0.1 µM. D-Luciferin 6′-methyl ether, a D-luciferin analog, shows non-specific interactions at ATP- and luciferin-binding sites of the PpyLuc active site .
    D-Luciferin 6′-methyl ether
  • HY-15463R
    Imatinib (Standard)

    STI571 (Standard); CGP-57148B (Standard)

    		 Reference Standards Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib (Standard) is the analytical standard of Imatinib. This product is intended for research and analytical applications. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
    Imatinib (Standard)
  • HY-161681
    Formycin triphosphate

    		Guanylate Cyclase Metabolic Disease
    Formycin triphosphate is a fluorescent analogue of ATP which on binding to enzyme active sites exhibits enhanced fluorescence. Formycin triphosphate is an ATP-competitive chicken liver pyruvate carboxylase inhibitor. Formycin triphosphate potentiates atrial natriuretic factor (ANF)-stimulated guanylate cyclase activity with an EC50 at about 90 μM and inhibits ATP-stimulated guanylate cyclase activity with an IC50 at about 100 μM .
    Formycin triphosphate
  • HY-178980
    APL-5125

    		Casein Kinase Cancer
    APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer .
    APL-5125
  • HY-18010
    PCI 29732
    3 Publications Verification

    		 Btk BCRP Inflammation/Immunology
    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .
    PCI 29732
  • HY-128778
    Gozanertinib

    DBPR112

    		 EGFR Cancer
    Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy .
    Gozanertinib
  • HY-164523
    PV1162

    		Checkpoint Kinase (Chk) Cancer
    PV1162 is a selective Chk2 inhibitor with an IC50 of 0.29 nM. PV1162 inhibits ATP binding to Chk2 by targeting the gatekeeper-dependent hydrophobic pocket, which is specific to Chk2 and located behind the ATP-binding site (adenine-binding region), thereby inhibiting the phosphorylation activity of Chk2. PV1162 holds potential application value in the field of cancer therapy .
    PV1162
  • HY-161800
    Aminoacyl tRNA synthetase-IN-3

    		Aminoacyl-tRNA Synthetase Infection
    Aminoacyl tRNA synthetase-IN-3 (compound 36K3) is an inhibitor of lysine tRNA synthetase (PfLysRS) from Plasmodium falciparum (IC50=59.2 nM), which inhibits the activity of PfLysRS by occupying the ATP binding site and L-lysine binding site of PfLysRS. Aminoacyl tRNA synthetase-IN-3 can be used in the development of antimalarial drugs .
    Aminoacyl tRNA synthetase-IN-3
  • HY-153761
    ASK1-IN-4

    		MAP3K ASK1 Apoptosis Inflammation/Immunology Cancer
    ASK1-IN-4 (Compound 17) is an ASK1 inhibitor (IC50=0.2 μM). ASK1-IN-4 interacts with ATP-binding site of ASK1 .
    ASK1-IN-4
  • HY-145422
    KIRA9

    		IRE1 Apoptosis Others
    KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis .
    KIRA9
  • HY-149292
    SR-4133

    		Casein Kinase Cancer
    SR-4133 is a potent and highly CK1ε selective inhibitor with an IC50 of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .
    SR-4133
  • HY-120600
    Sibiriline

    		Necroptosis Apoptosis RIP kinase Inflammation/Immunology
    Sibiriline is a specific competitive inhibitor of RIPK1 that targets the RIPK1 ATP-binding site and locks it in an inactive conformation. Sibiriline inhibits TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis, but does not protect cells from caspase-dependent apoptosis. Sibiriline protects mice from concanavalin A-induced hepatitis and has the potential to inhibit immune-dependent hepatitis. .
    Sibiriline
  • HY-15463S3
    Imatinib-13C,d3

    STI571-13C,d3; CGP-57148B-13C,d3

    		 Isotope-Labeled Compounds Autophagy SARS-CoV Bcr-Abl PDGFR c-Kit Cancer
    Imatinib- 13C,d3 (STI571- 13C,d3) is 13C labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
    Imatinib-13C,d3
  • HY-144381
    Glutamate-5-kinase-IN-1

    		Bacterial Infection
    Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 μM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents .
    Glutamate-5-kinase-IN-1
  • HY-158618
    Aurora kinase inhibitor-14

    		Aurora Kinase Apoptosis Cancer
    Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia .
    Aurora kinase inhibitor-14
  • HY-N11784
    Triptolidenol

    		Apoptosis Caspase NF-κB COX IKK Inflammation/Immunology Cancer
    Triptolidenol, a traditional Chinese medicine, is an epoxy diterpene lactone that can be isolated from Tripterygium wilfordii. Triptolidenol has anti-inflammatory and anticancer activities. Triptolidenol significantly inhibits tumor cell proliferation and migration, arrests cell cycle arrest at S phase and induces apoptosis by activating the cytochrome c/caspase cascade signaling pathway. Triptolidenol disrupts NF-κB/COX-2 pathway by inhibiting IKKβ at ATP-binding sites. Triptolidenol can be used for chronic nephritis and kidney cancer like clear cell renal cell carcinoma (ccRCC) research .
    Triptolidenol
  • HY-172544
    TTBK1/2-IN-3

    		Tau Protein Neurological Disease
    TTBK1/2-IN-3 (Compound 10) is a potent inhibitor of tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 579 nM and 258 nM, respectively. TTBK1/2-IN-3 inhibits the phosphorylation of TDP-43. TTBK1/2-IN-3 reduces the expression of primary cilia on the surface of iPSCs .
    TTBK1/2-IN-3
  • HY-150537
    AChE/GSK-3β-IN-1

    		Cholinesterase (ChE) GSK-3 Microtubule/Tubulin ROS Kinase Neurological Disease
    AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
    AChE/GSK-3β-IN-1

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