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anti-tumor efficacy

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305

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-150256
    YTP-17

    		YAP Cancer
    YTP-17 is an orally active YAP-TEAD protein-protein interaction inhibitor with an IC50 of 4 nM. YTP-17 shows anti-tumor efficacy .
    YTP-17
  • HY-109084A
    Conteltinib tetrahydrochloride

    CT-707 tetrahydrochloride

    		 FAK Cancer
    Conteltinib tetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride salt form of Conteltinib (HY-109084). Conteltinib tetrahydrochloride is the inhibitor for FAK (IC50=1.6 nM), ALK, and Pyk2. Conteltinib tetrahydrochloride exhibits a synergistic anti-tumor efficacy with Cabozantinib (HY-13016) .
    Conteltinib tetrahydrochloride
  • HY-111458
    GSK2643943A
    5 Publications Verification

    		 Deubiquitinase Cancer
    GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
    GSK2643943A
  • HY-15496
    E6201

    ER-806201

    		 MEK FLT3 Cancer
    E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
    E6201
  • HY-157302
    c-Met-IN-21

    		c-Met/HGFR Cancer
    c-Met-IN-21 (compound 54) is a c-met inhibitor with an IC50 value of 0.45? nM, and shows anti-tumor efficacy in vivo .
    c-Met-IN-21
  • HY-155146
    Anticancer agent 146

    		Necroptosis Cancer
    Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model .
    Anticancer agent 146
  • HY-164959
    ZINC00230567

    		Lipocalin Family Cancer
    ZINC00230567 is an inhibitor for Lipocalin-2 (LCN2). ZINC00230567 reduces the colony formation and cell viability of cell SUM149, and exhibits anti-tumor efficacy .
    ZINC00230567
  • HY-13646C
    Encequidar mesylate hydrochloride

    HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride

    		 P-glycoprotein Cancer
    Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models .
    Encequidar mesylate hydrochloride
  • HY-130116A
    IACS-8779 disodium

    		STING Cancer
    IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma .
    IACS-8779 disodium
  • HY-130628
    PAK4-IN-1

    		PAK Cancer
    PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions .
    PAK4-IN-1
  • HY-113003
    H-γ-Glu-Gln-OH

    γ-Glutamylglutamine; γ-Glu-Gln

    		 Amino Acid Derivatives Others Cancer
    H-γ-Glu-Gln-OH is a hydrophilic peptide and can be conjugated to drugs. The carrier composed of H-γ-Glu-Gln-OH has the characteristics of high water solubility and drug-loading capacity, good biocompatibility, low toxicity, improved tumor targeting ability, and anti-tumor efficacy .
    H-γ-Glu-Gln-OH
  • HY-157029S
    KRASG12D-IN-1

    		Ras Cancer
    KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
    KRASG12D-IN-1
  • HY-157031S
    KRASG12D-IN-2

    		Ras Cancer
    KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
    KRASG12D-IN-2
  • HY-115400
    1V209
    3 Publications Verification

    TLR7 agonist T7

    		 Toll-like Receptor (TLR) Cancer
    1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity .
    1V209
  • HY-13659
    KRN5500

    NSC 650426

    		 Antibiotic Bcl-2 Family Apoptosis Infection Cancer
    KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice .
    KRN5500
  • HY-155681
    SWS1

    		PD-1/PD-L1 Monoamine Oxidase Cancer
    SWS1 is a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM) with anticancer activity. SWS1 can increase the number of tumor-infiltrating lymphocytes and exhibit anti-tumor efficacy in the B16-F10 mouse model (TGI=66.1%) .
    SWS1
  • HY-118899
    XR5944

    		Endogenous Metabolite Cancer
    XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
    XR5944
  • HY-115581
    Thymidine 3',5'-disphosphate

    Deoxythymidine 3′,5′-diphosphate; pdTp

    		 Apoptosis Cancer
    Thymidine 3',5'-disphosphate (Deoxythymidine 3′,5′-diphosphate; pdTp) is a selective small molecule inhibitor of staphylococcal nuclease and tudor domain containing 1 (SND1, the miRNA regulatory complex RISC subunit) and inhibits SND1 activity. Thymidine 3',5'-disphosphate exhibits anti-tumor efficacy in vivo .
    Thymidine 3',5'-disphosphate
  • HY-169347
    dCK1α-2

    LC-05-004

    		 Molecular Glues Casein Kinase Cancer
    dCK1α-2 is an orally active CK1α molecular glue degrader that targets p53 pathway-related targets. dCK1α-2 exhibits anti-tumor efficacy in mouse models and can increase the expression of p53-related genes. .
    dCK1α-2
  • HY-170947
    Antitumor agent-195

    		STAT Quinone Reductase Cancer
    Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
    Antitumor agent-195
  • HY-165421
    Mps1-IN-10

    		Mps1 Cancer
    Mps1-IN-10 (Compound 9) is an inhibitor for Mps1 with an IC50 of 6.4 nM. Mps1-IN-10 inhibits the proliferation of cancer cell MDA-MB-231 with a GI50 of 11 nM. Mps1-IN-10 exhibits anti-tumor efficacy in mice MDA-MB-231 xenograft models .
    Mps1-IN-10
  • HY-B0067B
    (R)-Amrubicin

    (R)-SM-5887

    		 Topoisomerase Cancer
    (R)-Amrubicin ((R)-SM-5887) is an anthracycline that effectively treats lung cancer by intercalating into DNA and inhibiting topoisomerase II activity, which consequently hampers DNA replication as well as RNA and protein synthesis, leading to cell growth inhibition and apoptosis. This compound exhibits superior anti-tumor efficacy compared to traditional anthracycline drugs while lacking the cumulative cardiac toxicity typically associated with this drug class.
    (R)-Amrubicin
  • HY-169310
    ATM Inhibitor-11

    		ATM/ATR Cancer
    ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
    ATM Inhibitor-11
  • HY-115567
    5-NIdR

    1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole

    		 Apoptosis Cancer
    5-NIdR (1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole), an artificial nucleoside, exhibits the ability to inhibit the replication of DNA lesions generated by Temozolomide (HY-17364). 5-NIdR induces cancer cells apoptosis and arrests cell cycle at G0 phase. 5-NIdR enhances Temozolomide anti-tumor efficacy in murine glioblastoma model .
    5-NIdR
  • HY-149428
    AD4
    1 Publications Verification

    		 PROTACs Cancer
    AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy .
    AD4
  • HY-161826
    Antitumor agent-174

    		β-catenin HSP CDK c-Myc Cancer
    Antitumor agent-174 (Compound 10) directly engages the N-terminal site of Hsp90 and promotes the degradation of β-catenin, thereby suppressing the Wnt/β-catenin signaling. Antitumor agent-174 effectively inhibits proliferation, induce S and G2/M phases arrest and block the clonogenic ability in CRC cells. Antitumor agent-174 down-regulates CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, and upregulaties P21 proteins. Antitumor agent-174 has significant anti-tumor efficacy against colorectal cancer (CRC) with excellent pharmacokinetics and low toxicity .
    Antitumor agent-174
  • HY-155995
    PRO-905

    MK-905

    		 Biochemical Assay Reagents Cancer
    Pro-905 is a phosphite peptide with antitumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to the tumor. Pro-905 effectively prevents incorporation of purine salvage substrates into nucleic acids and inhibits colony formation in human malignant peripheral nerve sheath tumors (MPNST) cells. Pro-905 inhibits purine salvage incorporation to nucleic acids and prevents cell growth. Pro-905 inhibits the growth of MPNST and enhances the anti-tumor efficacy of JHU395 (HY-124778) .
    PRO-905
  • HY-156249
    NMS-P528

    		ADC Cytotoxin Cancer
    NMS-P528 is a Duocarmycin derivative that can be used as an ADC payload. NMS-P528 can be used to synthesize NMS-P945 .
    NMS-P528
  • HY-147214
    GNE-7883
    1 Publications Verification

    		 YAP Cancer
    GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
    GNE-7883
  • HY-121349
    Aerothionin

    		Bacterial Fungal Antibiotic Infection Cancer
    Aerothionin is an antibiotic with potent antimicrobial efficacy against bacteria and fungi. Aerothionin exhibits antitumor efficacy against adrenal pheochromocytomas and extra-adrenal paragangliomas (PPGLs) .
    Aerothionin
  • HY-151443
    HDAC-IN-47

    		HDAC Cancer
    HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
    HDAC-IN-47
  • HY-149539
    PLM-101

    		FLT3 RET Cancer
    PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
    PLM-101
  • HY-130115
    IACS-8803

    		STING Cancer
    IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy .
    IACS-8803
  • HY-159803
    IST-622

    6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin

    		 Endogenous Metabolite Cancer
    IST-622 (6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin) is an anti-tumor agent with significant growth inhibitory activity. IST-622 exhibits significant anti-tumor effects against a variety of mouse tumors such as P388 and L1210 leukemias, B16 melanoma, Lewis lung carcinoma, Colon 26 and Colon 38 adenocarcinomas, and M5076 reticulum cell sarcoma. IST-622 was orally administered and the results showed efficacy in different tumor types. In addition, IST-622 provided significant inhibitory effects against two human tumor xenograft models: large cell lung carcinoma (Lu-116) and gastric adenocarcinoma (St-4). IST-622 also exhibited significant growth inhibitory activity against P388 leukemia in vitro, with a half inhibitory concentration (IC50) more than 20 times lower than CT .
    IST-622
  • HY-130116
    IACS-8779

    		STING Cancer
    IACS-8779 is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy .
    IACS-8779
  • HY-161077
    QP5020

    		Amyloid-β Cancer
    QP5020 (compound 28) is an inhibitor of QPCTL with an IC 50 value of 15 nM. QP5020 has antitumor efficacy .
    QP5020
  • HY-161078
    QP5038

    		Amyloid-β Cancer
    QP5038 (compound 28) is an inhibitor of QPCTL with an IC50 value of 3.8 nM. QP5038 has antitumor efficacy .
    QP5038
  • HY-162449
    GIC-20

    		Apoptosis Ferroptosis Cancer
    GIC-20 is a dual inducer for apoptosis and ferroptosis. GIC-20 exhibits antitumor efficacy against fibrosarcoma .
    GIC-20
  • HY-115833
    Histamine H4 receptor antagonist-2

    		Histamine Receptor Cancer
    Histamine H4 receptor antagonist-2 serves as a potent activator of p53, demonstrating significant antitumor efficacy.
    Histamine H4 receptor antagonist-2
  • HY-158156
    NF-κB-IN-16

    		NF-κB Apoptosis Cancer
    NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models .
    NF-κB-IN-16
  • HY-163534
    PD-1/PD-L1-IN-43

    		PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-43 (compound Z13) is a small-molecule inhibitors targeting the PD-1/PD-L1 interaction. PD-1/PD-L1-IN-43 exhibites potent in vivo antitumor efficacy against B16-F10 melanoma. PD-1/PD-L1-IN-43 inhibits tumor growth by blocking the interaction between PD-1 and PD-L1. PD-1/PD-L1-IN-43 can be used in anti-tumor studies .
    PD-1/PD-L1-IN-43
  • HY-N1934
    Dihydroberberine

    		Potassium Channel HSP Cardiovascular Disease Inflammation/Immunology Cancer
    Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
    Dihydroberberine
  • HY-U00279B
    Nitracrine hydrochloride

    		DNA/RNA Synthesis Cancer
    Nitracrine hydrochloride is a platinum-based antineoplastic drug with selective toxicity to hypoxic cells. Nitracrine hydrochloride exhibits significant cytotoxicity against the Chinese hamster ovary cell line AA8 under hypoxic conditions and is approximately 100,000 times more potent than misonidazole. Nitracrine hydrochloride exerts its effect by binding to the insertion of DNA and forming covalent adducts. The cytotoxicity of Nitracrine hydrochloride under hypoxic conditions is related to its reductive metabolism to form alkylated substances. At the same time, it may enhance the reactivity to DNA through the insertion of DNA, thereby improving the efficacy. Nitracrine hydrochloride can also inhibit RNA synthesis, contributing to its anti-tumor effect .
    Nitracrine hydrochloride
  • HY-116452
    YLT192

    		VEGFR Cancer
    YLT192 is an orally active and highly bioavailable VEGFR2 inhibitor with potent anti-angiogenic activity and anti-tumor efficacy. YLT192 significantly inhibited the kinase activity of VEGFR2 and inhibited the proliferation, migration, invasion and tube formation of human umbilical cord vascular endothelial cells. YLT192 also inhibited VEGF-induced VEGFR2 phosphorylation and its downstream signaling regulators. YLT192 also showed the ability to inhibit angiogenesis in vivo in zebrafish embryo models and alginate-coated tumor cell experiments. YLT192 can directly inhibit the proliferation of cancer cells and induce their apoptosis .
    YLT192
  • HY-123891
    NS-062

    		EGFR Cancer
    NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC50 of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .
    NS-062
  • HY-130115A
    IACS-8803 disodium
    1 Publications Verification

    		 STING Cancer
    IACS-8803 disodium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 disodium has a robust systemic antitumor efficacy .
    IACS-8803 disodium
  • HY-130115B
    IACS-8803 diammonium
    1 Publications Verification

    		 STING Cancer
    IACS-8803 diammonium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 diammonium has a robust systemic antitumor efficacy .
    IACS-8803 diammonium
  • HY-155020
    Antitumor agent-101

    		Histone Methyltransferase GLP Receptor Cancer
    Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model .
    Antitumor agent-101
  • HY-119272
    EF24
    1 Publications Verification

    		 ERK Caspase NF-κB Apoptosis p38 MAPK Reactive Oxygen Species Inflammation/Immunology Cancer
    EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
    EF24
  • HY-100510
    RAF709
    5+ Cited Publications

    		 Raf Cancer
    RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively . Antitumor efficacy .
    RAF709

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