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Anti-tumor Efficacy

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211

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6

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2

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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-113003
    H-γ-Glu-Gln-OH

    γ-Glutamylglutamine; γ-Glu-Gln

    		 Others Others
    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-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-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-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-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-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-163745
    MTX-3937

    		Others Cancer
    MTX-3937 is a Siglec-9 inhibitor with a Kd value of 3.15 μM. MTX-3937 enhances the functions and homeostasis of natural killer (NK) cells. MTX-3937 remarkably improves NK cell-mediated anti-tumor efficacy against liver cancer in vivo .
    MTX-3937
  • HY-115400
    1V209
    2 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-119272
    EF24
    1 Publications Verification

    		 ERK Caspase Cancer
    EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
    EF24
  • 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-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-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

    		 Others 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-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-130115
    IACS-8803

    		STING Cancer
    IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy .
    IACS-8803
  • 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-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-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-130115A
    IACS-8803 disodium

    		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

    		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-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
  • HY-133117A
    (Rac)-BAY-985

    		IKK Cancer
    (Rac)-BAY-985 (Compound Example 100.01) is a potent, ATP-competitive and selective TBK1 inhibitor with an IC50 of 1.5 nM. Antitumor efficacy .
    (Rac)-BAY-985
  • HY-155647
    Microtubule stabilizing agent-1

    		Microtubule/Tubulin Cancer
    Microtubule stabilizing agent-1 (compound 3l) is a Paclitaxel derivative that efficiently promotes tubulin polymerization. Microtubule stabilizing agent-1 shows antitumor efficacy .
    Microtubule stabilizing agent-1
  • HY-162085
    Axl-IN-17

    		TAM Receptor Cancer
    Axl-IN-17 (compound 13c) is an orally active, selective AXL inhibitor with an IC50 value of 3.2 nM. Axl-IN-17 reveals antitumor efficacy .
    Axl-IN-17
  • HY-P10255
    K90-114TAT

    		Potassium Channel Cancer
    K90-114TAT is an inhibitor for EAG2-Kvβ2 interaction, and exhibits antitumor efficacy against glioblastomas .
    K90-114TAT
  • HY-164386
    Defoslimod

    OM 174

    		 Toll-like Receptor (TLR) Inflammation/Immunology Cancer
    Defoslimod (OM 174) is an agonist for TLR4 receptor and acts as an immunomodulator. Defoslimod activates macrophages and dendritic cells, induces cytokines secretion, and exhibits antitumor efficacy in rats .
    Defoslimod
  • HY-163768
    Antitumor agent-172

    		β-catenin Inflammation/Immunology Cancer
    Antitumor agent-172 (Compound 28) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 3.92 μM. Antitumor agent-172 exhibits high affinity to β-catenin with Kd of 82 nM. Antitumor agent-172 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
    Antitumor agent-172
  • HY-120885
    (+)-Oxanthromicin

    		Ras Cancer
    (+)-Oxanthromicin (Compound 1) mislocalizes the oncogenic mutant K-Ras from the plasma membrane of intact Madin-Darby canine kidney (MDCK) cells, and exhibits thereby antitumor efficacy .
    (+)-Oxanthromicin
  • HY-138799A
    KA2507 monohydrochloride

    		HDAC Inflammation/Immunology Cancer
    KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities. KA2507 hydrochloride shows antitumor efficacy and immune modulatory effects .
    KA2507 monohydrochloride
  • HY-116447
    Antitumor agent-159

    		Mitochondrial Metabolism Apoptosis Cancer
    Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
    Antitumor agent-159
  • HY-147136
    MYF-03-176

    		Others Cancer
    MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration .
    MYF-03-176
  • HY-146231
    SS47

    		PROTACs MAP4K Inflammation/Immunology Cancer
    SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy .
    SS47
  • HY-115690
    K-TMZ

    		Others Cancer
    K-TMZ is a derivative of methyl ketone, which exhibits antitumor efficacy against O 6 -methylguanine DNA methyltransferase (MGMT) deficient cell. K-TMZ can be used for research of glioblastoma .
    K-TMZ
  • HY-117807
    A-176120

    		Ras Cancer
    A-176120 is a potent inhibitor of farnesyltransferase, crucial for Ras protein farnesylation in cancer cells. It exhibits high selectivity for farnesyltransferase (IC50 1.2 ± 0.3 nM) over related enzymes like geranylgeranyltransferases and squalene synthase. Inhibition of Ras processing in H-ras and K-ras mutated cells demonstrates its efficacy in blocking Ras-mediated signaling. A-176120 shows anti-angiogenic effects by inhibiting vascular endothelial growth factor (VEGF) secretion and disrupting capillary formation in endothelial cells. In vivo studies reveal its ability to reduce tumor growth in Ras-transformed cells and enhance survival in animal models. These findings highlight A-176120 as a promising FPP analogue with potent anti-tumor and anti-angiogenic properties .
    A-176120

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