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Tumor Selectivity

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50895
    Gefitinib
    195+ Cited Publications

    ZD1839

    		 EGFR Autophagy Apoptosis Cancer
    Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
    Gefitinib
  • HY-101120
    666-15
    55+ Cited Publications

    		 Epigenetic Reader Domain Cancer
    666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model .
    666-15
  • HY-101566
    Elimusertib
    10+ Cited Publications

    BAY 1895344

    		 ATM/ATR Cancer
    Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity . Elimusertib can be used for the research of solid tumors and lymphomas .
    Elimusertib
  • HY-110203
    R-7050
    25+ Cited Publications

    TNF-α Antagonist III

    		 TNF Receptor Cancer
    R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
    R-7050
  • HY-139361
    Sulfopin
    3 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-P9978
    Toripalimab

    JS-001

    		 PD-1/PD-L1 Cancer
    Toripalimab is a selective, recombinant, humanized monoclonal antibody against PD-1. Toripalimab is able to bind to PD-1 and block the interaction with its ligands. Toripalimab has exhibited primary anti-tumor effects in tumors such as melanoma, lung cancer, digestive tract tumors, hepatobiliary and pancreatic tumors, neuroendocrine neoplasms, nasopharyngeal carcinoma and urothelial carcinoma .
    Toripalimab
  • HY-P6292A
    KS-133 TFA

    		PACAP Receptor Neurological Disease Inflammation/Immunology Cancer
    KS-133 TFA is a highly selective and potent antagonist of the vascular active enteropeptide receptor 2 (VIPR2) with IC50 values for Ca influx measurement and cAMP measurement of 24.8 nM and 500 nM, respectively. KS-133 TFA reverses the tumor-promoting M2 phenotype of tumor-associated macrophages to the anti-tumor M1 phenotype, alters the tumor immune microenvironment, and inhibits tumor growth. KS-133 TFA can be used for research on schizophrenia and cancer immune regulation .
    KS-133 TFA
  • HY-136979
    RBN012759
    10+ Cited Publications

    		 PARP Inflammation/Immunology Cancer
    RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants .
    RBN012759
  • HY-50895A
    Gefitinib hydrochloride
    195+ Cited Publications

    ZD-1839 hydrochloride

    		 EGFR Cancer
    Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity .
    Gefitinib hydrochloride
  • HY-12710
    Rauwolscine
    1 Publications Verification

    α-Yohimbine; Corynanthidine; Isoyohimbine

    		 Adrenergic Receptor Cancer
    Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis .
    Rauwolscine
  • HY-134957
    VT107
    5+ Cited Publications

    		 YAP Cancer
    VT-107, as an analogous to VT104, is an orally active and potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer .
    VT107
  • HY-13775
    XL019
    5 Publications Verification

    		 JAK Apoptosis Cancer
    XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .
    XL019
  • HY-P99547
    Trastuzumab duocarmazine

    (vic)-Trastuzumab duocarmazine

    		 Antibody-Drug Conjugates (ADCs) Cancer
    Trastuzumab duocarmazine ((vic)-Trastuzumab duocarmazine) is a HER2-targeting ADC that is recognized and cleaved by histone B in tumor cells and selectively targets tumor cells. Trastuzumab duocarmazine has anti-tumor activity and can be used in cancer research related to uterine and ovarian sarcomas .
    Trastuzumab duocarmazine
  • HY-106033
    Edotreotide
    2 Publications Verification

    DOTATOC; SDZ-SMT 487; SMT 487

    		 Radionuclide-Drug Conjugates (RDCs) Cancer
    Edotreotide is a ligand that selectively targets SSTR2 and can competitively bind to the receptor. Edotreotide mediates the targeted delivery, while modificated with radionuclides (such as 90Y, 177Lu, and 68Ga) to SSTR-positive tumors and induces tumor cell apoptosis by releasing β rays. Edotreotide has strong tumor targeting and precise killing activity. Edotreotide is used in the synthesis of radionuclide-drug conjugates (RDCs) and is widely used in the field of neuroendocrine tumors (such as metastatic carcinoids, lung and thymus NETs) .
    Edotreotide
  • HY-153358
    TNG260

    		HDAC Cancer
    TNG260 is a selective, orally effective inhibitor of HDAC1 and CoREST complex, with a 10-fold selectivity for HDAC1 over HDAC3 and a 500-fold selectivity for CoREST complex over NuRD and Sin3 complex. TNG260 reshapes the tumor immune microenvironment, reduces immunosuppressive neutrophil infiltration, promotes effector T cell recruitment, and reverses anti-PD-1 resistance caused by STK11 deficiency by inhibiting the activity of the CoREST-HDAC1 complex. TNG260 induces durable tumor regression in combination with α-PD1 in MC38 tumor-bearing mice with STK11 mutations, and has lower toxicity to bone marrow cells than non-selective HDAC inhibitors .
    TNG260
  • HY-172429
    Enozertinib

    ORIC-114

    		 EGFR Neurological Disease Cancer
    Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
    Enozertinib
  • HY-106381
    Aurothiomalate sodium

    		PKC Inflammation/Immunology Cancer
    Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cell apoptosis. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity .
    Aurothiomalate sodium
  • HY-134463
    NHWD-870
    1 Publications Verification

    		 Epigenetic Reader Domain Apoptosis Cancer
    NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
    NHWD-870
  • HY-114169
    WRG-28
    2 Publications Verification

    		 Discoidin Domain Receptor Inflammation/Immunology Cancer
    WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice .
    WRG-28
  • HY-138742
    HPK1-IN-7

    		MAP4K Cancer
    HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .
    HPK1-IN-7
  • HY-P1007
    Z-VEID-FMK

    Z-VE(OMe)ID(OMe)-FMK

    		 Caspase Apoptosis Cancer
    Z-VEID-FMK (Z-VE(OMe)ID(OMe)-FMK) is a selective and irreversible caspase-6 peptide inhibitor. Z-VEID-FMK alleviates the drug-induced augmentation of caspase-6 activity, DNA fragmentation, and cell apoptosis .
    Z-VEID-FMK
  • HY-121087
    BCI-215
    3 Publications Verification

    		 Phosphatase Cancer
    BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells .
    BCI-215
  • HY-128587
    Mevociclib
    5+ Cited Publications

    SY-1365

    		 CDK Cancer
    Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors .
    Mevociclib
  • HY-101566A
    Elimusertib hydrochloride
    10+ Cited Publications

    BAY 1895344 hydrochloride

    		 ATM/ATR Cancer
    Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity . Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas .
    Elimusertib hydrochloride
  • HY-112181
    KO-947
    4 Publications Verification

    		 ERK Cancer
    KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
    KO-947
  • HY-151590
    DKFZ-748

    		HDAC Cancer
    DKFZ-748 is a selective HDAC10 inhibitor (pIC50=7.66), and shows anti-tumor activity .
    DKFZ-748
  • HY-126330
    SS-208

    AVS100

    		 HDAC Cancer
    SS-208 is a selective HDAC6 inhibitor, with an IC50 of 12 nM. SS-208 possesses anti-tumor activity in melanoma .
    SS-208
  • HY-160215
    GFH018

    		TGF-β Receptor p38 MAPK TGF-beta/Smad Interleukin Related Cancer
    GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma .
    GFH018
  • HY-124676A
    DB2115 tertahydrochloride
    1 Publications Verification

    		 Apoptosis Cancer
    DB2115 tetrahydrochloride is a highly selective PU.1 inhibitor that suppresses the binding of PU.1 to DNA (IC50: 2.3 nM). DB2115 tetrahydrochloride can inhibit tumor cell proliferation and induce apoptosis. DB2115 tetrahydrochloride can be used in the research of tumors such as leukemia .
    DB2115 tertahydrochloride
  • HY-143889
    Senexin C

    		CDK Cancer
    Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
    Senexin C
  • HY-P2526
    LyP-1
    2 Publications Verification

    		 Complement System Cancer
    LyP-1 is a cyclic 9-amino-acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
    LyP-1
  • HY-134885
    RMC-0331
    1 Publications Verification

    RM-023

    		 SHP2 SOS1 Ras Cancer
    RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction .
    RMC-0331
  • HY-143510
    RMC-4627

    		mTOR Cancer
    RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.
    RMC-4627
  • HY-151425
    TDO-IN-1

    		Indoleamine 2,3-Dioxygenase (IDO) Cancer
    TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), shows excellent selectivity over indoleamine-2,3-dioxygenase (IDO), with an IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo .
    TDO-IN-1
  • HY-19747
    HPOB
    3 Publications Verification

    		 HDAC Apoptosis Cancer
    HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6 .
    HPOB
  • HY-172429A
    Enozertinib hemihydrate

    ORIC-114 hemihydrate

    		 EGFR Neurological Disease Cancer
    Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
    Enozertinib hemihydrate
  • HY-P991061
    Tagmokitug

    CHS-114; SRF-114

    		 CCR Cancer
    Tagmokitug (CHS-114; SRF-114) is a fully human IgG1 antibody targeting CCR8. Tagmokitug selectively binds to human CCR8 (Kd = 502 pM) and mediates the death of CCR8-expressing cells via antibody-dependent cellular cytotoxicity and antibody-dependent cellular phagocytosis. Tagmokitug selectively eliminates intratumoral regulatory T cells, induces tumor growth inhibition, remodels the tumor immune microenvironment, and promotes the differentiation of cytotoxic CD8 + T cell subsets. Tagmokitug can be used for the research of solid tumors .
    Tagmokitug
  • HY-172663A
    Trabectedin derivative 1 TFA

    		DNA/RNA Synthesis Apoptosis Cancer
    Trabectedin derivative 1 TFA is a selective DNA minor groove binder. Trabectedin derivative 1 TFA inhibits DNA transcription and repair to induce tumor cell apoptosis. Trabectedin derivative 1 TFA is promising for research of solid tumors such as soft tissue sarcoma and ovarian cancer .
    Trabectedin derivative 1 TFA
  • HY-16405
    PR-104

    		DNA Alkylator/Crosslinker Cancer
    PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
    PR-104
  • HY-137813
    PERK-IN-4

    		PERK Neurological Disease Metabolic Disease Cancer
    PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states .
    PERK-IN-4
  • HY-124711
    TBOPP
    1 Publications Verification

    		 DOCK Cancer
    TBOPP is a selective inhibitor of DOCK1 with an IC50 of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (Kd of 7.1 μM), has anti-tumor activity for broader types of tumors .
    TBOPP
  • HY-111213
    PRMT5-IN-20

    		Histone Methyltransferase Cancer
    PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity .
    PRMT5-IN-20
  • HY-129125
    YMU1

    		STAT Cancer
    YMU1 is a selective inhibitor of human thymidylate kinase (hTMPK) with an IC50 of 610 nM. YMU1 inhibits tumor proliferation .
    YMU1
  • HY-147894
    PCAF-IN-1
    1 Publications Verification

    		 Histone Acetyltransferase Cancer
    PCAF-IN-1 is a highly selective PCAF inhibitor. PCAF-IN-1 is a antitumor agents, which can be used in tumor research research .
    PCAF-IN-1
  • HY-110201
    Estrogen receptor modulator 1

    		Estrogen Receptor/ERR Cancer
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
    Estrogen receptor modulator 1
  • HY-172930
    PVTX-405

    		Molecular Glues IKZF Family Potassium Channel Inflammation/Immunology Cancer
    PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50  of  0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
    PVTX-405
  • HY-149616
    PPM-3

    		PROTACs ERK Cancer
    PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages .
    PPM-3
  • HY-164546
    WB436B

    		STAT Apoptosis Cancer
    WB436B is a highly selective STAT3 inhibitor. WB436B can selectively inhibit STAT3-Tyr705 phosphorylation and the expression of STAT3 target genes, showing cytotoxic effects on pancreatic cancer cells and inducing apoptosis. WB436B can suppress tumor growth and metastasis in pancreatic cancer mouse models, extending the survival of tumor-bearing mice .
    WB436B
  • HY-156675A
    Plecstatin-1 hydrochloride
    1 Publications Verification

    		 Microtubule/Tubulin Cancer
    Plecstatin-1 hydrochloride is an anticancer agent containing organoeuropium. Plecstatin-1 hydrochloride selectively targets plectin, a scaffolding protein and cellular connector, in tumor spheroids .
    Plecstatin-1 hydrochloride
  • HY-156602
    Bocodepsin

    OKI-179

    		 HDAC Cancer
    Bocodepsin (OKI-179) is an orally active and selective HDAC inhibitor, with antitumor activity. Bocodepsin can be used for suppression on solid tumor and hematologic malignancies .
    Bocodepsin

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