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Xenografted

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18

阻害剤およびアゴニスト

1

阻害性抗体

1

同位体標識化合物

製品番号 製品名 Target 研究分野 構造式
  • HY-131904
    POMHEX
    3 Publications Verification

    		 Enolase Apoptosis Metabolic Disease Cancer
    POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) proagent of HEX, is a potent, ENO2-specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor .
    POMHEX
  • HY-B0413
    Fenbendazole
    Maximum Cited Publications
    9 Publications Verification

    		 Parasite HIF/HIF Prolyl-Hydroxylase Microtubule/Tubulin Antibiotic Infection Cancer
    Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
    Fenbendazole
  • HY-B0413S
    Fenbendazole-d3
    5 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Parasite Microtubule/Tubulin Antibiotic Infection
    Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole-d3 is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
    Fenbendazole-d3
  • HY-139401
    FAPI-34

    		FAP Cancer
    FAPI-34 is a SPECT imaging agent targeting FAP. FAPI-34 specifically binds to FAP, is highly internalized by FAP-expressing cells, accumulates in FAP-expressing tumor lesions, and shows low uptake in normal tissues except the kidneys. FAPI-34 is applicable for tumor-related research .
    FAPI-34
  • HY-121607
    INI-43
    1 Publications Verification

    		 AP-1 Apoptosis Cancer
    INI-43 is an inhibitor of Kpnβ1, interfering with the nuclear localization of Kpnβ1 and known Kpnβ1 cargo proteins, NFAT, NFκB, AP-1, and NFY. INI-43 can inhibit the proliferation of cancer cells, cause G2-M cell cycle arrest in cancer cells, and induce the intrinsic apoptosis pathway .
    INI-43
  • HY-169240
    MX69-102

    		MDM-2/p53 Cancer
    MX69-102 (compound MX69-102) is an MDM-2/p53 inhibitor, inducing MDM2 degradation, resulting in p53 activation and cancer cell apoptosis. MX69-102 shows effective inhibition on xenografted human MDM2-overexpressing ALL in SCID mice. .
    MX69-102
  • HY-15805
    KIN-8194

    		Src Btk Cancer
    KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice .
    KIN-8194
  • HY-14811
    Beloranib

    ZGN-440; CKD-732 free base

    		 MetAP NF-κB Metabolic Disease
    Beloranib (ZGN-440; CKD-732 free base) is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib can be used in research on obesity and hypothalamic obesity .
    Beloranib
  • HY-B0413R
    Fenbendazole (Standard)

    		Reference Standards Parasite HIF/HIF Prolyl-Hydroxylase Microtubule/Tubulin Antibiotic Infection
    Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
    Fenbendazole (Standard)
  • HY-147696
    SMTIN-T140

    		HSP AMPK Reactive Oxygen Species (ROS) Cancer
    SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells .
    SMTIN-T140
  • HY-14811A
    Beloranib hemioxalate

    ZGN-440 hemioxalate; ZGN-433 hemioxalate; CDK732 hemioxalate

    		 NF-κB MetAP Metabolic Disease
    Beloranib (ZGN-440; CKD-732 free base) hemioxalate is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib hemioxalate blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib hemioxalate significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib hemioxalate also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib hemioxalate can be used in research on obesity and hypothalamic obesity .
    Beloranib hemioxalate
  • HY-174828
    ATR/PARP1-IN-1

    		PARP ATM/ATR Apoptosis Cancer
    ATR/PARP1-IN-1 is a potent ATR and PARP1 dual inhibitor with IC50s of 17.3 nM and 0.38 nM, respectively. ATR/PARP1-IN-1 effectively reduces cell viability, induces apoptosis and DNA damage. ATR/PARP1-IN-1 significantly impairs triple-negative breast cancer (TNBC) colony formation, migration, and invasion. ATR/PARP1-IN-1 suppresses tumor growth effectively in MDA-MB-468 xenografted mice, with no significant body weight change .
    ATR/PARP1-IN-1
  • HY-134920
    LW106

    		Indoleamine 2,3-Dioxygenase (IDO) Apoptosis SWI/SNF Complex Cancer
    LW106 is a selective IDO1 inhibitor with an IC50 of 1.57 μM. LW106 has no inhibitory effect on IDO2 and TDO. LW106 inhibits tumor outgrowth by limiting stroma-immune crosstalk and CSC enrichment in the tumor microenvironment. LW106 reduces subpopulation of cancer stem cells (CSCs) in xenografted tumors in which less proliferative/invasive tumor cells and more tumor cells apoptosis. LW106 can be used for the studies of lung cancer and melanoma .
    LW106
  • HY-146452
    Anticancer agent 57

    		Apoptosis Cancer
    Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC) .
    Anticancer agent 57
  • HY-B0530A
    Azacyclonol hydrochloride

    γ-pipradol hydrochloride

    		 Reactive Oxygen Species (ROS) mAChR NADPH Oxidase Cancer
    Azacyclonol (γ-pipradol) hydrochloride is a compound with promising anticancer activity, showing effectiveness in inhibiting NOX-derived ROS in A549 human lung cancer cells. Azacyclonol hydrochloride exhibits enhanced proliferation inhibition against androgen-refractory cancer cell lines, specifically DU145 and PC-3. Azacyclonol hydrochloride demonstrates antitumor activity in DU145-xenografted chorioallantoic membrane tumor models. Azacyclonol hydrochloride also acts as a ligand for the M3 muscarinic acetylcholine receptor, which is overexpressed in ARPC. Azacyclonol hydrochloride effectively blocks carbachol-induced proliferation and NOX activity in DU145 cells. Azacyclonol hydrochloride can also be utilized for the treatment of chronic schizophrenia.
    Azacyclonol hydrochloride
  • HY-118032
    Bozepinib

    		Apoptosis Autophagy JNK ERK Cancer
    Bozepinib is a PKR (RNA-dependent protein kinase) activator and potently inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces PKR-mediated apoptosis and synergizes with IFNα to trigger apoptosis, autophagy and senescence. Bozepinib also demonstrates in vivo antitumor and antimetastatic efficacy in xenografted nude mice .
    Bozepinib
  • HY-170576
    FLT3-IN-28

    		FLT3 STAT Apoptosis Cancer
    FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD .
    FLT3-IN-28
  • HY-P992372
    huAA98

    		Drug Derivative Transmembrane Glycoprotein Cancer
    huAA98 is a humanized monoclonal antibody and also a CD146 inhibitor. huAA98 binds to human CD146, regulates its activity and inhibits cancer-related angiogenesis, as well as tube formation, motility, proliferation and migration of endothelial cells. huAA98 inhibits angiogenesis in the chick chorioallantoic membrane assay and reduces microvessel density in human tumor xenograft models. huAA98 shows immunoreactivity only to neovascular vessels within tumors and inhibits the growth of tumor xenograft models. huAA98 can be used in studies related to cancer-related angiogenesis, liver cancer, leiomyosarcoma and pancreatic cancer .
    huAA98

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