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MDA-MB-231 xenograft models

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42

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2

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0841
    Bruceine A
    3 Publications Verification

    Dihydrobrusatol; NSC310616

    		 Parasite NF-κB p38 MAPK Phosphatase Apoptosis Infection Cancer
    Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research .
    Bruceine A
  • HY-173496
    ST6GAL1-IN-1

    		Sialyltransferase Integrin VEGFR Akt Cancer
    ST6GAL1-IN-1 is an orally active selective ST6GAL1 inhibitor (IC50 = 20 μM). ST6GAL1-IN-1 exhibits high antimetastatic potential, effectively inhibiting the migration of MDA-MB-231 cells at noncytotoxic concentrations. ST6GAL1-IN-1 can disrupt integrin sialylation in MDA-MB-231 cells. ST6GAL1-IN-1 inhibits tumor angiogenesis and cancer metastasis via the Integrin/VEGFR2-mediated signaling pathway. ST6GAL1-IN-1 effectively suppresses both tumor growth and cancer metastasis on the MDA-MB-231 xenograft model. ST6GAL1-IN-1 can be used for the study of Triple-negative breast cancer (TNBC) .
    ST6GAL1-IN-1
  • HY-P991577
    DS-8895

    DS-8895A

    		 Ephrin Receptor Cancer
    DS-8895(DS-8895A) is an anti-EphA2 monoclonal antibody with specific binding to EphA2 receptors and EphA2-expressing cells. DS-8895, when conjugated with 89Zr, 111In, or 125I, supports molecular imaging of EphA2 expression in xenograft models. DS-8895 allows noninvasive measurement of EphA2 expresssion in tumors in vivo. .
    DS-8895
  • HY-156715
    MASTL-IN-1

    		MASTL Cancer
    MASTL-IN-1 is a selective and orally active MASTL inhibitor with a Ki <0.03 nM. MASTL-IN-1 inhibits phosphorylation of ENSA and inhibits proliferation in cancer cells. MASTL-IN-1 induces tumor growth inhibition and stasis in pancreatic cancer xenograft models .
    MASTL-IN-1
  • HY-W111581
    Copper(II) diethyldithiocarbamate
    1 Publications Verification

    Diethyldithiocarbamic acid copper salt

    		 Apoptosis Caspase Cancer
    Copper(II) diethyldithiocarbamate (Diethyldithiocarbamic acid copper salt) is a Copper(II) and diethyldithiocarbamate coordination polymer. Copper(II) diethyldithiocarbamate binds tightly to NPL4 and induces its aggregation, disrupting the p97-NPL4-UFD1 pathway. Copper(II) diethyldithiocarbamate causes ubiquitinated proteins accumulation and impairs waste proteins degradation, thus resulting in cell apoptosis. Copper(II) diethyldithiocarbamate inhibits tumor growth in MDA-MB-231 xenograft mice models. Copper(II) diethyldithiocarbamate can be used for the research of cancer, such as breast cancer .
    Copper(II) diethyldithiocarbamate
  • HY-176428
    PROTAC MNK1 degrader-1

    P11-2

    		 PROTACs MNK Apoptosis Eukaryotic Initiation Factor (eIF) Cancer
    PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety . Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430
    PROTAC MNK1 degrader-1
  • 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-172888
    SPP-037

    		Endogenous Metabolite Sialyltransferase FAK Integrin Cancer
    SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50 = 3.59 μM). SPP-037 inhibits integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 inhibits cancer cell proliferation, migration and exhibits antiangiogenic activity. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used for the research of triple-negative breast cancer .
    SPP-037
  • HY-178367
    PFKFB4-IN-1

    		Phosphatase Apoptosis Caspase PARP Cancer
    PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. PFKFB4-IN-1 exhibits >12-fold selectivity over PFKFB1/4 and PFKFB3/4. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and inhibits cell migration. PFKFB4-IN-1 inhibits tumor growth in the MDA-MB-231 xenograft mouse model. PFKFB4-IN-1 can be used for breast, lung and liver cancer research .
    PFKFB4-IN-1
  • 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-164548
    WK88-1

    		HSP Apoptosis PI3K Akt NF-κB Inflammation/Immunology Cancer
    WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases .
    WK88-1
  • HY-179468
    STAT3-IN-49

    		STAT Cancer
    STAT3-IN-49 (compound B16) is a potent and selective STAT3 inhibitor. STAT3-IN-49 binds to the SH2 domain of STAT3, thereby suppressing its phosphorylation and nuclear translocation. STAT3-IN-49 inhibits triple-negative breast cancer (TNBC) cell migration, invasion, and colony formation. STAT3-IN-49 inhibits tumor growth in an MDA-MB-231 xenograft mouse model. STAT3-IN-49 can be used for TNBC research .
    STAT3-IN-49
  • HY-125807
    IS20

    		G Protein-coupled Receptor Kinase (GRK) Apoptosis Reactive Oxygen Species (ROS) Akt p38 MAPK Cardiovascular Disease Cancer
    IS20 is a Prokineticin receptor 1 (PKR1) agonist. IS20 diminishes Doxorubicin (HY-15142A) mediated apoptosis and ROS production by activating Akt or MAPK pathways. IS20 protects the heart against Doxorubicin-induced cardiovascular toxicity and improves the survival rate and cardiac function in mouse models. IS20 does not alter the cytotoxicity and antitumor activity of acute DOX treatment in breast cancer cells and MDA-MB-231 xenograft mouse models. IS20 can be used for cancers research .
    IS20
  • HY-103043
    Pz 285

    		Others Cancer
    Pz 285 is an anti-cancer agent. Pz 285 shows significant inhibitory effect on the viability of MDA-MB-231 breast cancer cells, with an IC50 of 15.0 μM. Pz 285 exhibits remarkable antitumor effects in the mouse tumor xenograft model constructed with highly lung-metastatic MDA-MB-231 LM24 Her2+ breast cancer cells. Pz 285 can be used for the study of breast cancer, especially metastatic breast cancer .
    Pz 285
  • HY-178343
    Aurora A-IN-5

    		Aurora Kinase Apoptosis Cancer
    Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
    Aurora A-IN-5
  • HY-122650
    PHY34

    		Autophagy Cancer
    PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer .
    PHY34
  • HY-176220
    GPX4-AUTAC

    		AUTACs Autophagy Glutathione Peroxidase Ferroptosis Cancer
    GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)) .
    GPX4-AUTAC
  • HY-203817
    IITZ-02

    		Autophagy Apoptosis Mitochondrial Metabolism Cancer
    IITZ-02 is a lysosomotropic Autophagy inhibitor. IITZ-02 enhances autophagosome accumulation but inhibits autophagosomal degradation by impairing lysosomal function, finally inducing the inhibition of autophagy. IITZ-02 abolishes mitochondrial membrane potential and induces apoptosis through the mitochondria-mediated pathway. IITZ-02 has a potent antitumor activity in MDA-MB-231 xenograft mouse models. IITZ-02 can be used for cancers research .
    IITZ-02
  • 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-106159
    SB-T-101141

    		Reactive Oxygen Species (ROS) p38 MAPK JNK PERK Ferroptosis Cancer
    SB-T-101141 is a novel taxane. SB-T-101141 effectively induces a noncanonical ferroptosis to overcome Paclitaxel (HY-B0015) resistance of breast cancer. SB-T-101141 facilitates the production of iron and ferrous ions and ROS. SB-T-101141 stably binds to KHSRP to inhibit the iron-dependent expression of CISD1 related to iron homeostasis. SB-T-101141 synergistically enhances the iron-dependent activation of JNK and PERK pathways via KHSRP. SB-T-101141 suppresses breast tumor growth in MCF-7(PR)/MDA-MB-231(PR) or KHSRP knock-down MCF-7 xenograft mice model .
    SB-T-101141
  • HY-173075
    Anticancer agent 267

    		RIP kinase Mixed Lineage Kinase Necroptosis Cancer
    Anticancer agent 267 (Compound 5q) is the activator for RIPK3 and MLKL. Anticancer agent 267 inhibits the proliferation in a variety of cancer cell lines (IC50 for MDA-MB-231, MDA-MB-486 and MCF-7 is 9.79, 10.77 and 5.94 μM, respectively), arrests cell cycle at subG1 phase, and induces necroptosis in cell MDA-MB-231. Anticancer agent 267 exhibits antitumor activity in mouse xenograft models .
    Anticancer agent 267
  • HY-139795
    ZYJ-25e

    		HDAC Cancer
    ZYJ-25e is a potent histone deacetylase inhibitor (HDACi) with IC50s of 0.047 μM and 0.139 μM for HDAC6 and HDAC8, respectively. ZYJ-25e is a tetrahydroisoquinoline-bearing hydroxamic acid analogue. ZYJ-25e shows marked antitumor potency in the MDA-MB231 xenograft model .
    ZYJ-25e
  • HY-172891
    CDK9/HDAC1/HDAC3-IN-1

    		CDK HDAC Apoptosis Cancer
    CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC50 s of 0.17  μM, 1.73  μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer .
    CDK9/HDAC1/HDAC3-IN-1
  • HY-163527
    FGFR-IN-13

    		FGFR Cancer
    FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
    FGFR-IN-13
  • 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-P991328
    MAb604.107

    		Notch Cancer
    MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .
    MAb604.107
  • HY-156077
    anti-TNBC agent-2

    		Apoptosis DNA/RNA Synthesis Cancer
    anti-TNBC agent-2 (3j) an anti-Triple negative breast cancer (TNBC) purine derivative. anti-TNBC agent-2 induces MDA-MB-231 cells apoptosis, and inhibits its migration and angiogenesis. anti-TNBC agent-2 inhibits tumor growth and metastasis and reduces the expression of Ki67 and CD31 protein in TNBC xenograft models. anti-TNBC agent-2 can be used for Triple negative breast cancer (TNBC) research .
    anti-TNBC agent-2
  • HY-162688
    Anticancer agent 239

    		Telomerase G-quadruplex Apoptosis Ferroptosis Others
    Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (Kd = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model .
    Anticancer agent 239
  • HY-139815
    ZYJ-34c

    		HDAC Cancer
    ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model .
    ZYJ-34c
  • HY-169994
    BC13

    		CDK Epigenetic Reader Domain Apoptosis DNA/RNA Synthesis Reactive Oxygen Species (ROS) Cancer
    BC13 is a CDK6/BRD4 inhibitor with the IC50 values of 234 nM and 36 nM for CDK6 and BRD4, respectively. BC13 shows antiproliferative activity and induces cell apoptosis and DNA damage. BC13 increases in ROS levels .
    BC13
  • HY-179430
    TTK-IN-5

    		Mps1 Cancer
    TTK-IN-5 is an orally active covalent threonine tyrosine kinase (TTK) inhibitor with selectivity (IC50 = 8.918 nM). TTK-IN-5 exhibits anti-proliferative potencies against MDA-MB-231, A2780, HCT116, HCC1569 and MKN1 cell lines (IC50 values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively). TTK-IN-5 potently suppresses tumor growth without notable toxicity in A2780 and MDA-MB-231 xenograft mouse models. TTK-IN-5 can be used for the research of cancer such as breast cancer and ovarian cancer .
    TTK-IN-5
  • HY-175805
    EGFR/HDAC-IN-2

    		EGFR HDAC Apoptosis Cancer
    EGFR/HDAC-IN-2 (Compound 38) is dual-functional inhibitor of EGFR and HDAC3 with IC50s of 20.34 and 1.09 nM for CDK9 and HDAC3, respectively. EGFR/HDAC-IN-2 has superior anti-proliferative activity against cancer cells, inhibits cell migration and induces late-stage cell apoptosis. EGFR/HDAC-IN-2 significantly inhibits triple-negative breast cancer (TNBC) tumor growth in xenograft mouse models. EGFR/HDAC-IN-2 can be used for cancers like TNBC research .
    EGFR/HDAC-IN-2
  • HY-180814
    SKF-83566-PEG1-pomalidomide

    		Drug Derivative Dopamine Receptor Cancer
    SKF-83566-PEG1-pomalidomide is an anti-tumor agent and is formed by the covalent connection of SKF-83566 (HY-103430A) (dopamine D1 receptor antagonist) and Pomalidomide (HY-10984) (immunomodulatory agent). SKF-83566-PEG1-pomalidomide can inhibit cancer cells invasion, migration and colony formation. SKF-83566-PEG1-pomalidomide can inhibit tumor growth and angiogenesis in MDA-MB-231 cell chicken embryo chorioallantoic membrane (CAM) xenograft model. SKF-83566-PEG1-pomalidomide can be used for research of breast cancer .
    SKF-83566-PEG1-pomalidomide
  • HY-181928
    PARP1/c-Met-IN-3

    		c-Met/HGFR PARP Apoptosis Cancer
    PARP1/c-Met-IN-3 (Compound L19) is a selective c-Met and PARP1 inhibitor, with an IC50 of 5.4 nM against c-Met and an IC50 of 3.7 nM against PARP1. PARP1/c-Met-IN-3 inhibits PARP2 enzymatic activity with an IC50 of 4.52 nM, and shows no specificity for PARP1 and PARP2. PARP1/c-Met-IN-3 induces cell cycle arrest and apoptosis. PARP1/c-Met-IN-3 exhibits anti-tumor activity against triple-negative breast cancer .
    PARP1/c-Met-IN-3
  • HY-P10792A
    HYNIC-H6F

    		EGFR Cancer
    HYNIC-H6F is a SPECT imaging probe with binding specificity for human epidermal growth factor receptor 2 (HER2) domain II (IC50 = 11 nM). HYNIC-H6F accumulates in HER2-positive breast cancer xenografts via receptor-mediated uptake, while shows low uptake in HER2-negative breast cancer xenografts. HYNIC-H6F enables non-invasive detection of HER2-positive breast cancer in mouse models and allows evaluation of HER2 expression levels without blocking interference. HYNIC-H6F can be used in breast cancer-related research .
    HYNIC-H6F
  • HY-181823
    HOXA1-IN-1

    		HOXA TGF-beta/Smad Apoptosis Cancer
    HOXA1-IN-1 is a HOXA1 inhibitor. HOXA1-IN-1 downregulates HOXA1 protein levels, suppresses its transcriptional activity, and alters the expression of its downstream target genes. HOXA1-IN-1 induces DNA damage and apoptosis in cancer cells. HOXA1-IN-1 exhibits antitumor efficacy in xenograft models of colorectal cancer and triple-negative breast cancer. HOXA1-IN-1 shows synergistic activity in combination with Cisplatin (HY-17394). HOXA1-IN-1 can be used for the research of colorectal cancer and triple-negative breast cancer .
    HOXA1-IN-1
  • HY-183771
    CDK4/6-IN-28

    		CDK Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism Bcl-2 Family Caspase Cancer
    CDK4/6-IN-28 is a potent, orally active, and selective CDK4/6 inhibitor IC50 values of 14.02 and 10.03 nM, respectively. CDK4/6-IN-28 inhibits breast cancer cell colony formation, migration, and proliferation. CDK4/6-IN-28 induces G1-phase cell cycle arrest and apoptosis in breast cancer cells. CDK4/6-IN-28 exhibits tumor inhibitory activity in breast cancer xenograft mouse models. CDK4/6-IN-28 can be used for the research of breast cancer .
    CDK4/6-IN-28
  • HY-181797
    CL121

    		Amyloid-β CD47 Cancer
    CL121 is a Glutaminyl Cyclase inhibitor with an IC50 of 0.07 μM against human sQC and an IC50 of 0.54 μM against human gQC. CL121 reduces the level of pyroglutamate (pE)-modified CD47 on the surface of cancer cells. CL121 exhibits anti-tumor activity against triple-negative breast cancer .
    CL121
  • HY-181764
    LZL50

    		Ser/Thr Protease Cancer
    LZL50 is an orally effective human caseinolytic protease P (hClpP) activator with an EC50 of 0.29 μM. LZL50 activates hClpP, a serine protease that mediates mitochondrial quality control by degrading damaged or misfolded mitochondrial proteins. LZL50 exhibits antitumor activity in a breast cancer xenograft mouse model. LZL50 can be used in research related to breast cancer .
    LZL50
  • HY-182700
    NRPa-308

    		Complement System VEGFR Cancer
    NRPa-308 is a potent and orally active Neuropilin-1 (NRP-1) antagonist with an IC50 of 42 μM for inhibiting VEGF-A165 binding to NRP-1. NRPa-308 blocks the specific interaction between VEGF-A165 and NRP-1. NRPa-308 effectively suppresses angiogenesis in vitro and in vivo and reduces the viability of a broad spectrum of human solid and haematological cancer cells. NRPa-308 inhibits tumor growth and prolongs median survival in a human breast cancer xenograft mouse model. NRPa-308 can be used for the research of multiple human malignancies including solid tumors and hematological cancers .
    NRPa-308
  • HY-181562
    WRN-IN-24

    		DNA/RNA Synthesis Cancer
    WRN-IN-24 is an orally active allosteric covalent Werner syndrome helicase (WRN) inhibitor with an IC50 of 201 nM. WRN-IN-24 binds to a novel allosteric cavity, forms an additional hydrogen bond with K894, and functionally inhibits WRN activity. WRN-IN-24 inhibits colorectal cancer cells proliferation and exerts dose-dependent antitumor activity in xenograft mouse models. WRN-IN-24 can be used for the research of microsatellite instability-high cancers, including colorectal cancer .
    WRN-IN-24
  • HY-181529
    NCATS-SM0225

    		VDAC PERK Cancer
    NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, VDAC2 and VDAC3. NCATS-SM0225 exhibits an IC50of 1.02 μM for ERAD and a Kd of 3.13 μM for human VDAC1 binding. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling and activating PERK. NCATS-SM0225 selectively kills cancer cells, exhibits tumor growth inhibitory effects in melanoma xenograft models. NCATS-SM0225 can be used for research on multiple cancers including melanoma, as well as the molecular mechanisms of ERAD and calcium homeostasis regulation .
    NCATS-SM0225

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