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triple-negative breast tumor

" in MedChemExpress (MCE) Product Catalog:

62

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1

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1

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9

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-141600

    BAY 1187982

    Antibody-Drug Conjugates (ADCs) FGFR Microtubule/Tubulin Apoptosis Cancer
    Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) to target FGFR2 and the first to use Auristatin-based payload. Aprutumab ixadotin contains a fully human anti-FGFR2 monoclonal antibody (Aprutumab) (HY-P99007) conjugated by lysine side chains to a non-cleavable linker and via this an innovative Auristatin W derivative. Aprutumab ixadotin can be used for the study of advanced solid tumors, such as FGFR2-positive gastric cancer and triple-negative breast cancer .
    Aprutumab ixadotin
  • HY-P990552A

    MNPR-101

    Integrin Cancer
    huATN-658 (MNPR-101) is a humanized monoclonal antibody inhibitor targeting urokinase-type plasminogen activator receptor (uPAR). huATN-658 blocks the interaction between uPAR and integrins, inhibiting the proliferation, invasion and migration of tumor cells. huATN-658 is promising for research of breast cancer (especially triple-negative breast cancer) .
    huATN-658
  • HY-155663
    GPX4-IN-5
    1 Publications Verification

    Glutathione Peroxidase Ferroptosis Cancer
    GPX4-IN-5 is a covalent inhibitor of GPX4 (IC50: 0.12 μM). GPX4-IN-5 can induce ferroptosis and has anti-tumor effects. GPX4-IN-5 can be used in the study of triple-negative breast cancer (TNBC) .
    GPX4-IN-5
  • HY-18953

    mTOR Cancer
    mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .
    mTOR inhibitor-23
  • HY-122703

    Epigenetic Reader Domain Cancer
    BETi-211 is an orally active BET inhibitor (Ki: <1 nM). BETi-211 inhibits growth of triple-negative breast cancers (TNBC) cell lines with IC50 < 1 μM. BETi-211 degrades BET proteins and suppress tumor growth in xenograft breast tumors .
    BETi-211
  • HY-P10853

    Autophagy Cancer
    Bacilotetrin C analogue is cytotoxic to triple-negative breast cancer cell line MDA-MB-231 with an IC50 of 0.48 μM. Bacilotetrin C analogue can induce tumor cell autophagy and has anti-tumor activity .
    Bacilotetrin C analogue
  • HY-149847

    Ras Cancer
    JH530 is an effective methuosis inducer that inhibits the triple-negative breast cancer (TNBC) cells proliferation by causing intracellular complete vacuolization. JH530 has anti-tumor activity and can be used for cancer research .
    JH530
  • HY-155251

    Apoptosis Bcl-2 Family Cancer
    anti-TNBC agent-3 (compound 3g) is an apoptosis inducer with anti-cancer cell proliferation activity. anti-TNBC agent-3 inhibits tumor growth and metastasis in triple-negative breast cancer (TNBC) xenograft models .
    anti-TNBC agent-3
  • HY-168950

    Annexin A Cancer
    ANXA3 degrader 1 (Compound 18a5) is a highly selective ANXA3 degrader with cancer cell inhibition activity. ANXA3 degrader 1 displays excellent inhibitory effect in a triple-negative breast cancer (TNBC) tumor xenograft model (TGI=96%) .
    ANXA3 degrader 1
  • HY-161774

    CD73 Cancer
    ST80 is an inhibitor for interaction of OTUD4 and CD73. ST80 decreases CD73 protein level, increases CD73 protein turnover, reduces immune evasion of tumor cells, and thus exhibits antitumor efficacy against immunosuppressive triple-negative breast cancer (TNBC) .
    ST80
  • HY-173211

    Photosensitizer Cancer
    anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic agent targeting mitochondrial DNA G4 (mtG4). Under white light irradiation, its IC50 against 4T1 cells is 0.42 μM. anti-TNBC agent-8 binds tightly to mtG4 and generates a large amount of reactive oxygen species (ROS) under white light irradiation, leading to the loss of mitochondrial membrane potential (MMP), a decrease in ATP production, and an increase in the ROS level. This, in turn, induces significant apoptosis in triple-negative breast cancer (TNBC) cells, exerting the activity of inhibiting tumor cell growth. anti-TNBC agent-8 can be used in the research of triple-negative breast cancer.
    anti-TNBC agent-8
  • HY-136420

    PROTACs Raf Apoptosis Cancer
    SJF-0628 is a RAF PROTAC degrader. SJF-0628 induces targeted degradation of BRAF in various cancer cell lines (colorectal cancer cell lines (Colo-205, LS-411N, HT-29, RKO) and triple-negative breast cancer cell line DU-4475). SJF-0628 decreases pMEK and pErk levels in DU-4475 cells. SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of colorectal cancer and triple-negative breast cancer. (Pink: RAF ligand (HY-12057), Blue: VHL Ligand ( HY-125845), Black: Linker (HY-B0912)) .
    SJF-0628
  • HY-157210

    CDK Cancer
    CDK7-IN-26 (compound 36) is an orally active CDK7 inhibitor (IC50: 7.4 nM). CDK7-IN-26 potently inhibits the growth of triple-negative breast cancer (TNBC) cell line-derived xenograft (CDX) tumors in vivo and inhibits MDA-MB-453 cells in vitro with an IC50 of 0.15 μM .
    CDK7-IN-26
  • HY-P991372

    RN927C antibody

    TROP2 Cancer
    Anti-TROP2 Antibody (RN927C antibody) is a human monoclonal antibody (mAb) targeting TROP2. Anti-TROP2 Antibody has an inhibitory effect on multiple tumor cell lines in vitro. Anti-TROP2 Antibody has anti-tumor activity in mouse pancreatic PDX, ovarian PDX, lung LG0476 PDX, and triple-negative breast cancer (TNB) PDX models .
    Anti-TROP2 Antibody
  • HY-158378

    R-AST-OH

    Glutaminase Cancer
    Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy .
    Trivalent hydroxyarsinothricn
  • HY-W338764

    Apoptosis Aryl Hydrocarbon Receptor Cancer
    AHR agonist 3 is an aryl hydrocarbon receptor (AhR) agonist, that can induces cell cycle arrest or apoptosis via activation of tumor-suppressive transcriptional programs. AHR agonist 3 inhibits triple-negative breast cancer (TNBC) stem cell growth via AhR while exhibits minimal cytotoxicity against normal human primary cells and can be used for cancer research .
    AHR agonist 3
  • HY-157396

    Aurora Kinase Apoptosis Caspase Cancer
    JAB-2485 is an orally active and selective Aurora kinase A (AURKA) inhibitor with an IC50 value of 0.327 nM. JAB-2485 exhibits inhibitory activity against various tumor cell lines such as neuroblastoma, triple-negative breast cancer, small cell lung cancer, and epithelial ovarian cancer. JAB-2485 can induce cell cycle arrest and apoptosis in tumor cells. JAB-2485 has antitumor activity .
    JAB-2485
  • HY-172175

    mTOR Akt PI3K Apoptosis Autophagy Cancer
    HYS-072 is an orally active derivative of chrysin (HY-14589) with antitumor activity. HYS-072 induces apoptosis and autophagy by inhibiting the PI3K/AKT/mTOR signaling pathway and suppresses tumor growth in vivo in xenograft models by modulating autophagy-related pathways. HYS-072 can be used in the research of triple-negative breast cancer .
    HYS-072
  • HY-178487

    HDAC DNA/RNA Synthesis NO Synthase Apoptosis Cancer
    anti-TNBC agent-12 (Compound 23a) is a multi-target antitumor agent targeting HDAC6 (IC50=30.3 nM), DNA, and inducing nitric oxide (NO) release. anti-TNBC agent-12 induces tumor cell apoptosis and G2/M phase cell cycle arrest. anti-TNBC agent-12 is promising for research of triple-negative breast cancer (TNBC) .
    anti-TNBC agent-12
  • HY-P10947

    Epigenetic Reader Domain YAP Cancer
    MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206 + tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models .
    MACTIDE-V
  • HY-176259

    PROTACs Galectin Apoptosis Cancer
    F3-PEG8-RiboTAC is a RiboTAC that can specifically degrade the mRNA of the oncogene LGALS1. F3-PEG8-RiboTAC can induce tumor cell apoptosis and inhibit invasion. F3-PEG8-RiboTAC has anti-tumor activity and can be used in the research of tumors such as leukemia and triple-negative breast cancer. (RNase L ligand (HY-177030); RNA binder (HY-177031); Linker (HY-W019798)) .
    F3-PEG8-RiboTAC
  • HY-162494

    Protein Arginine Deiminase Cancer
    PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC50=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research .
    PAD4-IN-4
  • HY-170948

    Adenosine Receptor Cancer
    A2AR modulator-1 (Compound 45) is a selective negative allosteric adenosine A2a receptor (A2aR) modulator with an IC50 value of 9 nM. A2AR modulator-1 reduces the affinity of endogenous adenosine for the receptor and inhibits cAMP signaling pathway activation. A2AR modulator-1 potently restores pCREB phosphorylation in CD4 + T cells, reversing immunosuppression in the tumor microenvironment, and shows potential to suppress tumor growth and metastasis in triple-negative breast cancer models .
    A2AR modulator-1
  • HY-168894

    Ferroptosis Cancer
    CT-1 is a derivative of Cryptotanshinone (HY-N0174). CT-1 is a ferroptosis inducer. CT-1 promotes the interaction between NCOA4 and ferritin by targeting FTH1, triggering ferritinophagy-mediated ferroptosis. CT-1 has anticancer activity against triple-negative breast cancer (TNBC). CT-1 induces ferroptosis in both N2-type tumor-associated neutrophils (TANs) and TNBC cancer cells .
    CT-1
  • HY-P99045
    Sacituzumab
    3 Publications Verification

    ADC Antibody TROP2 Cancer
    Sacituzumab is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab can be used for the synthesis of antibody-drug conjugates (ADC) drug Sacituzumab govitecan (HY-132254). Sacituzumab govitecan can be used in the field of triple-negative breast cancer .
    Sacituzumab
  • HY-175039

    FAK Apoptosis Reactive Oxygen Species (ROS) Caspase Cancer
    FAK-IN-28 is an orally active FAK inhibitor (IC50 = 0.4 nM). FAK-IN-28 exhibits dual antiproliferative and anti-metastatic properties. FAK-IN-28 triggers caspase-3-dependent apoptosis via ROS elevation. FAK-IN-28 inhibits tumor growth without causing weight loss or hepatotoxicity. FAK-IN-28 is useful in the study of FAK-driven malignancies, such as colon cancer, cervical cancer, triple-negative breast cancer, and melanoma .
    FAK-IN-28
  • HY-P991621

    EOS-215

    TREM receptor Cancer
    EOS006215 is a humanized monoclonal antibody inhibitor targeting TREM-2. EOS006215 reprograms TREM2 + macrophages, significantly blocks their pleiotropic pro-tumoral functions and overcomes resistance. EOS215 decreases metastasis burden in orthotopic 4T1 triple negative breast cancer mice model and significantly inhibits tumor growth in anti-PD-1 resistant mice model. EOS006215 can be used to study advanced malignant solid neoplasm, such as triple negative breast cancer (TNBC) .
    EOS006215
  • HY-155246

    Apoptosis PARP Cancer
    PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations .
    PARP1-IN-15
  • HY-P99045A

    ADC Antibody TROP2 Cancer
    Sacituzumab (powder) is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab (powder) demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab (powder) can be used for the synthesis of antibody-drug conjugates (ADC) drug Sacituzumab govitecan (HY-132254). Sacituzumab govitecan can be used in the field of triple-negative breast cancer .
    Sacituzumab (powder)
  • HY-174345

    Ferroptosis Glutathione Peroxidase Reactive Oxygen Species (ROS) Cancer
    Ferroptosis inducer-8 is a ferroptosis inducer with high selectivity for other cell death mechanism. Ferroptosis inducer-8 induces ferroptosis by affecting ACSL4, GPX4, and FTH1, thereby disrupting intracellular iron homeostasis and the GSH/GPX4 antioxidant defense system, ultimately leading to the accumulation of lipid peroxidation. Ferroptosis inducer-8 also induces ROS production. Ferroptosis inducer-8 inhibits tumor growth and can be used for research of triple-negative breast cancer (TNBC) .
    Ferroptosis inducer-8
  • HY-P991664

    Src Akt ERK TAM Receptor c-Met/HGFR MMP HIF/HIF Prolyl-Hydroxylase VEGFR Cancer
    AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers .
    AG01
  • HY-175341

    Acyltransferase Ras Akt Cancer
    Rac1-IN-5 is a specific, reversible inhibitor of RAC1 (KD = 30 nM). Rac1-IN-5 competes with guanine nucleotides for specific binding to RAC proteins, effectively blocking RAC1 activity and RAC1-dependent cellular functions. Rac1-IN-5 exhibits anti-tumor metastasis effects in vivo and can improve survival. Rac1-IN-5 can be used to study invasive cancers such as triple-negative breast cancer and colon cancer .
    Rac1-IN-5
  • HY-P99682

    hLIV22

    ADC Antibody Cancer
    Ladiratuzumab (hLIV22) is a humanized monoclonal antibody against zinc transporter LIV-1/ZIP6. Ladiratuzumab is conjugated to MMAE (HY-15162) via a cleavable dipeptide linker to synthesize an antibody-drug conjugate (ADC) Ladiratuzumab vedotin (HY-P99683). Ladiratuzumab vedotin selectively targets LIV-1 protein overexpressed on the surface of tumor cells, enters cells through antibody-mediated receptor endocytosis, releases MMAE to inhibit microtubule polymerization, and kills adjacent tumor cells with a bystander effect. Ladiratuzumab can be used in the study of solid tumors such as metastatic triple-negative breast cancer (mTNBC) .
    Ladiratuzumab
  • HY-173522

    Kinesin Cancer
    KIF2C-IN-1 (Compound 7S9) is a selective and potent small-molecule KIF2C inhibitor. KIF2C-IN-1 stabilizes the KIF2C-tubulin interaction, blocking the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel (HY-B0015) in paclitaxel-resistant triple-negative breast cancer (TNBC) cells and significantly reduces tumor growth combined with Paclitaxel in mouse models .
    KIF2C-IN-1
  • HY-112591

    XMH95

    Apoptosis HIV Wnt Bcl-2 Family Cancer
    NSC260594 induces Apoptosis. NSC260594 binds the shallow groove of the Mcl-1 protein, and inhibits Mcl-1 expression through down-regulation of Wnt signaling proteins. NSC260594 can also recognize G9-G10-A11-G12 RNA tetraloop of HIV and prevent the binding of the Gag protein within the 5’-UTR. NSC260594 inhibits tumor growth, and can be used for research of Triple-negative breast cancers (TNBCs) .
    NSC260594
  • HY-175805

    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-178007

    CDK Cancer
    CDK2 degrader 8 (Compound1) is a CDK2 degrader. CDK2 degrader 8 shows potential anti-tumor activity by targeting CDK2. CDK2 degrader 8 can be used for the study of solid tumors (breast cancer, triple negative breast cancer, ovarian serous cystadenocarcinoma) and liquid tumors (diffuse large B-cell lymphoma, acute myelogenous leukemia) associated with abnormal CDK2 function .
    CDK2 degrader 8
  • HY-156077

    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-175604

    PD-1/PD-L1 Cancer
    SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor. SCL-1 can inhibit PD-1/PD-L1 binding. SCL-1 increases T cells, B cells and natural killer cells. SCL-1 exerts strong tumor growth inhibitory effects that were mediated by effector T-cell induction inside tumors and the up-regulated expression of long non-coding RNAs as neoantigens leading to cytotoxic T lymphocyte activation. SCL-1 can be used for the research of cancer, such as triple-negative breast cancer .
    SCL-1
  • HY-174828

    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-175544

    Drug Derivative Cancer
    anti-TNBC agent-10 is an anti-TNBC agent. anti-TNBC agent-10 shows potent anti-TNBC activity against BT549 cells (IC50 = 0.018 μM) and maintains activity against MDA-MB-231 cells (IC50 = 4.16 μM). anti-TNBC agent-10 9 demonstrates significant anti-tumor efficacy in mice bearing subcutaneous MDA-MB-231 TNBC xenografts. anti-TNBC agent-10 can be used for the study of triple-negative breast cancer (TNBC) .
    anti-TNBC agent-10
  • HY-172551

    Apoptosis Cadherin MMP Bcl-2 Family Cancer
    anti-TNBC agent-9 (Compound 3as) is an anti-cancer agent for triple-negative breast cancer (TNBC). anti-TNBC agent-9 exhibits significant inhibitory activity against MDA-MB-453 cells with an IC50 value of 8.5 μM. anti-TNBC agent-9 inhibits tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. anti-TNBC agent-9 induces apoptosis by increasing the expression of the pro-apoptotic protein BAX and decreasing the expression of the anti-apoptotic protein BCL-2, thereby inhibiting tumor cell proliferation .
    anti-TNBC agent-9
  • HY-164789

    SKB264; MK-2870

    Antibody-Drug Conjugates (ADCs) TROP2 Cancer
    Sacituzumab tirumotecan (SKB264/MK-2870) is a TROP2 ADC. The internalization and anti-tumor activity of Sacituzumab tirumotecan are enhanced in tumor cell lines with EGFR mutations. Sacituzumab tirumotecan can be used in the research of triple negative breast cancer (TNBC), non small cell lung cancer (NSCLC) and other cancers .
    Sacituzumab tirumotecan
  • HY-171955

    Lipoxygenase Apoptosis Reactive Oxygen Species (ROS) FAK Cancer
    LXG6403 is an orally active and irreversible LOX inhibitor (IC50 = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin (HY-15142) resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors .
    LXG6403
  • HY-N7694
    Isotoosendanin
    1 Publications Verification

    TGF-β Receptor JAK STAT Apoptosis Inflammation/Immunology Cancer
    Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation .
    Isotoosendanin
  • HY-176561

    Casein Kinase HDAC Cancer
    IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research .
    IOR-160
  • HY-145601

    TT 00420

    Aurora Kinase FGFR VEGFR Cancer
    Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment .
    Tinengotinib
  • HY-150613

    Epigenetic Reader Domain PARP Apoptosis Cancer
    PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
    PARP1/BRD4-IN-2
  • HY-175497

    ROR Apoptosis Bcl-2 Family PARP Cancer
    ROR1-IN-4 is a selective ROR1 inhibitor with a Kd of 52 nM. ROR1-IN-4 shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 75 nM). ROR1-IN-4 reduces colony formation, induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. ROR1-IN-4 demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts. ROR1-IN-4 can be used for the study of triple-negative breast cancer (TNBC) .
    ROR1-IN-4
  • HY-156096

    HDAC Histone Methyltransferase Caspase Apoptosis DNA/RNA Synthesis Cancer
    HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
    HDAC3-IN-2

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