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Catalog No.
Product Name
Application
Product Information
Citations
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DNA/RNA Synthesis Inhibitor
Methotrexate α-tert-butyl ester is an antimetabolite and antifolate compound that acts as a potent inhibitor of DNA and RNA synthesis. It demonstrates significant anti-tumor activity by effectively reducing tumor growth in HT1080 tumor-bearing mouse models. This compound is also utilized for its immunosuppressive and antineoplastic properties in various research applications. -
RNA Polymerase I Transcription Inhibitor
BMH-22 is a selective inhibitor of RNA polymerase I transcription, functioning independently of p53 pathways. This benzonaphthyridin compound induces reorganization of nucleolar marker proteins, indicative of nucleolar segregation, and destabilizes RPA194 through a proteasome-dependent mechanism. Additionally, BMH-22 effectively inhibits the synthesis of nascent rRNA and the expression of the 45S rRNA precursor. Its potent anticancer properties make it a valuable tool for studying cancer biology and RNA transcription regulation in various tumor models. -
RNA Polymerase Inhibitor
MMV688845 is an RNA polymerase inhibitor targeting nontuberculous mycobacteria (NTM) with demonstrated bactericidal activity against Mycobacterium abscessus. This compound exhibits potential anti-tuberculosis efficacy, making it a valuable tool for research in tackling mycobacterial infections. Its selective mechanism positions MMV688845 as a promising candidate for further exploration in antimicrobial studies and drug development. -
NS5B Polymerase/RdRp Inhibitor
Lomibuvir is a selective non-nucleoside inhibitor of the NS5B RNA-dependent RNA polymerase (RdRp) associated with Hepatitis C Virus (HCV). It targets the thumb pocket 2 of the NS5B polymerase with a binding affinity (Kd) of 17 nM and effectively inhibits HCV replication, demonstrated by an EC50 value of 5.2 nM in the 1b/Con1 subgenomic replicon model. Lomibuvir primarily interferes with the elongation phase of RNA synthesis, making it a valuable tool for studying HCV replication mechanisms and developing antiviral therapies. -
RNA Polymerases Inhibitor
3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that serves as an inhibitor of DNA-dependent RNA polymerases I and II. It competitively inhibits the incorporation of UTP into RNA, demonstrating potent biological activity with a Ki value of 2.0 μM. This compound is valuable for research applications involving transcription regulation and the study of RNA synthesis mechanisms. -
DNA Synthesis Inhibitor
Cytarabine triphosphate (Ara-CTP) is a competitive inhibitor of DNA synthesis, serving as an active metabolite of Cytarabine. This compound plays a crucial role in cellular mechanisms by disrupting normal DNA replication processes. Its intracellular levels are valuable for predicting the chemosensitivity of leukemic blasts to Cytarabine, making it a significant biomarker in the treatment of leukemia and related hematological disorders. -
DNA Synthesis Inhibitor
Cytembena is a potent inhibitor of DNA synthesis, primarily targeting replicative DNA processes, purine biosynthesis, and tetrahydrofolate formylase activity. Its biological activity demonstrates significant anti-cancer effects, particularly in the treatment of ovarian and breast cancer, as well as providing pain relief in cases of skeletal metastases. This compound is valuable in research applications focused on cancer therapeutics and the mechanisms of DNA replication and repair. -
Topoisomerase I Inhibitor
Irinotecan-d10 is a deuterated derivative of Irinotecan, a potent inhibitor of topoisomerase I. By binding to the topoisomerase I-DNA complex, it disrupts the religation of DNA strands, thereby inducing DNA damage and apoptosis in rapidly dividing cells. This reagent is useful in cancer research, particularly in studies aimed at understanding the mechanisms of action of topoisomerase inhibitors and their therapeutic potential in oncology. -
Topoisomerase Inhibitor
Amonafide L-malate is a topoisomerase II inhibitor that functions as a DNA intercalator. This compound induces apoptotic signaling by disrupting the interaction between topoisomerase II and DNA, leading to inhibited DNA replication and cell proliferation. Amonafide L-malate is utilized in cancer research to study mechanisms of apoptosis and the effects of topoisomerase inhibition on tumor cells. -
HDAC Inhibitor
HDAC-IN-37 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.0551 μM for HDAC1, 1.24 μM for HDAC3, 0.948 μM for HDAC8, and 34.2 μM for HDAC6. This compound effectively increases histone acetylation through a slow-off binding mechanism. Additionally, HDAC-IN-37 disrupts the transition from the G1 phase to the S phase of the cell cycle and promotes early apoptosis in various cell types, making it a valuable tool for research in cancer biology and therapeutic development. -
c-Met/HDAC Inhibitor
c-Met/HDAC-IN-3 is a dual inhibitor targeting c-Met and histone deacetylase 1 (HDAC1), exhibiting IC50 values of 12.50 nM and 26.97 nM, respectively. This compound demonstrates significant biological activity by inducing apoptosis and causing cell cycle arrest at the G2/M phase. c-Met/HDAC-IN-3 serves as a valuable tool for research in cancer biology and therapeutic development, particularly in studies focused on synergistic inhibition of oncogenic pathways. -
PARP-1/2/TNKS1/2 Inhibitor
PARP1/2/TNKS1/2-IN-1 is an inhibitor targeting PARP-1, PARP-2, TNKS1, and TNKS2, with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM, and 4.15 nM, respectively. This compound demonstrates significant antitumor activity and promotes apoptosis, making it a valuable tool for research focused on cancer biology and therapeutic strategies. Its dual inhibitory action can facilitate the exploration of cellular repair mechanisms and enhance the understanding of poly(ADP-ribose) polymerases in cancer treatment. -
HDAC6 Inhibitor
HDAC6-IN-4 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 23 nM. This compound promotes apoptosis in cancer cells and demonstrates significant antitumor efficacy while exhibiting minimal toxicity. HDAC6-IN-4 is valuable for research in cancer biology, particularly in studies focused on epigenetic regulation and therapeutic development. -
HDAC Inhibitor
HDAC-IN-31 is a selective and orally active histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 84.90 nM for HDAC1, 168.0 nM for HDAC2, 442.7 nM for HDAC3, and greater than 10,000 nM for HDAC8. This compound induces apoptosis and triggers G2/M phase cell cycle arrest, demonstrating significant antitumor efficacy. HDAC-IN-31 is applicable in research focused on diffuse large B-cell lymphoma and other cancer studies. -
Topoisomerase/HDAC Inhibitor
Top/HDAC-IN-1 is a dual inhibitor targeting both topoisomerase and histone deacetylases (HDACs), demonstrating IC50 values of 18 nM for HDAC1, 230 nM for HDAC2, 790 nM for HDAC3, 87 nM for HDAC6, and 5250 nM for HDAC8. This compound exhibits significant antitumor activity against HCT116 cells, with an IC50 of 180 nM, effectively inducing apoptosis and promoting G2 cell cycle arrest. Top/HDAC-IN-1 serves as a valuable tool in cancer research, particularly for studies involving epigenetic modulation and cell proliferation. -
mTOR/HDAC6 Inhibitor
mTOR/HDAC6-IN-1 is a potent dual inhibitor targeting mTOR and HDAC6, exhibiting IC50 values of 133.7 nM and 56 nM, respectively. This compound is known to induce significant autophagy and apoptosis while suppressing cell migration. It holds potential for research applications in triple-negative breast cancer (TNBC) studies, offering insights into the interplay between these critical pathways in cancer progression. -
HDAC Inhibitor
HDAC-IN-59 is a potent inhibitor of histone deacetylases (HDACs), demonstrating significant biological activity in cancer research. This compound promotes the generation of reactive oxygen species (ROS), leading to DNA damage and the induction of apoptosis via the mitochondria-related pathway. Additionally, HDAC-IN-59 effectively disrupts the cell cycle at the G2/M phase, making it a valuable tool for studying the mechanisms of cell growth regulation and apoptosis in various cancer models. -
JAK/HDAC Inhibitor
JAK/HDAC-IN-2 is a dual-target inhibitor of Janus kinase (JAK) and histone deacetylase (HDAC), specifically inhibiting HDAC3/6 and JAK1/2 with nanomolar potency. This compound demonstrates proapoptotic activity by inhibiting histone deacetylation and STAT3 phosphorylation, contributing to its mechanism of action. JAK/HDAC-IN-2 exhibits significant antiproliferative effects in various hematological malignancies and solid tumors, making it a valuable tool for cancer research and therapeutic studies. -
c-Met/HDAC Inhibitor
c-Met/HDAC-IN-2 is a highly potent dual inhibitor targeting c-Met and histone deacetylases (HDACs), exhibiting IC50 values of 18.49 nM for HDAC1 and 5.40 nM for c-Met. This compound demonstrates significant antiproliferative effects against various cancer cell lines, notably inducing G2/M-phase cell cycle arrest and apoptosis in HCT-116 cells. c-Met/HDAC-IN-2 is a valuable tool for investigating mechanisms of anti-cancer resistance and exploring therapeutic strategies in oncology research. -
HDAC inhibitor
HDAC-IN-67 is a potent inhibitor of histone deacetylases HDAC1 and HDAC6, demonstrating IC50 values of 22 nM and 8 nM, respectively. This compound effectively inhibits cell proliferation and induces apoptosis in various cancer cell lines. Its significant antitumor activity makes HDAC-IN-67 a valuable tool for cancer research and a potential candidate for therapeutic development. -
PIM-1/HDAC Inhibitor
PIM-1/HDAC-IN-1 is a selective inhibitor of PIM-1 as well as histone deacetylases HDAC 1 and HDAC 6, exhibiting an IC50 of 343.87 nM for PIM-1 and 63.65 nM and 62.39 nM for HDAC 1 and HDAC 6, respectively. This compound demonstrates significant apoptotic activity in MCF-7 cell lines, inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase. PIM-1/HDAC-IN-1 is a valuable tool for research on cancer biology and the regulation of cell proliferation and apoptosis. -
FGFR/HDAC Inhibitor
HDAC-IN-50 is a potent dual inhibitor targeting FGFR and HDAC with IC50 values of 0.18 nM for FGFR1, 1.2 nM for FGFR2, 0.46 nM for FGFR3, 1.4 nM for FGFR4, and varying inhibitory effects on HDAC isoforms such as HDAC1 (1.3 nM), HDAC2 (1.6 nM), HDAC6 (2.6 nM), and HDAC8 (13 nM). This compound effectively induces apoptosis and causes cell cycle arrest at the G0/G1 phase. Additionally, HDAC-IN-50 decreases the expression of phosphorylated forms of FGFR1, ERK, and STAT3, indicating its potential applications in cancer research and therapy. -
VEGFR/PARP Inhibitor
VEGFR/PARP-IN-1 is a dual inhibitor targeting Vascular Endothelial Growth Factor Receptor (VEGFR) and Poly(ADP-ribose) Polymerase (PARP), with IC50 values of 191 nM and 60.9 nM, respectively. This compound inhibits DNA damage repair mechanisms, induces apoptosis, and causes G2/M phase cell cycle arrest. It demonstrates significant antiproliferative activity against BRCA wild-type breast cancer cell lines, specifically MDA-MB-231 and MCF-7, with IC50 values of 4.1 μM and 3.5 μM, respectively. VEGFR/PARP-IN-1 is an effective antitumor and anti-metastatic agent, making it valuable for cancer research applications. -
Tubulin/HDAC Inhibitor
Tubulin/HDAC-IN-1 is a dual inhibitor targeting tubulin and histone deacetylase 8 (HDAC8) through CH/π interaction and hydrogen bonding, respectively. This compound effectively inhibits tubulin polymerization and selectively inhibits HDAC8 with an IC50 value of 150 nM. Tubulin/HDAC-IN-1 demonstrates cytotoxic effects against a range of human cancer cell lines, induces cell cycle arrest in the G2/M phase, and promotes apoptosis. It is a valuable reagent for research involving hematologic malignancies and solid tumors, including neuroblastoma and leukemia. -
HDAC6 Inhibitor
SAHA-OH is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 23 nM, demonstrating a 10- to 47-fold selectivity over HDAC isoforms 1, 2, 3, and 8. This compound exhibits notable anti-inflammatory properties and has been shown to reduce macrophage apoptosis. It is a valuable tool for research focused on the modulation of histone acetylation and the investigation of HDAC6's role in various inflammatory pathways. -
VEGFR-2/HDAC Dual Inhibitor
VEGFR2/HDAC1-IN-1 is a potent dual inhibitor of VEGFR-2 and HDAC, demonstrating IC50 values of 57.83 nM and 9.82 nM, respectively. This compound effectively arrests the cell cycle at the S and G2 phases, leading to apoptosis in HeLa cells. Additionally, VEGFR2/HDAC1-IN-1 exhibits significant anti-angiogenic properties, making it a valuable tool for research in cancer biology and targeted therapies. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 7 is a selective inhibitor of the topoisomerase II alpha subtype, demonstrating an IC50 of 3.19 μM. This compound is capable of inducing cell cycle arrest and apoptosis, making it a valuable tool for research into cancer biology and therapeutic strategies. Its inhibition of topoisomerase II has potential applications in exploring mechanisms of genomic stability and drug resistance in cancer cells. -
HDAC Inhibitor
HDAC-IN-34 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.022 μM for HDAC1 and 0.45 μM for HDAC6. This compound binds to DNA, leading to DNA damage and inducing apoptosis through the p53 signaling pathway. Additionally, HDAC-IN-34 exhibits significant anti-proliferative effects against HCT-116 colorectal cancer cells, with an IC50 of 1.41 μM, making it a valuable tool for cancer research and epigenetic studies. -
TOPOI/PARP Dual Inhibitor
TOPOI/PARP-1-IN-1 is a dual inhibitor targeting topoisomerase I and PARP-1, demonstrating an IC50 value of 0.09 μM for PARP-1. This compound exhibits significant anti-proliferative and anti-migratory effects on cancer cells, leading to G0/G1 phase cell cycle arrest and apoptosis. In preclinical studies, TOPOI/PARP-1-IN-1 achieved a tumor growth inhibition rate of 75.4% in mice, highlighting its potential for cancer therapy research applications. -
SIRT6 Inhibitor
SIRT6-IN-4 is a selective inhibitor of SIRT6, demonstrating an IC50 of 5.68 μM. This compound effectively inhibits the proliferation of MCF-7 cells with an IC50 of 8.30 μM, leading to cell cycle arrest at the G2/M phase. Additionally, SIRT6-IN-4 reduces cell migration and invasion while inducing apoptosis. Its antitumor efficacy has been confirmed in mouse models, making it a valuable tool for cancer research and therapeutic development. -
PARP/NAMPT Inhibitor
PARP1/NAMPT-IN-2 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 0.8 nM and 18 nM, respectively. This compound effectively inhibits cell proliferation and migration, while inducing apoptosis in breast cancer cells. PARP1/NAMPT-IN-2 is particularly relevant for investigating therapeutic strategies in triple-negative breast cancer research. -
Topoisomerase I Inhibitor
Topoisomerase I inhibitor 3 is a potent inhibitor that targets topoisomerase I, interfering with the topoisomerase I-DNA complex. This compound demonstrates significant biological activity by inducing apoptosis in HepG2 cancer cells and causing cell cycle arrest at the G2/M phase. It serves as a valuable tool for research applications related to cancer biology and therapeutic development. -
PARP1/2/CDK12 Inhibitor
PARP-1/2-IN-2 is a potent inhibitor of PARP1, PARP2, and CDK12, exhibiting IC50 values of 34 nM, 30 nM, and 285 nM, respectively. This compound disrupts DNA damage repair mechanisms, leading to induced cell cycle arrest and apoptosis. Notable for its efficacy in targeted therapy, PARP-1/2-IN-2 effectively inhibits the growth of triple-negative breast cancer (TNBC) cells and demonstrates significant antitumor activity in TNBC xenograft models. This makes it a valuable tool for research in cancer biology and therapeutic development. -
HDAC/PSMD14 Inhibitor
HDAC/PSMD14-IN-1 is a dual-target inhibitor of HDAC1 and PSMD14, exhibiting IC50 values of 238.7 nM and 141.2 nM, respectively. This compound demonstrates significant cytotoxicity against esophageal squamous cell carcinoma (ESCC) cell lines, with IC50 values ranging from 30 to 250 nM. In addition to its ability to induce apoptosis, HDAC/PSMD14-IN-1 effectively reverses epithelial-mesenchymal transition (EMT) and shows promising anti-tumor activity in KYSE30 mouse xenograft models. It is a valuable tool for advancing research in esophageal cancer. -
HDAC Inhibitor
1-Alaninechlamydocin is a cyclic tetrapeptide that functions as a potent histone deacetylase (HDAC) inhibitor with an IC50 of 6.4 nM. This compound effectively induces G2/M cell cycle arrest and promotes apoptosis in MIA PaCa-2 cells, making it a valuable tool for cancer research. Its activity in modulating epigenetic regulation highlights its potential applications in therapeutic development and studies of cellular differentiation and survival. -
HDAC Class I Inhibitor
HDAC-IN-27 is a selective inhibitor of Class I histone deacetylases (HDAC1-3) with an IC50 range of 0.43 to 3.01 nM. It demonstrates significant anti-proliferative and pro-apoptotic effects against acute myeloid leukemia (AML) cell lines by promoting histone acetylation, specifically AcHH3 and AcHH4. This compound is valuable for research into the mechanisms of AML and potential therapeutic applications in histone modification regulation. -
HDAC6 Inhibitor
Daphnegiravone D is an inhibitor of HDAC6, targeting histone deacetylation to modulate gene expression. This compound demonstrates significant anti-hepatocellular carcinoma activity by inducing apoptosis and selectively inhibiting the proliferation of liver cancer cells. Its mechanism involves the p38 and JNK MAPK signaling pathways, making it a valuable tool for research in cancer therapeutics and cellular signaling. -
HDAC1/6 Inhibitor
HDAC1/6-IN-1 is a potent inhibitor targeting HDAC1 and HDAC6, exhibiting IC50 values of 1.3 nM and 13 nM, respectively. This compound effectively inhibits the methylation and deacetylation of H3K9, leading to significant biological activity, including the induction of apoptosis in cancer cells, G0/G1 cell cycle arrest, and the inhibition of cell migration and invasion. It serves as a valuable tool in cancer research and the study of epigenetic regulation. -
Topoisomerase I/III Inhibitor
Topoisomerase I/II inhibitor 3 is a dual inhibitor targeting both topoisomerase I and II. This compound exhibits potent anti-proliferative effects, inhibiting cell proliferation, invasion, and migration, while also inducing apoptosis through the PI3K/Akt/mTOR signaling pathway. It is particularly relevant for research applications in liver cancer studies. -
Topoisomerase Inhibitor
Topoisomerase Inhibitor 4 is a potent inhibitor targeting topoisomerase I and II. This compound effectively induces cell cycle arrest in the G2/M phase, leading to apoptosis in various cancer cell lines. Its significant antitumor activity makes it a valuable reagent for cancer research applications focused on exploring mechanisms of cell cycle regulation and apoptosis. -
Dual TOP1/PARP1 Inhibitor
DiPT-4 is a dual inhibitor of topoisomerase I (TOP1) and poly (ADP-ribose) polymerase 1 (PARP1). This compound induces substantial DNA double-strand breaks, leading to cell cycle arrest and apoptosis in various cancer cell lines. DiPT-4 is particularly valuable for research focused on overcoming mechanisms of cancer drug resistance. -
PARP Inhibitor
Schisandronic acid is a potent PARP inhibitor derived from the triterpenoid compound found in Schisandra chinensis. This compound exhibits significant cytotoxicity against human breast cancer cells, particularly MCF-7, with an IC50 value of 8.06 μM. Schisandronic acid effectively induces apoptosis through the upregulation of active caspase-3 and cleavage of PARP, while also reducing reactive oxygen species generation, thereby demonstrating notable antioxidant properties. Its mechanisms of action make Schisandronic acid a valuable tool for cancer research and therapeutic investigations. -
Topoisomerase II Inhibitor
Topoisomerase IIα-IN-5 is an inhibitor of topoisomerase IIα, effectively interfering with its catalytic activity. It operates by intercalating into DNA and binding to the minor groove, thereby inhibiting the enzyme's function. This compound demonstrates enhanced efficacy and reduced genotoxicity compared to Etoposide, making it a valuable tool for research applications focused on cancer therapy and DNA topology modulation. -
eIF4A Inhibitor
MG-002 is a selective eIF4A inhibitor that interferes with the recruitment and scanning of ribosomes by non-productively trapping the eukaryotic translation initiation factor 4A (eIF4A) onto RNA. This action effectively inhibits mRNA translation, leading to reduced growth and metastasis of triple-negative breast cancer (TNBC) tumors, as well as inducing apoptosis in cancer cells. Additionally, MG-002 significantly downregulates the protein expression of c-MYC and cyclin D1, making it a valuable tool for research applications focused on TNBC and other related malignancies. -
SIRT2 Inhibitor
SIRT2-IN-18 is a selective SIRT2 inhibitor, exhibiting IC50 values of 5.3 μM for SmSIRT2 and 12.3 μM for hSIRT2. This compound demonstrates significant antischistosomal effects against both Liberian and Puerto Rican strains of Schistosoma mansoni, effectively reducing schistosomula viability, adult worm pairing, and egg production while maintaining low cytotoxicity in mammalian cells. SIRT2-IN-18 also promotes histone H3 hyperacetylation and triggers cytochrome c-mediated apoptosis, making it a valuable tool for research into both parasitic infections and the modulation of acetylation pathways. -
HDAC Inhibitor
HDAC-IN-39 is a potent inhibitor of histone deacetylases (HDACs), exhibiting IC50 values of 1.07 μM for HDAC1, 1.47 μM for HDAC2, and 2.27 μM for HDAC3. This compound also significantly disrupts microtubule polymerization and induces cell cycle arrest at the G2/M phase, highlighting its potential for modulating cell cycle dynamics. Furthermore, HDAC-IN-39 demonstrates promising anticancer activity, particularly against resistant cancer cell lines, making it a valuable tool for cancer research and therapeutic exploration. -
Topoisomerase/HDAC Inhibitor
Top/HDAC-IN-3 is an orally active dual inhibitor targeting topoisomerase and histone deacetylase (HDAC). This compound enhances intracellular levels of reactive oxygen species (ROS), leading to DNA damage and subsequently inhibiting cancer cell colony formation and migration. Additionally, Top/HDAC-IN-3 induces apoptosis and cell cycle arrest in cancer cells. In non-small cell lung cancer (NSCLC) models, it demonstrates significant antitumor activity, achieving a tumor growth inhibition (TGI) of 77.5% at a dosage of 100 mg/kg. -
PARP1/BRD4 Inhibitor
PARP1/BRD4-IN-1 is a selective inhibitor targeting both PARP1 and BRD4, demonstrating IC50 values of 49 nM and 202 nM, respectively. This compound effectively represses the expression and activity of these proteins, leading to synergistic inhibition of malignant pancreatic cancer cell growth. PARP1/BRD4-IN-1 is a valuable tool for exploring therapeutic strategies in cancer research, particularly in the context of PARP and BRD4 signaling pathways. -
Topoisomerase I/II Inhibitor
Topoisomerase I/II Inhibitor 4 is a potent dual inhibitor targeting both topoisomerase I and II. This compound exhibits significant anti-proliferative effects, inhibiting cell growth, invasion, and migration while promoting apoptosis in cancer cells. Its primary research applications include studies focused on liver cancer therapeutics and the exploration of topoisomerase-related mechanisms in cellular processes. -
HDAC6 Inhibitor
TNI-97 is a highly selective and orally active inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 0.2 nM. This compound effectively suppresses the growth and clonogenicity of triple-negative breast cancer (TNBC) cells, specifically MDA-MB-453. TNI-97 induces PANoptosis, encompassing apoptosis, necroptosis, and pyroptosis in these cells. Additionally, TNI-97 demonstrates significant antitumor activity in mouse models, including xenografts and allografts of TNBC, making it a valuable tool for research focused on triple-negative breast cancer.
