Search Result
Results for "
In vivo tumor model
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-134813
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Ras
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Cancer
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MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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- HY-158101
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CC-94676
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PROTACs
Androgen Receptor
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Cancer
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BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC) .
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- HY-164388
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Caspase
Apoptosis
Autophagy
Necroptosis
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Cardiovascular Disease
Cancer
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Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
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- HY-157228
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PROTACs
Ras
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Cancer
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ACBI3 (compound 7), a chemical probe, is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
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- HY-147214
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YAP
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Cancer
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GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
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- HY-164992
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MRG002; Trastuzumab MMAE
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Antibody-Drug Conjugates (ADCs)
EGFR
Microtubule/Tubulin
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Cancer
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Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
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- HY-145799
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5A2-SC8
1 Publications Verification
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Liposome
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Cancer
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5A2-SC8 is an ionizable amino lipid in lipid nanoparticles (LNPs) that shows high delivery potential and low in vivo toxicity, enabling efficient delivery of small RNAs such as siRNA and miRNA into tumor cells. 5A2-SC8 LNPs can confer a unique delivery fate of RNA within the liver, thereby changing the therapeutic outcomes in cancer models .
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- HY-17444
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PPAR
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Metabolic Disease
Cancer
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Tesaglitazar is a dual-target PPARα/γ agonist with an EC50 of 13.4 μM for rat PPARα and 3.6 μM for human PPARα. Tesaglitazar affects lipid and glucose metabolism by activating PPARα and PPARγ receptors, and has the potential to improve blood sugar and relieve pain. Tesaglitazar can be used to induce in vivo tumor models and can be used in the study of type 2 diabetes, dyslipidemia, and neuropathic pain .
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- HY-104048
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Histone Demethylase
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Cancer
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QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
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- HY-150105
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BMF-219; MenIn-MLL Inhibitor 21
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Epigenetic Reader Domain
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Metabolic Disease
Inflammation/Immunology
Cancer
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Icovamenib (BMF-219) is a selective, orally active, irreversible Menin inhibitor. Icovamenib forms a stable and irreversible covalent bond with Menin. Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures. Icovamenib enhances glycemic control in animal diabetic models. Icovamenib induces a dose-dependent enhancement in insulin secretion potentiated by the GLP-1 RA. Icovamenib can be used for the study of multiple hematologic malignancies, solid tumors, and diabetes mellitus, such as diffuse large B-cell lymphoma (DLBCL), multiple myeloma (MM) and chronic lymphocytic leukemia and type 2 diabetes .
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- HY-148813
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AK-2292
2 Publications Verification
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PROTACs
STAT
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Cancer
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AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-W088065
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Environmental Pollutants
DNA/RNA Synthesis
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Others
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Sodium formate acts as a key promoter for heterogeneous nucleation of ZIF crystals and thin film synthesis. It is also recognized as a GRAS substance by the FDA, and serves as a cosmetic preservative and food additive. Sodium formate has low acute oral toxicity (acute oral LD50=7410 mg/kg and acute intravenous LD50=807 mg/kg in mice), with no heritable or carcinogenic effects, but exhibits embryonic developmental toxicity and teratogenicity at high concentrations. Sodium formate may cause moderate irritation to rabbit eyes, is relatively safe to the skin, and does not induce tumor formation in rats in vivo. Sodium formate is rapidly absorbed and oxidized to carbon dioxide in vivo, and forms DNA adducts in specific metabolic deficiency models or upon high-dose exposure .
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- HY-100685
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MS-444
2 Publications Verification
BE-34776
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HuR
Apoptosis
COX
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Neurological Disease
Cancer
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MS-444 (BE-34776) is a HuR (ELAVL1) inhibitor that blocks the cytoplasmic translocation of HuR and inhibits its dimerization. MS-444 reduces cytoplasmic HuR levels by preventing the binding of HuR to ARE-mRNA, without altering the total expression of HuR. MS-444 induces apoptosis, inhibits cell growth, angiogenesis and invasion, and also regulates immune function and microbiota. MS-444 effectively alters the number, size and invasiveness of tumors in various cancer models. MS-444 is tolerable to intraperitoneal injection in vivo and can be applied to research related to colorectal cancer, familial adenomatous polyposis, colitis-associated cancer and glioblastoma .
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- HY-N0538
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Xylite
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Environmental Pollutants
Endogenous Metabolite
Bacterial
Autophagy
Atg7
Atg8/LC3
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Metabolic Disease
Cancer
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Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
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- HY-13241A
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LY2228820
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p38 MAPK
Autophagy
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Cancer
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Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma .
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- HY-P991577
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DS-8895A
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Ephrin Receptor
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Cancer
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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. .
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- HY-12842
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IAP
Survivin
Apoptosis
Caspase
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Inflammation/Immunology
Cancer
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UC-112 is a XIAP inhibitor with anticancer activity. UC-112 selectively downregulates and degrades survivin via the ubiquitin-mediated proteasomal degradation pathway. UC-112 reduces XIAP levels in in vivo tumor models. UC-112 activates caspase-3/7 and caspase-9, and induces cancer cell apoptosis. UC-112 is applicable to studies on melanoma, prostate cancer and cancer-related research .
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- HY-115630
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RIP kinase
Caspase
Apoptosis
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Cancer
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cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models .
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- HY-148409
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Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
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Cancer
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MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
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- HY-160698
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MALT1
Apoptosis
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Cancer
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SGR-1505 is an oral small molecule MALT1 inhibitor with anti-proliferative and antitumor activity.SGR-1505 inhibits MALT1 enzymatic activity to modulate NF-κB pathway gene expression.SGR-1505 induces modulation of cell cycle, DNA damage, and apoptosis-related genes in in vivo tumor samples.SGR-1505 exerts tumorostatic and regressive activity in ABC-DLBCL xenograft models.SGR-1505 can be used for the research of activated B cell-like diffuse large B cell lymphoma, non-Hodgkin B-cell lymphomas, chronic lymphocytic leukemia, and mature B cell neoplasms .
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- HY-P99852
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ABT165; PR1283233
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VEGFR
Notch
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Cancer
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Dilpacimab (ABT165) is a bispecific variable domain immunoglobulin. Dilpacimab binds to and inhibits DLL4 and VEGF and acts as a tumor growth inhibitor. Dilpacimab can be used in research related to metastatic colorectal cancer and advanced solid tumors .
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- HY-156111
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PROTACs
Androgen Receptor
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Cancer
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ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
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- HY-122607
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Mitochondrial Metabolism
TSPO
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Inflammation/Immunology
Cancer
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DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model .
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- HY-P99925
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REGN421
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Notch
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Metabolic Disease
Cancer
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Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
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- HY-147008
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Epigenetic Reader Domain
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Cancer
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XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC) .
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- HY-P991336
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InBRX-106; ES-102
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Orexin Receptor (OX Receptor)
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Inflammation/Immunology
Cancer
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Ordastobart (INBRX-106; ES-102) is a hexavalent OX40 agonist antibody. Ordastobart enhances OX40 receptor clustering, signaling, and downstream activation, thereby increasing the proliferation and activation of CD4 + and CD8 + T cells in vitro and in vivo. Ordastobart exhibits anti-tumor effects and improves survival in mouse models of cancer. Ordastobart is indicated for research in cancers such as fibrosarcoma and colorectal cancer .
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- HY-W181530
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Molecular Glues
CDK
Apoptosis
Ligands for E3 Ligase
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Cancer
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NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models .
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- HY-P1380A
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Apoptosis
Bcl-2 Family
Caspase
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Cancer
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Difopein TFA is a 14-3-3 protein inhibitor. Difopein TFA acts as an apoptosis inducer, regulates apoptosis-related proteins, downregulates Bcl-2, upregulates Bax, activates caspase-9 and caspase-3, and induces nuclear fragmentation, membrane-enclosed apoptotic bodies and DNA ladder formation. Difopein TFA serves as a tumor growth inhibitor, which inhibits the proliferation of glioma cells and induces their apoptosis in in vivo nude mouse models. Difopein TFA is applicable to glioma-related research .
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- HY-132192
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model .
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- HY-W142432
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Biochemical Assay Reagents
β-catenin
Wnt
Arginase
TGF-beta/Smad
mTOR
Akt
ERK
Atg8/LC3
p62
Autophagy
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Metabolic Disease
Inflammation/Immunology
Cancer
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Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation .
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- HY-112411
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EGFR
ERK
PDGFR
FGFR
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Neurological Disease
Inflammation/Immunology
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PD 174265 is a highly selective, reversible EGFR/ErbB2 tyrosine kinase inhibitor (IC50=0.45 nM) and cell differentiation inducer. By blocking receptor autophosphorylation and the downstream ERK signaling pathway (with an IC50 of 0.45 μM for full-length ERK), PD 174265 effectively inhibits tumor growth and exhibits antitumor activity without obvious toxicity in in vivo models. PD 174265 drives oligodendrocyte precursor cells to switch from a proliferative state to a differentiated state, significantly upregulates the expression of myelin proteins such as CNP, PLP and MBP, and induces neurite branching. PD 174265 shows no inhibitory effect on other kinases including insulin, PDGF and basic FGF receptors, and serves as a crucial tool molecule for investigating the treatment of human epidermoid carcinoma and the mechanism of myelin repair in multiple sclerosis .
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- HY-148274
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PROTACs
IRAK
Apoptosis
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Cancer
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KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88 MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model .
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- HY-156096
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HDAC
Histone Methyltransferase
Caspase
Apoptosis
DNA/RNA Synthesis
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Cancer
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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 .
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- HY-D2062
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Fluorescent Dye
Integrin
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Cancer
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ATTO 740 NHS ester is a near-infrared fluorescent dye and a multimodal fluorescence/photoacoustic contrast agent with excellent near-infrared emission properties and extremely high photostability. The photoacoustic signal of ATTO 740 NHS ester shows no significant decrease after continuous irradiation with a 750 nm laser for 30 min, making it suitable for in vivo fluorescence imaging and photoacoustic contrast imaging. When conjugated with the cystine knot peptide R01, ATTO 740 NHS ester enables precise detection of integrin αvβ6-positive cells and tumors in nude mouse xenograft models .
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- HY-115514A
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BRK
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Cancer
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BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models .
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- HY-165245
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Transmembrane Glycoprotein
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Cancer
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SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
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- HY-P990947
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AZD9592 Antibody
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ADC Antibody
EGFR
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Cancer
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Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .
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- HY-118899
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Endogenous Metabolite
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Cancer
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XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
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- HY-147696
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HSP
AMPK
Reactive Oxygen Species (ROS)
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Cancer
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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 .
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- HY-150023
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EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
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Cancer
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BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
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- HY-145799A
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Liposome
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Cancer
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5A2-SC8 TFA is an ionizable amino lipid in lipid nanoparticles (LNPs) that shows high delivery potential and low in vivo toxicity, enabling efficient delivery of small RNAs such as siRNA and miRNA into tumor cells. 5A2-SC8 TFA LNPs can confer a unique delivery fate of RNA within the liver, thereby changing the therapeutic outcomes in cancer models .
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- HY-106219
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Microtubule/Tubulin
P-glycoprotein
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Cancer
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BMS 275183 is a potent, orally active analogue of Paclitaxel (HY-B0015). BMS 275183 can stabilize microtubules and exhibits antitumor activity in in vivo tumor models. BMS 275183 is active in vitro against Paclitaxel-resistant tumors including those harboring tubulin mutations or overexpressing P-glycoprotein. BMS 275183 can be used for cancer research, such as non-small cell lung cancer (NSCLC) and prostate carcinoma .
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- HY-132192A
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model .
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- HY-116861
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MetAP
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Cancer
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A-357300 is a reversible and selective MetAP2 inhibitor with IC50s of 0.12 and 57 μM against MetAP2 and MetAP1. A-357300 induces cytostasis by cell cycle arrest at the G1 phase selectively in endothelial cells and in a subset of tumor cells. A-357300 inhibits angiogenesis both in vitro and in vivo and shows potent antitumor efficacy in carcinoma, sarcoma, and neuroblastoma murine models. A-357300 can be used for the studies of neuroblastoma, fibrosarcoma and breast cancer .
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- HY-P990778
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ATG-101
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TNF Receptor
PD-1/PD-L1
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Inflammation/Immunology
Cancer
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Xirestomig (ATG-101) is a tetravalent "2+2″ PD-L1×4-1BB bispecific antibody. Xirestomig binds PD-L1 and 4-1BB concurrently, with a greater affinity for PD-L1, and potently activated 4-1BB+ T cells when cross-linked with PD-L1-positive cells. Xirestomig activates exhausted T cells upon PD-L1 binding. Xirestomig displays potent antitumor activity in numerous in vivo tumor models, including those resistant or refractory to immune checkpoint inhibitors (ICIs) .
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- HY-179180
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-59 (Compound MZ51) is a PD-1/PD-L1 inhibitor with an IC50 of 183 nM. PD-1/PD-L1-IN-59 can be used for the study of triple-negative breast cancer (TNBC) .
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-
-
- HY-135217
-
|
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Apoptosis
|
Cancer
|
|
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
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-
-
- HY-P5520
-
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|
Bombesin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
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-
-
- HY-162010
-
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|
Methionine Adenosyltransferase (MAT)
|
Cancer
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|
MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile. MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors research .
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-
-
- HY-N12044
-
|
|
Apoptosis
|
Cancer
|
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
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-
- HY-169937
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .
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-
- HY-156792
-
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|
RIO Kinase
|
Cancer
|
|
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
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-
- HY-175041
-
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|
Glutathione Peroxidase
Reactive Oxygen Species (ROS)
Cannabinoid Receptor
Ferroptosis
|
Cancer
|
|
GPX4-IN-18 (Compound 17) is a ferrocene-containing inhibitor of glutathione peroxidase 4 (GPX4). GPX4-IN-18 is also an inducer of ferroptosis. GPX4-IN-18 can increase the production of ROS and malondialdehyde (MDA) levels in OS-RC-2 clear cell renal cell carcinoma cells. GPX4-IN-18 induces ferroptosis in HT-1080 cells with IC50s of 0.007 μM (absence of ferrostatin-1) and 1.486 μM (presence of ferrostatin-1). GPX4-IN-18 reduces in vivo tumor volume and intratumoral GPX4 levels in OS-RC-2 xenograft murine model .
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-
- HY-118269
-
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|
c-Met/HGFR
|
Cancer
|
|
OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .
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-
- HY-N10447
-
|
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Apoptosis
|
Cancer
|
|
Kurzipene D (compound 4) is a potent anticancer agent. Kurzipene D induces the apoptosis and arrested the HepG2 cell cycle at S stage. Kurzipene D shows anti-tumor effects using in vivo zebrafish model. Kurzipene D has the property of inhibiting tumor proliferation and migration .
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-
- HY-143586
-
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CDK
|
Cancer
|
|
CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models .
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-
- HY-135217R
-
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Apoptosis
Reference Standards
|
Cancer
|
|
Apiole (Standard) is the analytical standard of Apiole. This product is intended for research and analytical applications. Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
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-
- HY-172453
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
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|
XW-032 is an apo-IDO1 inhibitor, with an IC50 of 21 nM. XW-032 (TGI = 63%) exhibits potent in vivo anti-tumor efficacy in the CT26 syngeneic mouse model and is expected to be applied in the research of the field of cancer .
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-
- HY-17658
-
|
|
Apoptosis
|
Cancer
|
|
Apiol analog-1 (Compound 2b) is an analog of Apiol (HY-135217). Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
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-
- HY-12965B
-
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TAM Receptor
|
Cancer
|
|
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
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-
- HY-143585
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-14 is a potent and selective CDK9 inhibitor with IC50 of 6.92 nM. CDK9-IN-14 has a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and has a good selectivity and a low toxicity and few side effects .
|
-
- HY-156085
-
|
|
PD-1/PD-L1
|
Cancer
|
|
LP23 is a non-arylmethylamine PD-1/PD-L1 inhibitor (IC50: 16.7 nM) with anti-tumor activity. LP23 restores immune cell function in HepG2/Jurkat T cells and promotes HepG2 cell death. LP23 is active in vivo in the B16-F10 tumor model (TGI=88.6% at 30 mg/kg) .
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-
- HY-155458
-
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PARP
|
Inflammation/Immunology
Cancer
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|
HYDAMTIQ is a PARP-1/2 inhibitor (IC50: 29-38 nM) with anticancer, anti-inflammatory, and ischemic protective effects. HYDAMTIQ inhibits pulmonary PARP activity, is effective against allergen-induced cough and dyspnea, and inhibits bronchial hyperresponsiveness to methacholine. HYDAMTIQ has broad-spectrum tumor suppressor effects, including ovarian and breast cancers, prostate and pancreatic tumors, and glioblastoma multiforme. HYDAMTIQ has demonstrated in vivo efficacy in animal models of cerebral ischemia, asthma, cancer, and more .
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-
- HY-111251
-
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Microtubule/Tubulin
Apoptosis
|
Cancer
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|
4SC-207 is a potent, orally active microtubule inhibitor. 4SC-207 inhibits microtubule growth to inhibit tumor cell proliferation in vitro and in vivo, and promotes a mitotic delay/arrest, followed by apoptosis or aberrant divisions. 4SC-207 inhibits tumor growth in taxane resistant xenograft mouse models. 4SC-207 can be used for cancer research, such as colon adenocarcinoma and other malignancies .
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-
- HY-122607R
-
|
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Mitochondrial Metabolism
|
Inflammation/Immunology
Cancer
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|
DPA-714 (Standard) is the analytical standard of DPA-714. This product is intended for research and analytical applications. DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model .
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-
- HY-170936
-
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FAK
Hippo (MST)
YAP
|
Cancer
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|
MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
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-
- HY-116504
-
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EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
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-
- HY-172175
-
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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 .
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-
- HY-159577
-
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PI3K
mTOR
Akt
|
Cancer
|
|
Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
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-
- HY-123237
-
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c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
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-
- HY-170919
-
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|
FGFR
|
Cancer
|
|
FGFR2/3-IN-2 (compound 10) is an orally active FGFR2 and FGFR3 inhibitor. FGFR2/3-IN-2 inhibits FGFR2 and FGFR3 with IC50s of 3.7 nM and 31.2 nM (preincubation time 1 h), respectively. FGFR2/3-IN-2 spares FGFR1/4 and other kinases without causing diarrhea and serum phosphate elevation in vivo. FGFR2/3-IN-2 induces tumor stasis or regression in the SNU-16 gastric cancer model .
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-
- HY-174324
-
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VEGFR
P-glycoprotein
Apoptosis
|
Cancer
|
|
VEGFR-2/P-gp-IN-1, a Licochalcone A (HY-N0372) derivative, is an orally active VEGFR-2 (IC50 = 0.885 μM) and P-gp inhibitor. VEGFR-2/P-gp-IN-1 achieves anti-tumor proliferation and overcomes chemotherapy resistance by synchronously inhibiting VEGFR-2 kinase activity and P-gp drug efflux pump function. VEGFR-2/P-gp-IN-1 inhibits phosphorylation of VEGFR-2 and downstream PI3K/AKT signaling pathway proteins, induces apoptosis, blocks cells in the S phase, and inhibits invasive migration. VEGFR-2/P-gp-IN-1 exerts potent in vivo anti-tumor effects in the HeLa/DDP cell xenograft tumor model. VEGFR-2/P-gp-IN-1 is used in cervical cancer research.
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-
- HY-137936
-
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Antibiotic
|
Infection
|
|
Terrecyclic acid is a sesquiterpene originally isolated from A. terreus with antibiotic and anticancer activity. It is active against S. aureus, B. subtilis, and M. roseus (MICs=25, 50, and 25 μg/mL, respectively). Terrecyclic acid induces a heat shock response, increases levels of reactive oxygen species (ROS), and inhibits NF-κB activity and cell growth in 3T3-Y9-B12 cells.2 In vivo, terrecyclic acid (0.1, 1, and 10 mg/ml) reduces the number of ascitic fluid tumor cells in a mouse model of P388 murine leukemia.
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-
- HY-164490
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
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-
- HY-122566
-
|
ZInC666243
|
Toll-like Receptor (TLR)
TNF Receptor
|
Cancer
|
|
SMU127 is an agonist of the toll-like receptor 1/2 (TLR1/2) heterodimer. It induces NF-κB signaling in cells expressing human TLR2 (EC50=0.55 μM) but not cells expressing human TLR3, -4, -5, -7, or -8 when used at concentrations ranging from 0.1 to 100 μM. SMU127 induces the production of TNF-α in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 0.01 to 1 μM. In vivo, SMU127 (0.1 mg/animal) reduces tumor volume in a 4T1 murine mammary carcinoma model.
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-
- HY-158156
-
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|
NF-κB
Apoptosis
|
Cancer
|
|
NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models .
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-
- HY-168715
-
|
|
SHP2
Apoptosis
MAPKAPK2 (MK2)
|
Cancer
|
|
SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC50 of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC50 of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2 .
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-
- HY-119618
-
|
|
Endogenous Metabolite
|
Cancer
|
|
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
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-
- HY-120482
-
|
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Microtubule/Tubulin
|
Others
|
|
CHM-1-P-Na is a sodium monophosphate salt of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one, which can be converted into CHM-1, a compound with a unique anti-tumor mechanism, in vitro and in vivo, and has excellent anti-tumor activity in tumor models and clear pharmacological effects on related enzymes.
|
-
- HY-165375
-
|
|
Others
|
Cancer
|
|
Plenolin is an anticancer agent. Plenolin exhibits inhibitory activity against human epidermoid carcinoma cells. Plenolin shows in vivo antitumor activity against ascites carcinosarcoma and lymphocytic leukemia in rodent models. Plenolin can be used for research related to ascites tumors and leukemia .
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-
- HY-122607S
-
|
|
Isotope-Labeled Compounds
Mitochondrial Metabolism
TSPO
|
Inflammation/Immunology
Cancer
|
|
DPA-714-d10 is the deuterium labeled DPA-714 (HY-122607). DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.
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-
- HY-183610
-
|
|
DNA/RNA Synthesis
PAK
|
Cancer
|
|
WRN-IN-26 is an orally active Werner syndrome helicase (WRN) inhibitor with a human Ki value of 58.7 μM and an IC50 value of 0.026 μM. WRN-IN-26 selectively targets the cysteine residues of WRN. WRN-IN-26 induces the expression of p21 protein in MSI-H tumor cells. WRN-IN-26 inhibits the growth of MSI-H tumor cells and exhibits potent in vivo efficacy in MSI-H xenograft tumor models. WRN-IN-26 can be used for the research of microsatellite instability-high (MSI-H) cancers .
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-
- HY-183253
-
|
|
Drug-Linker Conjugates for ADC
Eukaryotic Initiation Factor (eIF)
EGFR
|
Cancer
|
|
DL149 is a component of an antibody-drug conjugate (ADC) formed by conjugating the eIF4A inhibitor FD236 (HY-186186) with an ADC linker, and exhibits potential antitumor activity. DL149 can bind to an anti-HER2 antibody to form a complete ADC molecule, which precisely binds to the HER2 receptor on the surface of tumor cells. After internalization into cells, it releases the eIF4A inhibitor payload. DL149 irreversibly blocks the mRNA translation process in tumor cells, thereby inhibiting tumor cell proliferation and inducing their death. DL149 exhibits in vivo antitumor activity in the SK-OV-3 xenograft tumor model, and can be used for the research of HER2-positive solid tumors .
|
-
- HY-182238
-
|
|
MAP4K
Interleukin Related
|
Cancer
|
|
HPK1-IN-69 is an orally active HPK1 inhibitor with an IC50 of 1.7 nM. HPK1-IN-69 inhibits the HPK1-mediated TCR signaling pathway, reduces the phosphorylation level of SLP76, and promotes the release of IL-2. HPK1-IN-69 exhibits in vivo anti-tumor activity in mouse models. HPK1-IN-69 can be used for the research of colorectal cancer and MC38 syngeneic tumors .
|
-
- HY-183790
-
|
|
Microtubule/Tubulin
Apoptosis
Caspase
|
Cancer
|
|
SMU-G4 is a Tubulin polymerization inhibitor. SMU-G4 induces G2/M phase cell cycle arrest, triggers Apoptosis, and upregulates the expression of Cleaved-Caspase 3. SMU-G4 exhibits in vivo anti-tumor activity in melanoma xenograft models. SMU-G4 can be used for research related to melanoma .
|
-
- HY-D3353
-
|
|
PSMA
|
Cancer
|
|
PSMA-SulfoCy7 is a high-affinity imaging agent targeting PSMA/GCPII (with a Ki of 18.1 nM for human PSMA). PSMA-SulfoCy7 regulates PSMA-dependent NAAG hydrolysis. PSMA-SulfoCy7 exhibits excellent in vivo imaging capability, enabling clear visualization of PSMA-expressing tumors in xenograft models, with no obvious toxicity even at a dose of 87.9 mg/kg. PSMA-SulfoCy7 is widely used in prostate cancer-related studies .
|
-
- HY-P1380
-
|
|
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
Difopein is a 14-3-3 protein inhibitor. Difopein acts as an apoptosis inducer, regulates apoptosis-related proteins, downregulates Bcl-2, upregulates Bax, activates caspase-9 and caspase-3, and induces nuclear fragmentation, membrane-enclosed apoptotic bodies and DNA ladder formation. Difopein serves as a tumor growth inhibitor, which inhibits the proliferation of glioma cells and induces their apoptosis in in vivo nude mouse models. Difopein is applicable to glioma-related research .
|
-
- HY-116452
-
|
|
VEGFR
|
Cancer
|
|
YLT192 is an orally active and highly bioavailable VEGFR2 inhibitor with potent anti-angiogenic activity and anti-tumor efficacy. YLT192 significantly inhibited the kinase activity of VEGFR2 and inhibited the proliferation, migration, invasion and tube formation of human umbilical cord vascular endothelial cells. YLT192 also inhibited VEGF-induced VEGFR2 phosphorylation and its downstream signaling regulators. YLT192 also showed the ability to inhibit angiogenesis in vivo in zebrafish embryo models and alginate-coated tumor cell experiments. YLT192 can directly inhibit the proliferation of cancer cells and induce their apoptosis .
|
-
- HY-D3209
-
|
|
Fluorescent Dye
Quinone Reductase
|
Cancer
|
|
NIR-ASM is a near-infrared fluorescent probe that can cross cell membranes and be activated by NQO1. NIR-ASM can distinguish NQO1-expressing cancer cells from normal cells via fluorescence microscopy and flow cytometry. NIR-ASM generates near-infrared fluorescence with a high signal-to-noise ratio in tumor models with NQO1 activity, enabling the detection of endogenous NQO1 activity in vivo. NIR-ASM is applicable to the research of lung cancer and breast cancer .
|
-
- HY-182700
-
|
|
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 .
|
-
- HY-182242
-
|
|
c-Myc
|
Cancer
|
|
AGB-374 is an orally active NDUFS7 inhibitor. AGB-374 destabilizes NDUFS7 protein and inhibits oxidative phosphorylation by targeting mitochondrial complex I. AGB-374 reduces MYC protein levels in colon cancer cells in vivo and delays tumor growth in syngeneic mouse models of colon cancer. AGB-374 synergistically enhances the cytotoxicity of copper chelators against cancer cells. AGB-374 cooperates with copper chelators to downregulate MYC and NDUFS7 protein levels in cancer cells. AGB-374 can be used for the research of colon cancer .
|
-
- HY-181943
-
|
|
Acyltransferase
|
Cancer
|
|
SPT-IN-2 is an orally active serine palmitoyltransferase (SPT) inhibitor (with an IC50 of 0.71 nM against human SPT2). SPT-IN-2 inhibits ceramide synthesis, suppresses cancer cell growth, and exhibits in vivo anti-tumor activity, favorable metabolic stability and cell membrane permeability in xenograft mouse models. SPT-IN-2 blocks the de novo sphingolipid synthesis pathway, significantly reducing intracellular ceramide levels and the levels of 3-ketodihydrosphingosine (3-KDS), the immediate downstream product of SPT. SPT-IN-2 can be used in research related to lung adenocarcinoma, acute promyelocytic leukemia and breast cancer .
|
-
- HY-183632
-
|
|
Microtubule/Tubulin
Apoptosis
|
Neurological Disease
Cancer
|
|
QW-5-70 is a potent colchicine‑site tubulin inhibitor that blocks tubulin polymerization. QW-5-70 induces mitotic and G2/M cell cycle arrest, triggers mitochondrial apoptosis, and suppresses cancer cell colony formation and migration. QW-5-70 overcomes P‑glycoprotein‑mediated multidrug resistance and inhibits drug‑resistant tumor growth. QW-5-70 demonstrates strong in vitro and in vivo antitumor efficacy in neuroblastoma and prostate cancer models. QW-5-70 can be used for the research of high-risk neuroblastoma and castration-resistant prostate cancer .
|
-
- HY-104048R
-
|
|
Reference Standards
Histone Demethylase
|
Cancer
|
|
QC6352 (Standard) is the analytical standard of QC6352 (HY-104048). This product is intended for research and analytical applications. QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
|
-
- HY-181996
-
|
|
Btk
Caspase
Apoptosis
PARP
|
Cancer
|
|
BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies .
|
-
- HY-181906
-
|
|
PROTACs
Reactive Oxygen Species (ROS)
CDK
|
Cancer
|
|
ZnPc-PEG2-VH032 is a VHL-pathway-dependent photodegradation targeting chimera (PDTAC) and cytotoxic agent. ZnPc-PEG2-VH032 (HY-120217) binds to the VHL ligand domain, and then specifically degrades VHL under light irradiation, a process independent of non-specific ROS-mediated protein damage. ZnPc-PEG2-VH032 uses Zinc phthalocyanine (HY-19204) as a photosensitizer, and generates ROS via type I and type II photodynamic pathways under 680 nm LED irradiation. On one hand, it targets and degrades the bound VHL protein through ROS; on the other hand, it exerts direct photodynamic cytotoxicity. Meanwhile, the degradation of VHL downregulates the phosphorylation level of CDK2/4, induces cell cycle arrest in tumor cells, further enhances the sensitivity of tumor cells to oxidative damage caused by ROS, and achieves a synergistic anti-tumor effect. ZnPc-PEG2-VH032 exerts significant in vivo efficacy in an orthotopic mouse model of non-muscle invasive bladder cancer (NMIBC) .
|
-
- HY-126929
-
|
TXN-B
|
DNA Alkylator/Crosslinker
Apoptosis
Bacterial
Parasite
Fungal
|
Infection
Cancer
|
|
Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeted inhibitor. Trioxacarcin B disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B not only effectively inhibits the growth of various Gram-positive and Gram-negative bacteria as well as Plasmodium falciparum, but also blocks the colony formation of cancer stem cells, significantly reduces tumor volume and prolongs survival in preclinical in vivo models. The activity of Trioxacarcin B is highly dependent on its intact spiro-epoxide structure; it loses efficacy once this moiety undergoes hydrolysis, and Trioxacarcin B shows no activity against fungi, microalgae and small RNA viruses. Trioxacarcin B can be used for research on bacterial infections, malaria, and various cancers including colon cancer and melanoma .
|
-
- HY-179404
-
|
|
Ras
|
Cancer
|
|
KRASG12C IN-18 is an orally active covalent KRAS G12C inhibitor that achieves complete covalent engagement of KRAS G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS G12C and resistance-associated variants, including KRAS G12C/R68S, with low-nanomolar IC50 values.
KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS G12C-driven solid tumor and KRAS G12C/R68S xenograft models and can be used for colorectal cancer research .
|
-
- HY-W142432S
-
|
|
Isotope-Labeled Compounds
Biochemical Assay Reagents
β-catenin
Wnt
Arginase
TGF-beta/Smad
mTOR
Akt
ERK
Atg8/LC3
p62
Autophagy
|
Metabolic Disease
|
|
Perfluoroundecanoic acid- 13C7 is the 13C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation .
|
-
- HY-183246
-
|
|
PAK
Cdc42-binding kinase
|
Cancer
|
|
Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr 423/Thr 402/Thr 436 and Ser 141/Ser 144/Ser 154 in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer .
|
-
- HY-169480
-
|
|
Liposome
|
Infection
Cancer
|
|
Lipid C2 is an ionizable cationic lipid that has been used in the formation of lipid nanoparticles (LNP) for mRNA delivery in vivo. LNPs containing Lipid C2 and encapsulating an mRNA reporter selectively accumulate in the liver and spleen but not the heart, lungs, or kidneys in mice. LNP containing Lipid C2 and encapsulating mRNA encoding the Epstein-Barr virus (EBV) protein latent membrane protein 2 (LMP-2), in combination with an anti-programmed cell death protein 1 (PD-1) antibody, decrease tumor volume and reverse T cell exhaustion, as well as increase the percentage of CD3 +CD8 + central and CD3 +CD8 + effector memory T cells and decrease the percentage of CD3 + T cells expressing Pd-1, in the spleen in a CT26 murine EBV-infected colon cancer model .
|
-
- HY-13590
-
|
|
VEGFR
|
Cancer
|
|
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
|
-
- HY-W768347
-
|
Xylite-13C5
|
Isotope-Labeled Compounds
Bacterial
Autophagy
Endogenous Metabolite
Atg8/LC3
Atg7
|
Cancer
|
|
Xylitol- 13C5 (Xylite- 13C5) is the 13C-labeled Xylitol (HY-N0538). Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
|
-
- HY-178032
-
|
|
PARP
Apoptosis
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
STING
|
Cancer
|
|
PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy .
|
-
- HY-P992056
-
|
|
Autophagy
|
Cancer
|
|
Anti-Human/Mouse LY6E Antibody (9B12) is a high-affinity, multi-target antibody that binds specifically to LY6E. Anti-Human/Mouse LY6E Antibody (9B12) binds specifically to cell-surface LY6E and enters lysosomes via lipid raft-dependent endocytosis, thereby effectively inhibiting the growth of various LY6E-expressing solid tumors (such as breast cancer and lung cancer) in both in vitro and in vivo models. Anti-Human/Mouse LY6E Antibody (9B12) exerts a dual mechanism of action: on one hand, it blocks the interaction between PILRα and CD8α, specifically reduces the survival rate of peripheral CD8 + T cells and induces their activation, breaking the state of cellular quiescence; on the other hand, it recognizes and immunoprecipitates IDE under both non-denaturing and denaturing conditions, which is applicable to studies on the subcellular localization and protein interactions of IDE. The regulatory effect of Anti-Human/Mouse LY6E Antibody (9B12) on CD8 + T cells strictly depends on the presence of PILRα, and it does not affect CD4 + T cells or T cell development in the thymus, exhibiting high specificity .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-164992
-
|
MRG002; Trastuzumab MMAE
|
Fluorescent Dyes
|
|
Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
|
-
- HY-D2062
-
|
|
Fluorescent Dyes
|
|
ATTO 740 NHS ester is a near-infrared fluorescent dye and a multimodal fluorescence/photoacoustic contrast agent with excellent near-infrared emission properties and extremely high photostability. The photoacoustic signal of ATTO 740 NHS ester shows no significant decrease after continuous irradiation with a 750 nm laser for 30 min, making it suitable for in vivo fluorescence imaging and photoacoustic contrast imaging. When conjugated with the cystine knot peptide R01, ATTO 740 NHS ester enables precise detection of integrin αvβ6-positive cells and tumors in nude mouse xenograft models .
|
-
- HY-D3353
-
|
|
Fluorescent Dyes
|
|
PSMA-SulfoCy7 is a high-affinity imaging agent targeting PSMA/GCPII (with a Ki of 18.1 nM for human PSMA). PSMA-SulfoCy7 regulates PSMA-dependent NAAG hydrolysis. PSMA-SulfoCy7 exhibits excellent in vivo imaging capability, enabling clear visualization of PSMA-expressing tumors in xenograft models, with no obvious toxicity even at a dose of 87.9 mg/kg. PSMA-SulfoCy7 is widely used in prostate cancer-related studies .
|
-
- HY-D3209
-
|
|
Fluorescent Dyes
|
|
NIR-ASM is a near-infrared fluorescent probe that can cross cell membranes and be activated by NQO1. NIR-ASM can distinguish NQO1-expressing cancer cells from normal cells via fluorescence microscopy and flow cytometry. NIR-ASM generates near-infrared fluorescence with a high signal-to-noise ratio in tumor models with NQO1 activity, enabling the detection of endogenous NQO1 activity in vivo. NIR-ASM is applicable to the research of lung cancer and breast cancer .
|
| Cat. No. |
Product Name |
Type |
-
- HY-145799
-
5A2-SC8
1 Publications Verification
|
Biochemical Assay Reagents
|
|
5A2-SC8 is an ionizable amino lipid in lipid nanoparticles (LNPs) that shows high delivery potential and low in vivo toxicity, enabling efficient delivery of small RNAs such as siRNA and miRNA into tumor cells. 5A2-SC8 LNPs can confer a unique delivery fate of RNA within the liver, thereby changing the therapeutic outcomes in cancer models .
|
-
- HY-W088065
-
|
|
Biochemical Assay Reagents
|
Sodium formate acts as a key promoter for heterogeneous nucleation of ZIF crystals and thin film synthesis. It is also recognized as a GRAS substance by the FDA, and serves as a cosmetic preservative and food additive. Sodium formate has low acute oral toxicity (acute oral LD50=7410 mg/kg and acute intravenous LD50=807 mg/kg in mice), with no heritable or carcinogenic effects, but exhibits embryonic developmental toxicity and teratogenicity at high concentrations. Sodium formate may cause moderate irritation to rabbit eyes, is relatively safe to the skin, and does not induce tumor formation in rats in vivo. Sodium formate is rapidly absorbed and oxidized to carbon dioxide in vivo, and forms DNA adducts in specific metabolic deficiency models or upon high-dose exposure .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-164388
-
|
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
|
-
- HY-P1380A
-
|
|
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
Difopein TFA is a 14-3-3 protein inhibitor. Difopein TFA acts as an apoptosis inducer, regulates apoptosis-related proteins, downregulates Bcl-2, upregulates Bax, activates caspase-9 and caspase-3, and induces nuclear fragmentation, membrane-enclosed apoptotic bodies and DNA ladder formation. Difopein TFA serves as a tumor growth inhibitor, which inhibits the proliferation of glioma cells and induces their apoptosis in in vivo nude mouse models. Difopein TFA is applicable to glioma-related research .
|
-
- HY-P5520
-
|
|
Bombesin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
|
-
- HY-P1380
-
|
|
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
Difopein is a 14-3-3 protein inhibitor. Difopein acts as an apoptosis inducer, regulates apoptosis-related proteins, downregulates Bcl-2, upregulates Bax, activates caspase-9 and caspase-3, and induces nuclear fragmentation, membrane-enclosed apoptotic bodies and DNA ladder formation. Difopein serves as a tumor growth inhibitor, which inhibits the proliferation of glioma cells and induces their apoptosis in in vivo nude mouse models. Difopein is applicable to glioma-related research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P991577
-
|
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. .
|
-
(5)
-
- HY-P99852
-
|
ABT165; PR1283233
|
VEGFR
Notch
|
Cancer
|
|
Dilpacimab (ABT165) is a bispecific variable domain immunoglobulin. Dilpacimab binds to and inhibits DLL4 and VEGF and acts as a tumor growth inhibitor. Dilpacimab can be used in research related to metastatic colorectal cancer and advanced solid tumors .
|
-
(5)
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
(5)
-
- HY-P991336
-
|
InBRX-106; ES-102
|
Orexin Receptor (OX Receptor)
|
Inflammation/Immunology
Cancer
|
|
Ordastobart (INBRX-106; ES-102) is a hexavalent OX40 agonist antibody. Ordastobart enhances OX40 receptor clustering, signaling, and downstream activation, thereby increasing the proliferation and activation of CD4 + and CD8 + T cells in vitro and in vivo. Ordastobart exhibits anti-tumor effects and improves survival in mouse models of cancer. Ordastobart is indicated for research in cancers such as fibrosarcoma and colorectal cancer .
|
-
(5)
-
- HY-P990947
-
|
AZD9592 Antibody
|
ADC Antibody
EGFR
|
Cancer
|
|
Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .
|
-
(5)
-
- HY-P990778
-
|
ATG-101
|
TNF Receptor
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Xirestomig (ATG-101) is a tetravalent "2+2″ PD-L1×4-1BB bispecific antibody. Xirestomig binds PD-L1 and 4-1BB concurrently, with a greater affinity for PD-L1, and potently activated 4-1BB+ T cells when cross-linked with PD-L1-positive cells. Xirestomig activates exhausted T cells upon PD-L1 binding. Xirestomig displays potent antitumor activity in numerous in vivo tumor models, including those resistant or refractory to immune checkpoint inhibitors (ICIs) .
|
-
(5)
-
- HY-P992056
-
|
|
Autophagy
|
Cancer
|
|
Anti-Human/Mouse LY6E Antibody (9B12) is a high-affinity, multi-target antibody that binds specifically to LY6E. Anti-Human/Mouse LY6E Antibody (9B12) binds specifically to cell-surface LY6E and enters lysosomes via lipid raft-dependent endocytosis, thereby effectively inhibiting the growth of various LY6E-expressing solid tumors (such as breast cancer and lung cancer) in both in vitro and in vivo models. Anti-Human/Mouse LY6E Antibody (9B12) exerts a dual mechanism of action: on one hand, it blocks the interaction between PILRα and CD8α, specifically reduces the survival rate of peripheral CD8 + T cells and induces their activation, breaking the state of cellular quiescence; on the other hand, it recognizes and immunoprecipitates IDE under both non-denaturing and denaturing conditions, which is applicable to studies on the subcellular localization and protein interactions of IDE. The regulatory effect of Anti-Human/Mouse LY6E Antibody (9B12) on CD8 + T cells strictly depends on the presence of PILRα, and it does not affect CD4 + T cells or T cell development in the thymus, exhibiting high specificity .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-W768347
-
|
|
|
Xylitol- 13C5 (Xylite- 13C5) is the 13C-labeled Xylitol (HY-N0538). Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
|
-
-
- HY-122607S
-
|
|
|
DPA-714-d10 is the deuterium labeled DPA-714 (HY-122607). DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.
|
-
-
- HY-W142432S
-
|
|
|
Perfluoroundecanoic acid- 13C7 is the 13C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-134813
-
|
|
|
Alkynes
|
|
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-148813
-
AK-2292
2 Publications Verification
|
|
PROTAC Synthesis
|
|
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-179404
-
|
|
|
Alkynes
|
|
KRASG12C IN-18 is an orally active covalent KRAS G12C inhibitor that achieves complete covalent engagement of KRAS G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS G12C and resistance-associated variants, including KRAS G12C/R68S, with low-nanomolar IC50 values.
KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS G12C-driven solid tumor and KRAS G12C/R68S xenograft models and can be used for colorectal cancer research .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-145799
-
5A2-SC8
1 Publications Verification
|
|
Cationic Lipids
|
|
5A2-SC8 is an ionizable amino lipid in lipid nanoparticles (LNPs) that shows high delivery potential and low in vivo toxicity, enabling efficient delivery of small RNAs such as siRNA and miRNA into tumor cells. 5A2-SC8 LNPs can confer a unique delivery fate of RNA within the liver, thereby changing the therapeutic outcomes in cancer models .
|
-
- HY-N0538
-
|
Xylite
|
|
Fillers
|
|
Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
|
-
- HY-145799A
-
|
|
|
Cationic Lipids
|
|
5A2-SC8 TFA is an ionizable amino lipid in lipid nanoparticles (LNPs) that shows high delivery potential and low in vivo toxicity, enabling efficient delivery of small RNAs such as siRNA and miRNA into tumor cells. 5A2-SC8 TFA LNPs can confer a unique delivery fate of RNA within the liver, thereby changing the therapeutic outcomes in cancer models .
|
-
- HY-169480
-
|
|
|
Cationic Lipids
|
|
Lipid C2 is an ionizable cationic lipid that has been used in the formation of lipid nanoparticles (LNP) for mRNA delivery in vivo. LNPs containing Lipid C2 and encapsulating an mRNA reporter selectively accumulate in the liver and spleen but not the heart, lungs, or kidneys in mice. LNP containing Lipid C2 and encapsulating mRNA encoding the Epstein-Barr virus (EBV) protein latent membrane protein 2 (LMP-2), in combination with an anti-programmed cell death protein 1 (PD-1) antibody, decrease tumor volume and reverse T cell exhaustion, as well as increase the percentage of CD3 +CD8 + central and CD3 +CD8 + effector memory T cells and decrease the percentage of CD3 + T cells expressing Pd-1, in the spleen in a CT26 murine EBV-infected colon cancer model .
|
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