Search Result
Results for "
Tumor uptake
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-15763
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Erastin
Maximum Cited Publications
805 Publications Verification
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VDAC
Ferroptosis
Disulfidptosis
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Cancer
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Erastin is a ferroptosis inducer. Erastin exhibits the mechanism of ferroptosis induction related to ROS and iron-dependent signaling. Erastin inhibits voltage-dependent anion channels (VDAC2/VDAC3) and accelerates oxidation, leading to the accumulation of endogenous reactive oxygen species. Erastin also disrupts mitochondrial permeability transition pore (mPTP) with anti-tumor activity. Furthermore, Erastin can block the uptake of cystine mediated by SLC7A11 and also spares UMRC6-EV and -C91A cells from disulfidptosis under glucose starvation .
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- HY-P99974
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Nanoparticle albumin-bound Paclitaxel; Nanoparticle albumin-bound ABI-007
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Microtubule/Tubulin
Apoptosis
Autophagy
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Cancer
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Nab-Paclitaxel (Nanoparticle albumin-bound Paclitaxel) is an albumin-bound nanoparticle formulation of Paclitaxel (HY-B0015). Nab-Paclitaxel is composed of albumin and the active pharmaceutical ingredient Paclitaxel, in which human albumin is used as an excipient to disperse and stabilize particles and carry the main drug. Nab-Paclitaxel is a solvent-free taxane with higher response rates and improved tolerability. Nab-Paclitaxel displays less toxicity and greater antitumor activity. Nab-Paclitaxel is more readily available for tumor cell uptake in three rhabdomyosarcoma, seven neuroblastoma cell lines, and one ostersarcoma cell line Nab-Paclitaxel can be studied in cancer research for example breast cancer and solid tumors. (The product specifications below only indicate the effective content of Paditaxel, the actual albumin quality depends on the batch; the ratio of each ingredient in this product is Paditaxel: albumin -1:7~1:11) .
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- HY-137331
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FAPI-46
2 Publications Verification
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FAP
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Cancer
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FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted tracer. Use radioactivity FAPI-46 labeled with 68Ga or 177Lu can be used for tumor imaging in a variety of cancers and has higher tumor uptake rates and longer tumor accumulation .
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- HY-D1063
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Fluorescent Dye
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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IR-780 is a near-infrared fluorescent probe for in vivo imaging of tumor cells. IR-780 is transported into tumor cells via OATPs and ABCB10, with uptake dependent on glycolytic activity and plasma membrane potential. IR-780 preferentially accumulates in tumor cell mitochondria, including those of drug-resistant cancer cells, without chemical conjugation. IR-780 generates reactive oxygen species (ROS), induces hyperthermia and apoptosis, inhibits tumor growth and recurrence, and modulates HSP70 expression upon ultrasound or 808 nm laser exposure. IR-780 acts as a sonosensitizer, photodynamic and photothermal agent, and drug delivery carrier, with low acute imaging-dose toxicity and rapid vital organ clearance. IR-780 can be used for the research of cancer, such as breast cancer, lung cancer, and non-small cell lung cancer (NSCLC) .
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- HY-W1126504
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MC339
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Notch
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Cancer
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ETN029 (MC339) is a selective DLL3 ligand. ETN029 labeled with 225Ac has dose-dependent cytotoxicity in SCLC, NEPC and metastatic melanoma cells and increases the phosphorylation of H2AX expression. ETN029 labeled with 177Lu shows rapid uptake persistent tumor retention and favorable tumor-to-kidney ratio. ETN029 can be used for cancers like SCLC and NEPC imaging and research .
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- HY-P5321
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FGFR
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Cancer
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bFGF (119-126) is a ligand of bFGF. The complex formed by bFGF (119-126) and bFGF can bind to FGFR1, while inhibiting the bFGF-FGFR1 interaction, FGFR1 phosphorylation and downstream signaling pathways. Therefore, bFGF (119-126) induces cell apoptosis and inhibits cell proliferation, migration, angiogenesis and metastasis. When conjugated with a carrier, bFGF (119-126) enhances cellular uptake via FGFR-mediated endocytosis and serves as an effective FGFR-targeted ligand. When used in combination with ultrasound and Doxorubicin (HY-15142A), bFGF (119-126) significantly enhances the inhibitory effect on tumors. bFGF (119-126) is applicable to research related to lung cancer, breast cancer, glioblastoma and ovarian cancer .
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- HY-W087028
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Radionuclide-Drug Conjugates (RDCs)
Biochemical Assay Reagents
CXCR
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Cancer
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NOTA-NHS ester is a chelating agent. NOTA-NHS ester can be coupled with T140 (HY-P4810) to produce NOTA-T140. NOTA-T140 can be radiolabeled with Al[ 18F]. The uptake of Al[ 18F]NOTA-T140 in tumors is correlated with the expression level of CXCR4. Al[ 18F]NOTA-T140 can be used in tumor PET imaging studies. NOTA-NHS ester can be used for fluorescent labeling .
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- HY-12203
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Autophagy
Apoptosis
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Cancer
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PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria .
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- HY-W614269
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Radionuclide-Drug Conjugates (RDCs)
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Cancer
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DOTA-GA(tBu)4 stabilizes the attachment of radiometals to ligands. DOTA-GA(tBu)4 improves the biodistribution of radiolabeled second-generation Affibody molecules by increasing their net negative charge and reducing hepatic uptake, leading to enhanced tumor-to-blood and tumor-to-liver ratios. DOTA-GA(tBu)4 targets HER2>-expressing breast and gastrointestinal cancer .
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- HY-P5126
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 and 68 Ga-DOTA-LM3. 68 Ga-DOTA-LM3 shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis . DOTA-LM3 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-139401
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FAP
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Cancer
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FAPI-34 is a SPECT imaging agent targeting FAP. FAPI-34 specifically binds to FAP, is highly internalized by FAP-expressing cells, accumulates in FAP-expressing tumor lesions, and shows low uptake in normal tissues except the kidneys. FAPI-34 is applicable for tumor-related research .
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- HY-158302
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GLUT
Apoptosis
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Cancer
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Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis .
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- HY-P5362
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Neurological Disease
Cancer
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NODAGA-LM3 is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC50 = 1.3 nM). NODAGA-LM3 does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 shows low uptake in normal tissues such as the liver and spleen, but high uptake in the lungs and blood pool. 68Ga-labeled NODAGA-LM3 can serve as a PET imaging agent for well-differentiated neuroendocrine tumors, and is applied in studies related to small cell lung cancer and well-differentiated neuroendocrine tumors .
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- HY-101849
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GLUT
TNF Receptor
Apoptosis
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Cardiovascular Disease
Cancer
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Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
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- HY-N2040
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Bacterial
Interleukin Related
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Infection
Inflammation/Immunology
Cancer
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(20R)-Protopanaxadiol is a metabolite of ginsenosides. (20R)-Protopanaxadiol has anti-inflammatory and antibacterial activities, but shows no significant cytotoxicity against tumor cell lines. In addition, (20R)-Protopanaxadiol can inhibit the uptake of 2-deoxy-D-glucose (2-DG) .
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- HY-B1231
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RP-2831 hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
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Heptaminol (RP-2831) hydrochloride is a vasoconstrictor used in the study of hypotension, especially orthostatic hypotension. Heptaminol is also a skin cancer proliferation inhibitor that inhibits immune inflammation induced by the tumor promoting factor 12-O-tetradecanoylphorbol-13-acetate (TPA) in an NO-dependent manner. Heptaminol also acts as a sympathomimetic amine, exerting indirect sympathetic effects. Heptaminol is also an antagonist of catecholamine release and uptake and can increase intracellular free calcium levels .
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- HY-P1723
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Spexin
2 Publications Verification
Neuropeptide Q
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Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
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Cardiovascular Disease
Neurological Disease
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Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
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- HY-P5126A
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 TFA is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 TFA and 68 Ga-DOTA-LM3 TFA. 68 Ga-DOTA-LM3 TFA shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 TFA can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis . DOTA-LM3 (TFA) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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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-P1848
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Interleukin Related
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Cancer
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Pep-1 (uncapped) is a specific ligand of IL-13Ra2. Pep-1 (uncapped) exerts cell penetrating activity through receptor-mediated endocytosis, can cross the blood-tumor barrier (BTB) and target glioma cells. Pep-1 (uncapped) can enhance the uptake of nanoparticles by tumor cells and enhance the cell penetration ability of nanoparticles, and can be used to develop targeted drug delivery systems for glioma .
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- HY-128878
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Cholecystokinin Receptor
P-glycoprotein
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Metabolic Disease
Endocrinology
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Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors .
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- HY-158302A
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GLUT
Apoptosis
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Cancer
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(R)-Glutor is the R-enantiomer of Glutor (HY-158302). Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis .
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- HY-106031
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Topoisomerase
DNA/RNA Synthesis
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Cancer
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F-14512 is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 can be used to study breast cancer .
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- HY-N6924
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HIV
PIN1
Fungal
GLUT
Reactive Oxygen Species (ROS)
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Infection
Neurological Disease
Metabolic Disease
Cancer
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Zingibroside R1 is an orally active triterpene saponin with multiple biological activities including antioxidant, anti-inflammatory, antiviral, and metabolic regulatory properties. Zingibroside R1 reduces the expression of PIN family members, inhibits the expression of PLT1/PLT2, WOX5, SHR, and SCR, disrupts auxin transport and distribution, triggers plant ROS responses, and inhibits root growth. Zingibroside R1 extends the lifespan of Caenorhabditis elegans, enhances its heat stress resistance, and improves its motor ability. Hydrogel derivatives of Zingibroside R1 inhibit the proliferation of Candida albicans by binding to its β-1,3-glucan and exhibit antifungal activity. Zingibroside R1 inhibits GLUT1-mediated uptake and alleviates liver injury. Zingibroside R1 can be used in research related to neurodegenerative diseases, vulvovaginal candidiasis, acute liver injury, Ehrlich ascites tumor and HIV-1 infection .
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- HY-175613
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FAP
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Cancer
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DOTA-ALB-02 is an albumin-bound FAP inhibitor (FAPI) ligand. DOTA-ALB-02 labeled with 177Lu has a high FAP-binding affinity and enhanced tumor uptake and retention with a significant tumor/nontarget ratio. DOTA-ALB-02 can be used for PET/CT and SPECT/CT imaging of cancers, especially late-stage cancers .
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- HY-159067
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DEAE-dextran, MW 500000 hydrochloride, from bacterial (Leuconostoc mesenteroides); Diethylaminoethyl-dextran, MW 500000 hydrochloride
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Biochemical Assay Reagents
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Cancer
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DEAE-dextran, MW 500000 hydrochloride (DEAE-dextran, MW 500000 hydrochloride, from bacterial (Leuconostoc mesenteroides)) is a high-molecular-weight positively charged polymer that significantly enhances the uptake of viral RNA by tissue culture cells. When employed in the delivery system for "tumor immunity" RNA-splenocyte transfer, DEAE-dextran can markedly extend the lifespan of tumor-bearing animals, comparable to that of actively immunized animals. Furthermore, DEAE-dextran serves as a complexing agent for nucleic acids, forming composite particles with DNA/RNA for extensive applications in gene delivery. Additionally, DEAE-dextran can be utilized as a coating for liposomes .
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- HY-123733A
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RPS-001 TFA
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PSMA
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Cancer
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MIP-1095 (RPS-001) TFA is a potent inhibitor of PSMA with good biodistribution and efficient targeting of tumor lesions. In applications, MIP-1095 TFA will be isotopically labeled ( 131I labeled) as an imaging probe to indicate tumor progression. And 131I-MIP-1095 showed higher renal uptake in mice .
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- HY-175744
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PSMA
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Cancer
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PSMA-MAL-5 is a PSMA ligand. PSMA-MAL-5 covalently binds to Cys466 of PSMA. PSMA-MAL-5 labeled with 177Lu and 225Ac has high radiostability and tumor uptake. PSMA-MAL-5 also effectively inhibits tumor growth. PSMA-MAL-5 can be used for SPECT/CT imaging and radionuclide therapy of prostate cancer .
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- HY-170779
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FAP
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Cancer
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DOTA-NI-FAPI-04 is a FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([68Ga]Ga/DOTA-NI-FAPI-04 and [177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact .
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- HY-P10781
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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PSMA-D5 has a binding affinity for PSMA with a Ki of 0.21 nM and can be used for PSMA tracing after radiolabeling. PSMA-D5 ([68Ga]-labeled) contains a DOTA chelator, allowing convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. PSMA-D5 ([68Ga]-labeled) shows excellent pharmacokinetic properties, exhibiting remarkable tumor uptake in 22Rv1 tumors . PSMA-D5 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-124689
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Arp2/3 Complex
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Metabolic Disease
Cancer
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TR-100 is a small molecule inhibitor of tumor-associated troponin (Tpm). TR-100 affects the interaction of Tpm3.1 with actin filaments by binding to the C-terminal of Tpm3.1, thereby affecting the stability and function of the actin filaments. This mechanism of action allows TR-100 to specifically affect actin filaments in cancer cells without compromising heart muscle function. TR-100 can be used to study the role of Tpm3.1 in cancer cell proliferation and survival and the effects of Tpm3.1 on insulin-stimulated glucose uptake and insulin secretion .
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- HY-D2281
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FAP
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Cancer
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FAP Ligand 2, a FAPI-46 derivative, is a specific fibroblast activation protein (FAP)-targeted tracer. FAP Ligand 2 exhibits good tumor uptake and acts as a promising molecular tracer for FAP tumor imaging .
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- HY-163281
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Fluorescent Dye
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Cancer
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FSY-OSO2F shows an uptake in MCF-7 cells through the regulation of L-Tyr, ASC, and ASC2 transporters. FSY-OSO2F can be used as a PET tracer, when labeled with 18F, and exhibits good uptake and good contrast in MCF-7 and 22Rv1 subcutaneous tumors .
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- HY-143618
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Biochemical Assay Reagents
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Cancer
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photoCORM-2 (compound 3) is a single carbon monoxide releasing molecule (CORM). photoCORM-2 exhibits good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach. photoCORM-2 has anti-tumor activity .
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- HY-175612
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FAP
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Cancer
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DOTA-ALB-01 is an albumin-bound FAP inhibitor (FAPI) ligand. DOTA-ALB-01 labeled with 68Ga or 177Lu has a high FAP-binding affinity and enhanced tumor uptake and retention. DOTA-ALB-01 can be used for PET/CT and SPECT/CT imaging of cancers, especially late-stage cancers .
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- HY-179578
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Enolase
AMPK
Autophagy
Apoptosis
mTOR
Caspase
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Metabolic Disease
Cancer
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SU212 is a podophyllotoxin-derived ENO1 inhibitor and AMPK activator. SU212 can selectively induce oxidative phosphorylation, reduce glycolysis activity and glucose uptake in tumor cells, and directly bind to ENO1 without affecting these pathways in normal cells. SU212 induces apoptosis and promotes ENO1 degradation via proteasomal and autophagic pathways without inhibiting the catalytic activity. SU212 leads to mitotic arrest and apoptosis in TNBC (triple-negative breast cancer) cells by activating AMPK, demonstrating potent anti-tumor activity in vitro. SU212 inhibits tumor growth and metastasis in syngeneic, xenograft, and diabetic mouse models, exhibiting an excellent safety profile. SU212 can be used in research on t TNBC, diabetes, and fatty liver disease .
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- HY-W241345
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Radionuclide-Drug Conjugates (RDCs)
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Cancer
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DOTA-bis(tert-butyl)ester is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide conjugates (RDCs). DOTA-bis(tert-butyl)ester can be conjugated with different salts to form different metal chelators, such as (HY-B1244) hydrochloride to obtain DOTA-MN2. DOTA-MN2 can be reacted with [67]Ga-citrate to obtain radiolabeling. When (67)Ga-DOTA-MN2 is incubated in phosphate buffer solution or mouse plasma for 24 hours, it does not undergo significant decomposition. In the biodistribution experiment of NFSa tumor mice, it has high tumor uptake and rapid plasma clearance, and is a good material for SPECT and PET studies.
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- HY-P10444
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Radionuclide-Drug Conjugates (RDCs)
CXCR
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Cancer
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DOTA Conjugated JM#21 derivative 7 (compound Ligand-7) is a derivative of CXCR4 targeting peptide conjugated with DOTA and can be used to produce radioligands. Radiolabeled DOTA Conjugated JM#21 derivative 7, i.e., 177Lu-DOTA, has excellent CXCR4 tumor targeting. In vitro biodistribution results of 177Lu-DOTA showed very low uptake in all non-targeted organs except kidney . DOTA Conjugated JM#21 derivative 7 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-169868
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Biochemical Assay Reagents
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Cancer
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NOTA-FAPI-52 is a tracer with potent tumor uptake. NOTA-FAPI-52 can be radiolabeled to enable PET imaging or other bioimaging techniques. NOTA-FAPI-52 can be used to study diseases in which fibroblast activation protein (FAP) is overexpressed .
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- HY-175014
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PD-1/PD-L1
Biochemical Assay Reagents
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Cancer
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LGT-1 is a PD-L1 ligand. LGT-1 labeled with 18F has an excellent specific uptake in B16-F10 tumor cells, and shows a high tumor uptake but a low liver uptake with good stability in B16-F10 tumor-bearing mice model. LGT-1 can be used as a radiotracer for PET imaging of PD-L1 expression in tumors .
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- HY-174440
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PSMA
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Cancer
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BWD is a PSMA ligand (IC50 = 35.86). BWD exhibits excellent in vitro stability and high affinity. BWD can enhance tumor uptake and retention. BWD can inhibit tumor growth in vivo. BWD can be studied in anticancer research .
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- HY-173116
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Carbonic Anhydrase
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Cancer
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DOTA-XYIMSR-01 is a molecular probe targeting CAIX that can be labeled with 177Lu for the inhibition and localization of malignant gliomas. The uptake of [177Lu] Lu-XYIMSR-01 in U87MG tumors is 6.19 % of the injected dose per gram (% ID/g), and the tumor-to-muscle uptake ratio is 20.14. In the orthotopic glioma model, combined injection with Temozolomide (HY-17364) can significantly improve the survival rate of mice and inhibit tumor growth. DOTA-XYIMSR-01 shows promise for research in the field of anti-cancer therapy .
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- HY-163683
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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EB-PSMA-617 is a modified form of PSMA-617 that has enhanced pharmacokinetic properties by conjugating it to Evans Blue (EB) to extend its circulation half-life to improve prostate tumor uptake and radiotherapy efficacy. In preclinical studies using PC3-PIP-loaded mice, EB-PSMA-617 demonstrated prolonged blood half-life, increased accumulation in PSMA-positive tumors, and successful tumor elimination with lower radioactivity .
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- HY-159771
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FAP
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Cancer
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FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a Kd of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as 177Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with 111In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.
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- HY-P5362A
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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NODAGA-LM3 TFA is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC50 = 1.3 nM). NODAGA-LM3 TFA does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 TFA shows low uptake in normal tissues such as the liver and spleen, but high uptake in the lungs and blood pool. 68Ga-labeled NODAGA-LM3 TFA can serve as a PET imaging agent for well-differentiated neuroendocrine tumors, and is applied in studies related to small cell lung cancer and well-differentiated neuroendocrine tumors .
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- HY-172366
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PSMA
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Cancer
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BQ0413 exhibits good affinity to PSMA with a KD of 89 pM. BQ0413 exhibits good uptake and internalization property with an internalization rate of 44% in PC3-pip cell. BQ0413 can be used as tumor imaging agent when labeled with 99mTc .
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- HY-P10239A
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Radionuclide-Drug Conjugates (RDCs)
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Cancer
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Tyr3-Octreotate acetate is a somatostatin analog. Tyr3-Octreotate acetate exhibits high uptake into tumor, that is capable to be labeled with radioactive metal and thus exhibits antitumor efficacy. Tyr3-Octreotate acetate can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .
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- HY-P11265
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GnRH Receptor
Fluorescent Dye
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Cancer
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|
YQGN-7 is a targeted fluorescent probe for the gonadotropin-releasing hormone receptor (RnRHR). YQGN-7 exhibits high selectivity and affinity for breast cancer cells (KD = 217.8 nM). YQGN-7 achieves precise visualization of the primary and metastatic lesions of breast cancer by targeting the highly expressed GnRHR in tumor cells. YQGN-7 can be used in the research of breast cancer breast-conserving surgery (BCS) .
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-
-
- HY-158266
-
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LNC1003
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
DOTA-PSMA-EB-01 (Compound LNC1003) is a specific inhibitor of PSMA (IC50= 10.77 nM).DOTA-PSMA-EB-01 enhances the uptake and retention time of 177Lu in tumors . DOTA-PSMA-EB-01 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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-
-
- HY-175248
-
|
|
PSMA
|
Cancer
|
|
PSMA-DIM is a dimeric PSMA ligand with a Kd of 37.09 nM for LNCaP cells. PSMA-DIM can be radiolabeled with [ 68Ga]Ga to form [ 68Ga]Ga-PSMA-DIM. [ 68Ga]Ga-PSMA-DIM can effectively distinguish between cells and animal models with different expression levels of PSMA. [ 68Ga]Ga-PSMA-DIM exhibits high LNCaP cells uptake and tumor uptake peak values. PSMA-DIM can be used for the study of prostate cancer (PCa) .
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- HY-175591
-
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Photosensitizer
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
|
|
Photosensitizer-7 is a endoplasmic reticulum (ER)-targeted photosensitizer (PS) (λab = 610 nm, λem = 622 nm). Photosensitizer-7shows an IC50 of 4.006 μM in HeLa cells and 3.28 μM in MCF-7 cells under light irradiation. Photosensitizer-7 exhibits dose-dependent cellular uptake and predominant colocalization with ER. Photosensitizer-7 induces dose-dependent intracellular ROS generation, reduces mitochondrial membrane potential, and increases apoptosis upon light irradiation in cells. Photosensitizer-7 significantly inhibits tumor growth in MCF-7 tumor-bearing mice. Photosensitizer-7 can be used for the study of photodynamic anticancer applications .
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-
- HY-P1723A
-
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Neuropeptide Q TFA
|
Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
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-
- HY-171852
-
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|
Biochemical Assay Reagents
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Cancer
|
|
Iodoquine is an analog of chloroquine. Iodoquine exhibits high uptake in tumor cells and can localize to cells with high ALDH1 content, including cancer stem cells. With low uptake in normal brain tissue, iodoquine can be used in research related to tumor diagnosis or as a radiotracer .
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-
- HY-121659
-
|
|
PSMA
|
Cancer
|
|
DCFBC is a prostate-specific membrane antigen (PSMA) inhibitor that can be used for small animal positron emission tomography (PET) imaging. DCFBC labeled with F 18 ([18F]DCFBC) can images in severe combined immunodeficient mice. [18F]DCFBC uptake is higher in PIP tumors, but almost absent in FLU tumors. [18F]DCFBC uptake is also high in the kidney and bladder, but the radioactivity washout time is shorter than that in PIP tumors. Indicating that [18F]DCFBC can specifically localize to PSMA+ expressing tumors and is applicable to the study of prostate cancer .
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-
- HY-171331
-
|
|
PD-1/PD-L1
Integrin
|
Cancer
|
|
AB-3PRGD2 is a radiotherapeutic agent targeting integrin αvβ3. AB-3PRGD2 shows improved tumor uptake and prolonged tumor retention, leading to significantly enhanced tumor growth suppression. AB-3PRGD2 can remodel the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8 + T cells .
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-
- HY-121470
-
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AH5183
|
Others
|
Others
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|
Vesamicol is a compound used to synthesize radiolabeled derivatives that can be used as sigma receptor ligands for tumor targeting inhibition and have shown certain potential in cellular uptake, biodistribution and inhibition experiments.
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-
- HY-170490
-
|
|
Photosensitizer
Apoptosis
|
Cancer
|
|
TTQ-SA is a near-infrared (NIR) spiro-AIEgen (aggregation-induced emission luminogen), that converts near-infrared light (NIR) into thermal energy, causing thermal damage and death of tumor cells. TTQ-SA exhibits cellular uptake and targeting ability in cancer cell MF-7. TTQ-SA silences the expression of survivin gene with combination of DNAzyme, enhances the sensitivity of tumor cells to photothermal therapy .
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-
- HY-156124
-
|
|
Sigma Receptor
|
Cancer
|
|
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts .
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-
- HY-143617
-
|
|
Photosensitizer
|
Cancer
|
|
photoCORM-1 (compound 8) is a combinatorial carbon monoxide releasing molecule (CORM). photoCORM-1 exhibits good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach. photoCORM-1 has anti-tumor antivity .
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-
- HY-144793
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Deac-SS-Biotin is a potent antitumor agent with improved tumor targeting effects and reduced off-target toxicities. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity .
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-
- HY-114253
-
|
|
EGFR
|
Cancer
|
|
ODS-2004436 is a small molecule radiotracer that uses positron emission tomography (PET) imaging to measure the activity of the epidermal growth factor receptor (EGFR) in tumors. ODS-2004436 labeled with the radioactive isotope fluorine-18 shows significantly higher uptake in the xenograft models of lung cancer with EGFR mutations compared to the wild-type models, and could be used to distinguish the mutation status. ODS-2004436 can be used to identify EGFR-positive tumors and predict their response to certain reagent treatments, especially for non-small cell lung cancer (NSCLC) .
|
-
- HY-101849R
-
|
|
Reference Standards
GLUT
TNF Receptor
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Fasentin (Standard) is the analytical standard of Fasentin. This product is intended for research and analytical applications. Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
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-
- HY-162828
-
|
|
STAT
HDAC
|
Cancer
|
|
STAT3/HDAC-IN-2 (compound 18) is a dual inhibitor of STAT3 and HDAC, inducing autophagy and apoptosis. STAT3/HDAC-IN-2 is an amphiphilic hydroxamic acid hybrid based on the natural product isopropanol lactone (IAL) and is a nanoscale anticancer agent. STAT3/HDAC-IN-2 can self-assemble in water to form nanoparticles, which have higher tumor tissue accumulation, cellular uptake and anticancer properties compared to the free state .
|
-
- HY-128878R
-
|
|
Cholecystokinin Receptor
P-glycoprotein
Reference Standards
|
Metabolic Disease
Endocrinology
|
|
Dexloxiglumide (Standard) is the analytical standard of Dexloxiglumide. This product is intended for research and analytical applications. Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors .
|
-
- HY-P10873
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
|
Cancer
|
|
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
|
-
- HY-106031A
-
|
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer .
|
-
- HY-B1231R
-
|
RP-2831 hydrochloride (Standard)
|
Adrenergic Receptor
Reference Standards
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Heptaminol (hydrochloride) (Standard) is the analytical standard of Heptaminol (hydrochloride). This product is intended for research and analytical applications. Heptaminol (RP-2831) hydrochloride is a vasoconstrictor used in the study of hypotension, especially orthostatic hypotension. Heptaminol is also a skin cancer proliferation inhibitor that inhibits immune inflammation induced by the tumor promoting factor 12-O-tetradecanoylphorbol-13-acetate (TPA) in an NO-dependent manner. Heptaminol also acts as a sympathomimetic amine, exerting indirect sympathetic effects. Heptaminol is also an antagonist of catecholamine release and uptake and can increase intracellular free calcium levels .
|
-
- HY-W010713
-
|
Fimaporfin free base
|
Photosensitizer
|
Cancer
|
|
Meso-tetraphenylchlorin (TPCS2a) is a photosensitizer with poor water solubility, which limits its use in the blood circulation. However, TPCS2a@NPs nanoparticles can be prepared based on polylactic-co-polyethylene glycol acid (PLGA) polymer core loaded with TPCS2. Such nanoparticles can be coated with mesenchymal stem cell-derived plasma membranes (mMSCs) to form mMSC-TPCS2a@NPs, which prolongs blood circulation time and improves tumor targeting ability. Compared with uncoated TPCS2a@NPs, mMSC-TPCS2a@NPs can reduce macrophage uptake by 54% to 70% under different conditions. Both nanoparticle forms are effectively accumulated in MCF7 and MDA-MB-231 breast cancer cells, while uptake in normal breast epithelial cells MCF10A is significantly lower .
|
-
- HY-N3055
-
|
|
Apoptosis
AMPK
Platelet-activating Factor Receptor (PAFR)
Caspase
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Pinusolide is an AMPK activator and PAF receptor antagonist. Pinusolide activates AMPK, phosphorylates ACC, enhances IRS-1 tyrosine phosphorylation, boosts glucose uptake, and modulates insulin signaling. Pinusolide inhibits caspase-3/7 activation, intracellular calcium elevation, reactive oxygen species overproduction, lipid peroxidation, and tumor cell proliferation. Pinusolide stabilizes superoxide dismutase activity, reduces apoptotic hallmarks, induces mitochondrial pathway apoptosis, and triggers DNA fragmentation. Pinusolide can be used for the research of type 2 diabetes, neurodegenerative diseases, acute lymphoblastic leukemia, acute myeloid leukemia, and Burkitt lymphoma .
|
-
- HY-182387
-
|
|
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
NM404 is a targeted radionuclide processing agent with slow clearance. Radioiodine-labeled NM404 is a small-molecule phospholipid ether analog that exhibits significant tumor uptake capacity and persistent tumor retention properties in more than 45 spontaneous and xenograft tumor models .
|
-
- HY-P11591
-
|
PSMA-DOTA-PEI2
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
PDI2 (PSMA-DOTA-PEI2) is a prostate-specific membrane antigen (PSMA) ligand that acts as a tumor retention agent, renal uptake reducer, imaging agent and antitumor agent, applicable in SPECT diagnostic imaging and radiotheranostics. PDI2 specifically binds to PSMA on prostate cancer cells, enters cells via clathrin-dependent endocytosis, and exhibits higher tumor retention rate and lower renal uptake level. PDI2 is applicable in research related to prostate cancer and castration-resistant metastatic prostate cancer .
|
-
- HY-181285
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A ligand 1 is a MAT2A ligand inhibitor (IC50=29.5 nM) and PET tracer that crosses the blood-brain barrier. MAT2A ligand 1 enables non-invasive imaging of MAT2A-expressing tumors, with rapid tumor uptake equilibrium, a high tumor-to-muscle ratio, and specific tumor-binding properties. MAT2A ligand 1 is applicable to research related to non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, gastric cancer, glioblastoma, pancreatic adenocarcinoma, urothelial carcinoma, breast cancer, and prostate cancer .
|
-
- HY-P992339
-
|
|
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
cT84.66 is a highly efficient tumor-targeting agent against carcinoembryonic antigen (CEA). cT84.66 engages in bivalent binding with CEA via variable region antigen-binding sites, enabling precise targeting of CEA-producing tumor cells for delivery of therapeutic radiation. cT84.66 exhibits high tumor uptake rate, rapid clearance rate, and excellent tumor-to-blood ratio. With dual functions as an imaging agent and an antibody-directed radiotherapy agent, cT84.66 is widely used in studies of colorectal cancer and metastatic CEA-positive malignancies .
|
-
- HY-P11737
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
|
Cancer
|
|
IPM-N001 is a carbonic anhydrase IX (CAIX) ligand with a Kd value of <0.0337 nM for hCAIX. When radio-conjugated with 68Ga, IPM-N001 serves as a CAIX-targeted radionuclide tracer. [ 68Ga]Ga-IPM-N001 exhibits excellent tumor uptake and significantly improves the tumor-to-background ratio in PET/CT imaging studies using OS-RC-2 tumor-bearing mice. IPM-N001 can be used for the research of clear cell renal cell carcinoma .
|
-
- HY-P0036D
-
|
|
Drug Derivative
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
Apoptosis
|
Cancer
|
|
NOTA‑Octreotide is a selective SSTR2‑targeting PET tracer. NOTA‑Octreotide binds specifically to SSTR2 and accumulates in SSTR2‑expressing tissues. NOTA‑Octreotide enables effective imaging of somatostatin receptor‑positive tumors in mice and shows high specific uptake in SSTR2‑expressing organs in healthy rats. NOTA-Octreotide can be used for PET imaging investigation of neuroendocrine tumors. .
|
-
- HY-181494
-
|
|
FAP
|
Cancer
|
|
FAPI-X5 is a fibroblast activation protein (FAP) inhibitor. FAPI-X5 binds to the FAP catalytic domain, forming hydrogen bonds with key active residues and engaging in π-π stacking to drive functional inhibition. FAPI-X5 exhibits albumin binding activity to prolong systemic circulation half-life. FAPI-X5 induces cytostatic effects on glioblastoma tumors, slowing tumor growth without regression. FAPI-X5, when labeled with 68Ga, acts as a PET tracer with rapid tumor uptake and high-contrast imaging in glioblastoma tumor-bearing mice. FAPI-X5, when labeled with 177Lu or 47Sc, functions as a targeted radionuclide agent with prolonged tumor retention. FAPI-X5 can be used for the research of glioblastoma .
|
-
- HY-182630
-
|
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
CJ-14897 is a cytokine production inhibitor, with IC50 values of 0.059 μM and 0.59 μM for IL-1β and TNF-α production, respectively, and an IC50 of 180 μM for leucine uptake. CJ-14897 is isolated from the fermentation broth of the basidiomycete Marasmius strain CL21624 .
|
-
- HY-182240
-
|
|
PSMA
|
Cancer
|
|
Cy5-ZW2-617 is a PSMA ligand with a IC50 of 4.39 nM. Cy5-ZW2-617 specifically binds to PSMA and is thereby internalized by PSMA-positive cells. Cy5-ZW2-617 shows uptake in PSMA-positive tumor cells and tumor xenografts in mice. Cy5-ZW2-617 can be used for the research of prostate cancer .
|
-
- HY-183147A
-
|
|
Amino acid Transporter
|
Cancer
|
|
LAT1-IN-2 hydrochloride is an orally active anticancer agent, as well as a LAT1 substrate and tubulin-binding agent. LAT1-IN-2 hydrochloride relies on LAT1 for cellular uptake, disrupts microtubule formation by binding to the colchicine site of tubulin, and induces actin depolymerization to transform cells into a spherical shape. LAT1-IN-2 hydrochloride effectively inhibits tumor growth in xenograft mice. Compared with Etoposide (HY-13629), LAT1-IN-2 hydrochloride shows higher distribution in tumor tissues, lower distribution in major organs, and better tolerability. LAT1-IN-2 hydrochloride has been applied in studies related to esophageal cancer .
|
-
- HY-177011
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRγ-IN-1 is a ERRγ inhibitor with an IC50 of 0.040 μM. ERRγ-IN-1 activates MAPK (p44/p42) and inhibits the activity of ERRγ. ERRγ-IN-1 significantly increases iodine uptake in anaplastic thyroid carcinoma xenografts and suppresses tumor growth in nude mice. ERRγ-IN-1 is applicable for the research of anaplastic thyroid carcinoma .
|
-
- HY-P11781A
-
|
|
Drug Derivative
|
Cancer
|
|
Cys-HW12 is a random peptide containing an N-terminal cysteine. Cys-HW12 can be coupled via the thiol group of Cys. Cys-HW12 can serve as a control for GE11 (HY-P10128)-conjugated mixed micelles targeting EGFR, and also functions as a cytotoxic agent, cellular uptake inhibitor, and tumor growth inhibitor. Cys-HW12 is applicable to pancreatic cancer-related research .
|
-
- HY-16265A
-
|
|
Ephrin Receptor
PDGFR
VEGFR
|
Cancer
|
|
JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .
|
-
- HY-P11594
-
|
|
Neurotensin Receptor
|
Cancer
|
|
JMV 7490 is a highly potent and highly hydrophilic neurotensin receptor NTS1 probe that can be successfully labeled with 68Ga and 111In. JMV 7490 acts as an efflux inhibitor to reduce its efflux in NTS1-positive cancer cells; it also serves as an internalization inducer and is efficiently and continuously internalized by NTS1-positive cancer cells. 111In-radiolabeled JMV 7490 shows persistent uptake in NTS1-positive xenografts in nude mice, but no significant uptake in NTS1-negative xenografts. JMV 7490 can be used for in vivo tracer applications of NTS1-positive tumors and supports related research on colorectal cancer .
|
-
- HY-182746
-
|
|
MDM-2/p53
Drug Derivative
|
Cancer
|
|
RG7388-PEG3-Click-F is a fluorinated analog of the MDM2 inhibitor RG7388 (HY-15676), with an IC50 of 16.8 nM against MDM2. [ 18F]RG7388-PEG3-Click-F exhibits high uptake and specificity in MDM2-expressing myeloma cells, and can be used for non-invasive assessment of MDM2 protein expression levels in tumors .
|
-
- HY-180805
-
|
|
Hexokinase
Mitophagy
Apoptosis
GLUT
|
Cancer
|
|
HK2-IN-3 (compound 12) is a potent hexokinase 2 (HK2) inhibitor with an IC50 of 56.4 nM. HK2-IN-3 reduces glucose uptake and downregulated GLUT1/GLUT4 in oral squamous cell carcinoma (OSCC). HK2-IN-3 induces mitophagy and apoptosis. HK2-IN-3 suppresses tumor growth and angiogenesis in OSCC xenograft mouse models. HK2-IN-3 can be used for OSCC research .
|
-
- HY-181816
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-60 is the counterpart of the small-molecule immuno-probe [ 18F] LG‑8, and the two together enable integrated immuno-diagnosis and therapy. PD-1/PD-L1-IN-60 exhibits potent anti-tumor activity in mouse models of melanoma and lung cancer with high PD‑L1 uptake. PD-1/PD-L1-IN-60 can be used for relevant research on melanoma and lung cancer .
|
-
- HY-182067
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
Ferroptosis
|
Cancer
|
|
anti-TNBC agent-15 is a platinum (IV) complex with anti-triple-negative breast cancer activity. anti-TNBC agent-15 inhibits cancer cell viability. anti-TNBC agent-15 reverses the resistance of triple-negative breast cancer cells to Cisplatin (HY-17394), increases intracellular uptake, and effectively triggers apoptosis by inducing DNA damage, enhancing intracellular ROS accumulation and activating the mitochondrial pathway. anti-TNBC agent-15 enhances lipid peroxidation, interferes with the signal transduction of the cystine/glutamate transporter-glutathione peroxidase axis, and induces ferroptosis. anti-TNBC agent-15 significantly inhibits tumor growth in triple-negative breast cancer/Cisplatin xenograft models. anti-TNBC agent-15 can be used for the research of triple-negative breast cancer .
|
-
- HY-179631
-
|
|
Apoptosis
|
Cancer
|
|
2DG-ODDA is a 2-deoxyglucose (2-DG) (HY-13966) derivative with potent antitumor activity. 2DG-ODDA induces apoptosis, and reduces ATP production. 2DG-ODDA is taken up through both fatty acid and glucose transporters and is cleaved by α-Mannosidase (HY-P2950), releases 2DG to inhibit N-glycosylation and disrupt cellular metabolism. 2DG-ODDA inhibits tumor growth in a 4T1 mouse model. 2DG-ODDA can be used for the research of triple-negative breast cancer (TNBC) .
|
-
- HY-13774
-
|
|
P-glycoprotein
BCRP
|
Cancer
|
|
WK-X-34 is a low-toxicity, highly effective multidrug resistance reversal agent. By potently inhibiting the transport functions of P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP), WK-X-34 significantly increases the intracellular accumulation of anticancer drugs and radiotracers in drug-resistant cells. WK-X-34 exerts no significant effect on MRP transporters. WK-X-34 not only restores the chemosensitivity of multidrug-resistant ovarian cancer cells, but also significantly enhances the uptake of 99mTc-Sestamibi in P-gp-positive xenograft tumors, brain and intestinal tissues. WK-X-34 exhibits extremely low toxicity and favorable safety profiles both in vitro and in mice (at doses up to 50 mg/kg), and can be used for research on overcoming multidrug resistance in ovarian cancer .
|
-
-
-
HY-L083
-
|
|
3,552 compounds
|
|
Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.
MCE provides a unique collection of 3,552 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D1063
-
|
|
Fluorescent Dyes
|
|
IR-780 is a near-infrared fluorescent probe for in vivo imaging of tumor cells. IR-780 is transported into tumor cells via OATPs and ABCB10, with uptake dependent on glycolytic activity and plasma membrane potential. IR-780 preferentially accumulates in tumor cell mitochondria, including those of drug-resistant cancer cells, without chemical conjugation. IR-780 generates reactive oxygen species (ROS), induces hyperthermia and apoptosis, inhibits tumor growth and recurrence, and modulates HSP70 expression upon ultrasound or 808 nm laser exposure. IR-780 acts as a sonosensitizer, photodynamic and photothermal agent, and drug delivery carrier, with low acute imaging-dose toxicity and rapid vital organ clearance. IR-780 can be used for the research of cancer, such as breast cancer, lung cancer, and non-small cell lung cancer (NSCLC) .
|
-
- HY-D2281
-
|
|
Fluorescent Dyes
|
|
FAP Ligand 2, a FAPI-46 derivative, is a specific fibroblast activation protein (FAP)-targeted tracer. FAP Ligand 2 exhibits good tumor uptake and acts as a promising molecular tracer for FAP tumor imaging .
|
| Cat. No. |
Product Name |
Type |
-
- HY-159067
-
|
DEAE-dextran, MW 500000 hydrochloride, from bacterial (Leuconostoc mesenteroides); Diethylaminoethyl-dextran, MW 500000 hydrochloride
|
Biochemical Assay Reagents
|
|
DEAE-dextran, MW 500000 hydrochloride (DEAE-dextran, MW 500000 hydrochloride, from bacterial (Leuconostoc mesenteroides)) is a high-molecular-weight positively charged polymer that significantly enhances the uptake of viral RNA by tissue culture cells. When employed in the delivery system for "tumor immunity" RNA-splenocyte transfer, DEAE-dextran can markedly extend the lifespan of tumor-bearing animals, comparable to that of actively immunized animals. Furthermore, DEAE-dextran serves as a complexing agent for nucleic acids, forming composite particles with DNA/RNA for extensive applications in gene delivery. Additionally, DEAE-dextran can be utilized as a coating for liposomes .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5321
-
|
|
FGFR
|
Cancer
|
|
bFGF (119-126) is a ligand of bFGF. The complex formed by bFGF (119-126) and bFGF can bind to FGFR1, while inhibiting the bFGF-FGFR1 interaction, FGFR1 phosphorylation and downstream signaling pathways. Therefore, bFGF (119-126) induces cell apoptosis and inhibits cell proliferation, migration, angiogenesis and metastasis. When conjugated with a carrier, bFGF (119-126) enhances cellular uptake via FGFR-mediated endocytosis and serves as an effective FGFR-targeted ligand. When used in combination with ultrasound and Doxorubicin (HY-15142A), bFGF (119-126) significantly enhances the inhibitory effect on tumors. bFGF (119-126) is applicable to research related to lung cancer, breast cancer, glioblastoma and ovarian cancer .
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- HY-P5126
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 and 68 Ga-DOTA-LM3. 68 Ga-DOTA-LM3 shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis . DOTA-LM3 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-P5362
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Neurological Disease
Cancer
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NODAGA-LM3 is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC50 = 1.3 nM). NODAGA-LM3 does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 shows low uptake in normal tissues such as the liver and spleen, but high uptake in the lungs and blood pool. 68Ga-labeled NODAGA-LM3 can serve as a PET imaging agent for well-differentiated neuroendocrine tumors, and is applied in studies related to small cell lung cancer and well-differentiated neuroendocrine tumors .
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- HY-P1723
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Spexin
2 Publications Verification
Neuropeptide Q
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Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
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Cardiovascular Disease
Neurological Disease
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Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
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- HY-P5126A
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 TFA is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 TFA and 68 Ga-DOTA-LM3 TFA. 68 Ga-DOTA-LM3 TFA shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 TFA can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis . DOTA-LM3 (TFA) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-P1848
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Interleukin Related
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Cancer
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Pep-1 (uncapped) is a specific ligand of IL-13Ra2. Pep-1 (uncapped) exerts cell penetrating activity through receptor-mediated endocytosis, can cross the blood-tumor barrier (BTB) and target glioma cells. Pep-1 (uncapped) can enhance the uptake of nanoparticles by tumor cells and enhance the cell penetration ability of nanoparticles, and can be used to develop targeted drug delivery systems for glioma .
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- HY-P10781
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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PSMA-D5 has a binding affinity for PSMA with a Ki of 0.21 nM and can be used for PSMA tracing after radiolabeling. PSMA-D5 ([68Ga]-labeled) contains a DOTA chelator, allowing convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. PSMA-D5 ([68Ga]-labeled) shows excellent pharmacokinetic properties, exhibiting remarkable tumor uptake in 22Rv1 tumors . PSMA-D5 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-P10444
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Radionuclide-Drug Conjugates (RDCs)
CXCR
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Cancer
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DOTA Conjugated JM#21 derivative 7 (compound Ligand-7) is a derivative of CXCR4 targeting peptide conjugated with DOTA and can be used to produce radioligands. Radiolabeled DOTA Conjugated JM#21 derivative 7, i.e., 177Lu-DOTA, has excellent CXCR4 tumor targeting. In vitro biodistribution results of 177Lu-DOTA showed very low uptake in all non-targeted organs except kidney . DOTA Conjugated JM#21 derivative 7 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-159771
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FAP
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Cancer
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FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a Kd of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as 177Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with 111In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.
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- HY-P5362A
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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NODAGA-LM3 TFA is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC50 = 1.3 nM). NODAGA-LM3 TFA does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 TFA shows low uptake in normal tissues such as the liver and spleen, but high uptake in the lungs and blood pool. 68Ga-labeled NODAGA-LM3 TFA can serve as a PET imaging agent for well-differentiated neuroendocrine tumors, and is applied in studies related to small cell lung cancer and well-differentiated neuroendocrine tumors .
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- HY-P10239A
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Radionuclide-Drug Conjugates (RDCs)
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Cancer
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Tyr3-Octreotate acetate is a somatostatin analog. Tyr3-Octreotate acetate exhibits high uptake into tumor, that is capable to be labeled with radioactive metal and thus exhibits antitumor efficacy. Tyr3-Octreotate acetate can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .
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- HY-P11265
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GnRH Receptor
Fluorescent Dye
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Cancer
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YQGN-7 is a targeted fluorescent probe for the gonadotropin-releasing hormone receptor (RnRHR). YQGN-7 exhibits high selectivity and affinity for breast cancer cells (KD = 217.8 nM). YQGN-7 achieves precise visualization of the primary and metastatic lesions of breast cancer by targeting the highly expressed GnRHR in tumor cells. YQGN-7 can be used in the research of breast cancer breast-conserving surgery (BCS) .
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- HY-158266
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LNC1003
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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DOTA-PSMA-EB-01 (Compound LNC1003) is a specific inhibitor of PSMA (IC50= 10.77 nM).DOTA-PSMA-EB-01 enhances the uptake and retention time of 177Lu in tumors . DOTA-PSMA-EB-01 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-P1723A
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Neuropeptide Q TFA
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Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
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Cardiovascular Disease
Metabolic Disease
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Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
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- HY-P10873
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Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
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Cancer
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ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
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- HY-P11591
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PSMA-DOTA-PEI2
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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PDI2 (PSMA-DOTA-PEI2) is a prostate-specific membrane antigen (PSMA) ligand that acts as a tumor retention agent, renal uptake reducer, imaging agent and antitumor agent, applicable in SPECT diagnostic imaging and radiotheranostics. PDI2 specifically binds to PSMA on prostate cancer cells, enters cells via clathrin-dependent endocytosis, and exhibits higher tumor retention rate and lower renal uptake level. PDI2 is applicable in research related to prostate cancer and castration-resistant metastatic prostate cancer .
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- HY-P10794
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Peptides
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Cancer
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LH2 peptide is a pH-responsive cell-penetrating peptide dimer with the amino acid sequence LHHLCHLLHHLCHLAG. It can increase its uptake in tumor cells under weakly acidic conditions (such as the tumor microenvironment) through the protonation of histidine residues (pKa approximately 6). When conjugated with the anticancer drug Paclitaxel (HY-B0015), the PTX-LH2 conjugate showed superior tumor suppression effects compared to paclitaxel alone in a subcutaneous breast tumor model. The LH2 peptide holds potential as a drug delivery vehicle in cancer research .
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- HY-P11737
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Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
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Cancer
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IPM-N001 is a carbonic anhydrase IX (CAIX) ligand with a Kd value of <0.0337 nM for hCAIX. When radio-conjugated with 68Ga, IPM-N001 serves as a CAIX-targeted radionuclide tracer. [ 68Ga]Ga-IPM-N001 exhibits excellent tumor uptake and significantly improves the tumor-to-background ratio in PET/CT imaging studies using OS-RC-2 tumor-bearing mice. IPM-N001 can be used for the research of clear cell renal cell carcinoma .
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- HY-P0036D
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Drug Derivative
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
Apoptosis
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Cancer
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NOTA‑Octreotide is a selective SSTR2‑targeting PET tracer. NOTA‑Octreotide binds specifically to SSTR2 and accumulates in SSTR2‑expressing tissues. NOTA‑Octreotide enables effective imaging of somatostatin receptor‑positive tumors in mice and shows high specific uptake in SSTR2‑expressing organs in healthy rats. NOTA-Octreotide can be used for PET imaging investigation of neuroendocrine tumors. .
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- HY-P11781A
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Drug Derivative
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Cancer
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Cys-HW12 is a random peptide containing an N-terminal cysteine. Cys-HW12 can be coupled via the thiol group of Cys. Cys-HW12 can serve as a control for GE11 (HY-P10128)-conjugated mixed micelles targeting EGFR, and also functions as a cytotoxic agent, cellular uptake inhibitor, and tumor growth inhibitor. Cys-HW12 is applicable to pancreatic cancer-related research .
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- HY-P11594
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Neurotensin Receptor
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Cancer
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JMV 7490 is a highly potent and highly hydrophilic neurotensin receptor NTS1 probe that can be successfully labeled with 68Ga and 111In. JMV 7490 acts as an efflux inhibitor to reduce its efflux in NTS1-positive cancer cells; it also serves as an internalization inducer and is efficiently and continuously internalized by NTS1-positive cancer cells. 111In-radiolabeled JMV 7490 shows persistent uptake in NTS1-positive xenografts in nude mice, but no significant uptake in NTS1-negative xenografts. JMV 7490 can be used for in vivo tracer applications of NTS1-positive tumors and supports related research on colorectal cancer .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P99974
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Nanoparticle albumin-bound Paclitaxel; Nanoparticle albumin-bound ABI-007
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Microtubule/Tubulin
Apoptosis
Autophagy
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Cancer
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Nab-Paclitaxel (Nanoparticle albumin-bound Paclitaxel) is an albumin-bound nanoparticle formulation of Paclitaxel (HY-B0015). Nab-Paclitaxel is composed of albumin and the active pharmaceutical ingredient Paclitaxel, in which human albumin is used as an excipient to disperse and stabilize particles and carry the main drug. Nab-Paclitaxel is a solvent-free taxane with higher response rates and improved tolerability. Nab-Paclitaxel displays less toxicity and greater antitumor activity. Nab-Paclitaxel is more readily available for tumor cell uptake in three rhabdomyosarcoma, seven neuroblastoma cell lines, and one ostersarcoma cell line Nab-Paclitaxel can be studied in cancer research for example breast cancer and solid tumors. (The product specifications below only indicate the effective content of Paditaxel, the actual albumin quality depends on the batch; the ratio of each ingredient in this product is Paditaxel: albumin -1:7~1:11) .
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(5)
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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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(5)
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- HY-P992339
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Radionuclide-Drug Conjugates (RDCs)
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Cancer
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cT84.66 is a highly efficient tumor-targeting agent against carcinoembryonic antigen (CEA). cT84.66 engages in bivalent binding with CEA via variable region antigen-binding sites, enabling precise targeting of CEA-producing tumor cells for delivery of therapeutic radiation. cT84.66 exhibits high tumor uptake rate, rapid clearance rate, and excellent tumor-to-blood ratio. With dual functions as an imaging agent and an antibody-directed radiotherapy agent, cT84.66 is widely used in studies of colorectal cancer and metastatic CEA-positive malignancies .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N2040
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- HY-N6924
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Infection
Structural Classification
Panax notoginseng (Burkill) F. H. Chen ex C. H. Chow
Classification of Application Fields
Panax japonicas C. A. Mey.
Metabolic Disease
Plants
Disease Research Fields
Saccharides
Araliaceae
Source Classification
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HIV
PIN1
Fungal
GLUT
Reactive Oxygen Species (ROS)
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Zingibroside R1 is an orally active triterpene saponin with multiple biological activities including antioxidant, anti-inflammatory, antiviral, and metabolic regulatory properties. Zingibroside R1 reduces the expression of PIN family members, inhibits the expression of PLT1/PLT2, WOX5, SHR, and SCR, disrupts auxin transport and distribution, triggers plant ROS responses, and inhibits root growth. Zingibroside R1 extends the lifespan of Caenorhabditis elegans, enhances its heat stress resistance, and improves its motor ability. Hydrogel derivatives of Zingibroside R1 inhibit the proliferation of Candida albicans by binding to its β-1,3-glucan and exhibit antifungal activity. Zingibroside R1 inhibits GLUT1-mediated uptake and alleviates liver injury. Zingibroside R1 can be used in research related to neurodegenerative diseases, vulvovaginal candidiasis, acute liver injury, Ehrlich ascites tumor and HIV-1 infection .
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- HY-N3055
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Cupressaceae
Classification of Application Fields
Terpenoids
Diterpenoids
Plants
Disease Research Fields
Calocedrus decurrens (Torr.) Florin
Source Classification
Cancer
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Apoptosis
AMPK
Platelet-activating Factor Receptor (PAFR)
Caspase
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Pinusolide is an AMPK activator and PAF receptor antagonist. Pinusolide activates AMPK, phosphorylates ACC, enhances IRS-1 tyrosine phosphorylation, boosts glucose uptake, and modulates insulin signaling. Pinusolide inhibits caspase-3/7 activation, intracellular calcium elevation, reactive oxygen species overproduction, lipid peroxidation, and tumor cell proliferation. Pinusolide stabilizes superoxide dismutase activity, reduces apoptotic hallmarks, induces mitochondrial pathway apoptosis, and triggers DNA fragmentation. Pinusolide can be used for the research of type 2 diabetes, neurodegenerative diseases, acute lymphoblastic leukemia, acute myeloid leukemia, and Burkitt lymphoma .
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