Cancer Targeted Therapy
Cancer targeted therapy is the foundation of precision medicine; it uses drugs or other substances to target specific genes and proteins that control cancer cells’ growth, division and spreading. Compared to traditional chemotherapy drugs, targeted-drugs can specifically act on cancer cells with high efficacy without damaging normal cells. Drugs used in cancer targeted therapy mainly includes small molecules and macromolecules (e.g., monoclonal antibodies), which can target cancer cells and constituents in the tumor microenvironment to activate the immune system. Anti-angiogenesis drugs, such as those targeting vascular endothelial growth factor (VEGF), epidermal growth factor receptor (EGFR), transforming growth factor (TGF)-α, TGF-β, Tumor necrosis factor (TNF)-α, and platelet-derived endothelial growth factor (PDGFR) inhibit the proliferation and metastasis of cancer cells. In recent years, the proportion of antibody drugs in cancer treatment has gradually become prominent. Antibody-drug conjugates (ADCs) are a new type of targeted drugs that are composed of monoclonal antibody, cytotoxic drug and linker. ADCs can deliver drugs to tumor cells and minimize the toxicity to normal tissues. Proteolysis-targeting chimera (PROTAC) is a useful technology for targeted protein degradation. PROTAC exploits the ubiquitin-proteasome system and forms a ternary complex with a hijacked E3 ubiquitin ligase and target protein, leading to polyubiquitination and degradation of the target protein.
Targeted therapy is a useful strategy in treatment of cancer either alone or in combination with standard chemotherapy. At present, targeted therapy has proved significant clinical success in the treatment of many types of cancer, including breast cancer, colorectal cancer, leukemia, ovarian cancer and lung cancer.
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Yatein
0 ImagesCat. No.: HY-N1060CAS No.: 40456-50-6Yatein is a lignan isolated from A. chilensis, with antiproliferative activity. Yatein suppresses herpes simplex virus type 1 (HSV-1 ) replication by interruption the immediate-early gene expression.
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1,1,1-Trifluoroethyl-PEG2-propargyl
0 ImagesCat. No.: HY-140886CAS No.: 1835759-73-31,1,1-Trifluoroethyl-PEG2-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. 1,1,1-Trifluoroethyl-PEG2-propargyl 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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BMPR2-IN-1
0 ImagesCat. No.: HY-154970BMPR2-IN-1 (Compound 8a) is a BMPR2 inhibitor with an IC50 of 506 nM and a KD of 83.5 nM. BMPR2-IN-1 can be used for research of pulmonary arterial hypertension, Alzheimer’s disease and cancer.
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MU876
0 ImagesCat. No.: HY-175812CAS No.: 1208829-24-6MU876 (Compound 32) is a MUS81 inhibitor with an IC50 of 0.5 μM. MU876 effectively inhibits MUS81-dependent homologous recombination (HR) and break-induced replication (BIR) pathways. MU876 sensitizes cancer cells to DNA-damaging agents, such as Cisplatin (HY-17394), through impairing their ability to repair DNA lesions. MU876 can be used for cancers chemotherapy research.
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Apocynin-d3
0 ImagesCat. No.: HY-N0088SCAS No.: 80404-23-5Synonyms: Acetovanillone-d3Apocynin-d3 is the deuterium labeled Apocynin. Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM.
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Dihydroevocarpine
0 ImagesDihydroevocarpine induces cytotoxicity in acute myeloid leukemia via suppressing the mTORC1/2 activity.
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Sanggenon G
0 ImagesCat. No.: HY-12372CAS No.: 85698-31-3Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspase activation.
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Idelalisib-d5
0 ImagesSynonyms: CAL-101 d5; GS-1101 d5Idelalisib-d5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor.
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Gluconate sodium (Standard)
0 ImagesSynonyms: D-Gluconic acid sodium salt (Standard); Sodium D-gluconate (Standard); D-Gluconate sodium salt (Standard)Gluconate (D-Gluconic acid) (Standard) is the analytical standard of Gluconate sodium (HY-B1092A). This product is intended for research and analytical applications. Gluconate (D-Gluconic acid) sodium is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury.
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Neocryptomerin
0 ImagesNeocryptomerin, a biflavonoid, shows inhibitory activity against U251, MCF-7, HeLa cell. Neocryptomerin has favorable binding affinities in the active pocket of SARS-CoV-2. Neocryptomerin is the leading compound of rational compounds against COVID-19.
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hsa-miR-367-5p inhibitor
0 ImagesCat. No.: HY-RI00786hsa-miR-367-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
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LP-184
0 ImagesLP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).
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NCDM-32B
0 ImagesCat. No.: HY-120766CAS No.: 1239468-48-4NCDM-32B is a potent and selective KDM4 inhibitor, with IC50 values of 3.0 μM for KDM4A and 1.0 μM for KDM4C in in vitro enzyme assays. NCDM-32B specifically increases global H3K9me3/me2 levels in basal breast cancer cells. NCDM-32B impairs the viability of KDM4C-amplified basal breast cancer cell lines (HCC1954 and Colo824). NCDM-32B can be used for the study of breast cancer.
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BPR1R024 mesylate
0 ImagesCat. No.: HY-132935ACAS No.: 2763365-40-6BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology.
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PKI (14-24)amide
0 ImagesCat. No.: HY-P3929CAS No.: 100853-61-0PKI (14-24)amide is a potent PKA inhibitor. PKI (14-24)amide strongly inhibited cyclic AMP-dependent protein kinase activity in the cell homogenate.
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GW583340 dihydrochloride
0 ImagesCat. No.: HY-103439CAS No.: 1173023-85-2GW 583340 dihydrochloride is an orally active ErbB-2/EGFR tyrosine kinase inhibitor. GW 583340 dihydrochloride exhibits antitumor activity in xenograft models with EGFR overexpression or ErbB-2 overexpression. GW 583340 dihydrochloride is applicable to research related to head and neck cancer, breast cancer, and gastric cancer.
