Cancer Targeted Therapy

hsa-miR-1290 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.

Methyl 2,5-dihydroxycinnamate is an erbstatin analog and a stable, potent inhibitor of EGFR kinase activity.

ADC Control Human IgG1-tirumotecan is an antibody-drug conjugate (ADC). The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is TL033 TFA (HY-147340A). ADC Control Human IgG1-tirumotecan can be as a control of Sacituzumab tirumotecan (HY-164789).

hsa-miR-1301-3p 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.

Deltasonamide 1 is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a K_D of 203 pM. Deltasonamide 1 can be used for the research of tumors.

NH2-UAMC1110 is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose-response, and has been used for tumor diagnosis. NH2-UAMC1110 introduces an active amino group into its structure, enabling it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.), thereby synthesizing molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling processes. Its key activity is high targeting and high affinity, and its core function is to be coupled with bifunctional chelators (such as DOTA, DATA5m) as a targeting module. NH2-UAMC1110 can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis.

HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo.

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1?(HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC₅₀ of 39.2 nM.

(S)-WSD0628 (Compound 28) is the S-isomer of WSD0628 (HY-162002). (S)-WSD0628 is the inhibitor for ATM that inhibits the phosphorylation of ATM in MCF-7 cell with IC₅₀ <100 nM. (S)-WSD0628 exhibits radiosensitizing activity. (S)-WSD0628 can cross blood-brain barrier.

m-PEG3-0-benzaldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

STAT3-IN-31 (compound K2071) is a STATtic-derived STAT3 and mitotic inhibitor. STAT3-IN-31 blocks mitotic progression and affects the formation of mitotic spindles. STAT3-IN-31 also affects glioblastoma cell migration and inhibits cell proliferation in tumor spheroids. STAT3-IN-31 is also able to induce glioblastoma senescence, inhibit the growth of Temozolomide (HY-17364)-resistant cells and the secretion of the pro-inflammatory cytokine monocyte chemoattractant protein MCP-1.

HPK1-IN-19 (Compound I-47) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor.

MDM2-IN-23 (compound 5d) is an inhibitor of MDM2. MDM2-IN-23 has an IC₅₀ of 60.09 μM on MCF-7 cells.

E16-uPA24 is a chimeric peptide targeting urokinase-type plasminogen activator receptor (uPAR). E16-uPA24 modifies senescent cells surface with polyglutamic acid, promoting immune cell-mediated responses through glutamate recognition. E16-uPA24 induces immune clearance of senescent cells and restores tissue homeostasis by enhancing immune cells recruitment and directly coupling senescent cells and immune cells. E16-uPA24 can be used for tissue degeneration, chronic inflammatory disease and age-related tumorigenesis research.

CH2COOH-PEG6-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

DJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC₅₀ values:5 and 50 nM) and MRCKα/β (IC₅₀ values:10 and 100 nM). DJ4 blocks stress fiber formation and inhibits migration and invasion of cancer cells. DJ4 can be used for study of lung cancer, breast cancer, and pancreatic (PANC-1) cancer.

Cucurbitacin B (Standard) is the analytical standard of Cucurbitacin B. This product is intended for research and analytical applications. Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids and is oral active. Cucurbitacin B inhibits tumor cell growth, migration and invasion and cycle arrest, but induces cell apoptosis. Cucurbitacin B has potent anti-inflammatory, antioxidant, antiviral, hypoglycemic, hepatoprotective, neuroprotective activity.

LARLLT TFA is an EGFR-binding peptide. LARLLT has the potential for research of EGFR overexpressing cancers, such as lung, ovarian and colorectal cancer.

Cobomarsen (MRG-106) is an oligonucleotide inhibitor of miR-155. Cobomarsen inhibits multiple gene pathways associated with cell survival (including JAK/STAT, MAPK/ERK and PI3K/AKT). Cobomarsen can be used for the research of B-cell lymphoma.

AZ-PRMT5i-1 (Compound 28) is an effective and orally active MTAP-selective PRMT5 inhibitor. AZ-PRMT5i-1 also demonstrates MTA cooperativity and exhibits both in vitro and in vivo antitumor activities, and can be used to study MTAP-deficient cancers.