Cancer Targeted Therapy

Napabucasin analogue is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Napabucasin analogue can be used in synthesis Napabucasin (HY-13919).

GPX4-IN-11 (compound I14) is a potent inhibitor of GPX4, with the K_D of 45.7 μM. GPX4-IN-11 plays an important role in ferroptosis research.

Thalidomide-N-C-piperidine-C7-Br, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. Thalidomide-N-C-piperidine-C7-Br can be used in the synthesis of ZS3-046 (HY-176457).

Jaceidin is a promising lead molecule for potent VEGFR inhibitor with excellent membrane permeability and oral bioavailability. Jaceidin exhibits anti-tumor activities.

Hydroxy-PEG24-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

hsa-miR-548f-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

Sodium acetate trihydrate, United States Pharmacopeia (USP) Reference Standard (Sodium acetate trihydrate (Pharmaceutical primary standard, USP)) is a carboxylic acid and short-chain fatty acid (SCFAs). Sodium acetate trihydrate activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Sodium acetate trihydrate exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Sodium acetate trihydrate regulates energy metabolism. Sodium acetate trihydrate has anticancer activity against gastric cancer. Sodium acetate trihydrate induces writhing reaction and ulcerative colitis. Sodium acetate trihydrate can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.

ZYJ-34v is an orally active histone deacetylase inhibitor. ZYJ-34v has antitumor activity.

N-(Biotin-PEG4)-N-bis(PEG4-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

hsa-miR-3158-5p 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.

Bis-methacrylate-PEG5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

DSPE-PEG1000-Mal-CLPLIPTHIISFS is a PEG compound composed of DSPE and the liver cancer targeting peptide SP94 (HY-P11050A) (sequence SFSIIHTPILPL). SP94 exhibits specific binding to hepatocellular carcinoma (HCC) cells. DSPE-PEG1000-Mal-CLPLIPTHIISFS can be used to prepare lipid nanoparticles to form liver cancer-targeting nanocarriers.

UNPD139734 is a CDK-1 inhibitor and PARP-1 inhibitor that forms stable complexes with each target protein. UNPD139734 serves as a lead compound for structural optimization to develop dual-target anticancer agents targeting CDK-1 and PARP-1. UNPD139734 can be used for the research of breast cancer.

MC-AcLys-GDEVD-PABC-Exatecan (MC-AcLys-GDEVD-PABC-DX8951) is a agent-linker conjugate for ADC. MC-AcLys-GDEVD-PABC-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with a novel caspase-3 cleavable peptide linker MC-AcLys-GDEVD-PABC linker. MC-AcLys-GDEVD-PABC-Exatecan can be used to prepare DX8951 antibody conjugate (ADC), and it exhibites significant bystander effect mediated by the caspase-3-triggered extracellular cleavage of the linker, enhancing payload release into the tumor microenvironment.

mmu-miR-3971 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.

mmu-miR-7013-3p 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.

rno-miR-3544 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.

SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation.

XF056-132 (MS132N TFA) is an inactive WDR5 PROTAC degrader with a K_d value of 106 nM against human targets, and exhibits no significant binding to the VHL complex, serves as a negative control for MS132. XF056-132 binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 can be used in the research of pancreatic ductal adenocarcinoma.

5’-O-Benzoyl-2’,3’-di-O-acetyl-4’-C-fluoromethyluridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc.