Cancer Targeted Therapy

Enpp-1-IN-4 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). Enpp-1-IN-4 has the potential for the research of cancer diseases (extracted from patent WO2019177971A1, compound 1).

BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with K_i value of > 40 µM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease.

DPPE-PEG2000-NGR (DPPE-PEG2000-Mal-Cys-NGR) is a functionalized PEGylated phospholipid conjugate composed of three modular components: 1,2-dipalmitoyl-sn-glycerol-3-phosphate ethanolamine (DPPE) as a lipid anchoring group, a 2000 Da polyethylene glycol (PEG) spacer arm, and an NGR (HY-P1043) peptide as a terminal targeting/functional ligand. DPPE-PEG2000-NGR can be used for tumor angiogenesis-targeted drug delivery.

MC-PSE is a fluorescent probe that can be used for glutathione (GSH) detection, NIR-II fluorescence imaging and ratiometric photoacoustic imaging. MC-PSE spontaneously forms J-aggregates in aqueous solution through π-π stacking, and its phenylselenyl group acts as a fluorescence quencher and GSH recognition receptor, thereby eliminating intrinsic fluorescence and generating a maximum absorption peak at 1000 nm. The excitation/emission wavelengths of MC-PSE are Ex = 808 nm and Em = 940 nm. MC-PSE can be applied in tumor-related research.

NYLTHRQ is a peptide. NYLTHRQ specifically blocks the interaction between sVEGFR1-i13 and β1 integrin, and inhibits the activation of VEGFR1 and VEGFR2. NYLTHRQ inhibits cancer cell proliferation. NYLTHRQ can be used in the research of tumors such as lung squamous cell carcinoma.

hsa-miR-4463 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.

hsa-miR-548i 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.

BTK ligand 1 (compound 1) is a ligand targeting Bruton’s tyrosine kinase (Btk). BTK ligand 1 can combine with E3 ligase ligand (Ligand for E3 Ligase) through PROTAC Linker to form PROTAC. PROTACs targeting Btk can be used in the study of chronic lymphocytic leukemia (CLL) and other BK cell malignancies.

5-(2-Azidoethyl)uridine 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. 5-(2-Azidoethyl)uridine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

hsa-miR-933 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-421-5p 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.

mmu-miR-7014-3p 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-3548 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 2,3,5-tri-O-benzyl-D-ribofuranoside 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.

S-acetyl-PEG20-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

DSPE-PEG34000-NGR is a PEG compound which composed of DSPE and an Asn-Gly-Arg (NGR) peptide. NGR peptide can target tumor vascular antigen CD13. DSPE-PEG3400-NGR can be used for drug delivery.

KB02-amide-PEG2-C2-acid is a synthesized E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs, such as KB02-SLF (HY-129610).

Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) is an anti-leukemic agent with potent ribosome-targeting protein synthesis inhibition. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) downregulates short-lived oncoproteins, including c-Myc and Mcl-1, by inhibiting protein synthesis. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) induces cell cycle arrest at the G0/G1 phase and triggers mitochondrial pathway-mediated apoptosis in acute myeloid leukemia (AML) cells. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) is applicable for research on leukemia.

PROTAC NSD2 degrader-1 is a PROTAC degrader that selectively targets NSD2, with a DC₅₀ of 0.37 μM. PROTAC NSD2 degrader-1 induces selective degradation of long and short isoforms of NSD2 containing the PWWP1 domain by forming a ternary complex with FBXO22. NSD2 degradation mediated by PROTAC NSD2 degrader-1 depends on the ubiquitin-proteasome system and the neddylation pathway. PROTAC NSD2 degrader-1 can be used in cancer-related research such as non-small cell lung cancer, multiple myeloma and prostate cancer.

HDAC6-IN-17 (compound 5b) is a potent HDAC6 inhibitor with IC₅₀ values of 150 nM, 1400 nM, and 2300 nM for HDAC6, HDAC8, and HDAC4, respectively. HDAC6-IN-17 has cytotoxic activity on human cancer cell lines. HDAC6-IN-17 can be used in research of cancer.