Cancer Targeted Therapy

ICMT-IN-5 (compound 46) is an inhibitor of ICMT (IC₅₀=0.3 μM).

hsa-miR-10396b-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.

hsa-miR-3190-3p 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.

N3-PEG16-Hydrazide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. N3-PEG16-Hydrazide 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.

rno-miR-3585-3p 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.

Amino-PEG6-amido-C16-COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

FLT3 ligand-2 is a Ligand for Target Protein for PROTAC. FLT3 ligand-2 can be used to synthesize PROTAC FLT-3 degrader 1 (HY-114323).

PRMT5 ligand 1 (compound 3) is the ligand for PRMT5 that can be used as target protein ligand for synthesis of PROTAC degrader MS4322 (HY-141877).

PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC₅₀ of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model.

mmu-miR-713 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.

Methoxsalen-¹³C,d₃ (8-Methoxypsoralen-¹³C,d₃) is the deuterium and ¹³C-labeled Methoxsalen (HY-30151). Methoxsalen (8-Methoxypsoralen) is a furanocoumarin compound used in psoralen, used in studies of psoriasis, eczema, vitiligo and some sun-exposed cutaneous lymphomas, and is a P450 inhibitor.

SphK2-IN-4 is a selective SphK2 inhibitor (IC₅₀=6.2 μM) with extremely low activity against SphK1 (IC₅₀ > 50 μM). SphK2-IN-4 exhibits broad-spectrum antiproliferative activity against colorectal cancer cells and induces apoptosis.

Mesenchymal-to-epithelial transition (MET) is a receptor tyrosine kinase for hepatocyte growth factor (HGF). MET overactivation is strongly associated with angiogenesis, cellular motility, growth, and invasion. Aberrant MET signaling can drive tumorigenesis in several cancer types through various molecular mechanisms, including MET amplification, MET exon 14 skipping mutation, MET overexpression, and MET fusions. MET L1195V is a mutant of MET. MET L1195V Recombinant Human Active Protein Kinase is a recombinant MET L1195V protein that can be used to study MET L1195V-related functions.

OICR-8268-acrylic acid is a ligand for E3 ubiquitin ligase. OICR-8268-acrylic acid can be connected to the ligand for protein by a linker to form OICR41114 (HY-169389). OICR41114 can be used in anti-cancer research.

BMS-577098 is an orally active and ATP-competitive insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC₅₀ of 0.016 μM. BMS-577098 shows anti-tumor effect.

hsa-miR-548a-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.

hsa-miR-6844 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.

mmu-miR-292b-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.

mmu-miR-677-3p 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.

Propargyl-PEG4-O-C1-NHS ester (compound 8) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG4-O-C1-NHS ester is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.