Cancer Targeted Therapy

EGFR-IN-73 (Compound 3f) is a potent inhibitor for the most common EGFR mutation EGFR Del19 with an IC₅₀ of 119 nM.

1-β-D-Arabinofuranosyl-5-bromo-2,4(1H,3H)-pyrimidinedione 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.

PROTAC SOS1 degrader-9 (Compound 10) is a SOS1 PROTAC degrader. PROTAC SOS1 degrader-9 can be used in cancer research.

CA IX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC₅₀ values of 41 and 48 nM, respectively. CA IX/VEGFR-2-IN-3 exhibits anticancer activity, inhibiting the growth of MCF-7 breast cancer cells (with an IC₅₀ of 22.33 μM) and mouse fibroblast cell line 3T3 (where cell viability is less than 40% at a concentration of 100 μM). CA IX/VEGFR-2-IN-3 can be used for research in the field of cancer treatment.

hsa-miR-1199-5p 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.

hsa-miR-33b-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.

Propargyl-PEG4-5-nitrophenyl carbonate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Propargyl-PEG4-5-nitrophenyl carbonate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

m-PEG5-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

hsa-miR-4671-3p 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-6082 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.

hsa-miR-8086 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-365-2-5p 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-6996-5p 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.

rno-miR-31b 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.

DOPE-PEG2000-NGR (DOPE-PEG2000-Mal-Cys-NGR) is an amphiphilic lipid-PEG-peptide conjugate composed of DOPE (1,2-dioleoyl-sn-glycero-3-phosphoethanolamine), PEG2000, and the NGR (Asn-Gly-Arg) peptide, a tumor-homing tripeptide motif. NGR peptide specifically binds to aminopeptidase N (CD13) that is overexpressed on angiogenic tumor vasculature. DOPE-PEG2000-NGR is used for tumor vasculature-targeted drug delivery and anti-angiogenic research.

P-gp inhibitor 2 is a potent P-gp inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC₅₀=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300).

Laduviglusib-d₄ (CHIR-99021-d₄) is the deuterium labeled Laduviglusib (HY-10182). Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC₅₀s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy.

SJL2-1 is a PRMT5 inhibitor, with an IC₅₀ of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC).

Topoisomerase II-IN-25 (Compound 6a) is a selective inhibitor of topoisomerase II and has no inhibitory activity on topoisomerase I. Topoisomerase II-IN-25 exhibits significant anti-PC-3 cell activity. Topoisomerase II-IN-25 significantly increases intracellular ROS levels, inducing oxidative stress. Topoisomerase II-IN-25 causes depolarization of mitochondrial membrane potential and promotes cell apoptosis. Topoisomerase II-IN-25 blocks PC-3 cells in the G2/M phase. Topoisomerase II-IN-25 can be used for the study of prostate cancer.

POI ligand-6-Linker Conjugate is a hydrophobic tag conjugate that binds to HDAC6. POI ligand-6-Linker Conjugate, as a target protein ligand-linker conjugate, is used to synthesize the hydrophobic tag degrader (Hyt) HDAC6 degrader-6 (HY-189299). POI ligand-6-Linker Conjugate is used in the study of leukemia.