Cancer Targeted Therapy

mmu-miR-669k-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-7673-3p 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.

DBCO-PEG9-DBCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. DBCO-PEG9-DBCO is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

B-Raf IN 5 (compound 3b) is a potent inhibitor of protein kinase B-Raf with an IC₅₀ of 2.0 nM. B-Raf IN 5 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease.

GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC₅₀ of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity.

6FC-GABA-Taxol is a fluorescent probe with cell permeability, which is formed by connecting 6FC to the anticancer drug Taxol (HY-B0015) via γ-aminobutyric acid (GABA). 6FC-GABA-Taxol can bind to microtubules in living cells and image them through confocal microscopy. Additionally, 6FC-GABA-Taxol enables the quantification of microtubule binding using flow cytometry without the addition of efflux inhibitors.

Pyrrocidine B (Compound 6), an alkaloid, is a microbial secondary metabolite. Pyrrocidine B can be isolated from the endophytic fungus Neonectria ramulariae Wollenw KS-246. Pyrrocidine B has significant cytotoxicity against leukemia cells (IC₅₀ of 4.6  μM for HL60 cells) with a weak Prolyl oligopeptidase (POP) inhibitory activity.

YQGN-7 is a targeted fluorescent probe for the gonadotropin-releasing hormone receptor (RnRHR). YQGN-7 exhibits high selectivity and affinity for breast cancer cells (K_D = 217.8 nM). YQGN-7 achieves precise visualization of the primary and metastatic lesions of breast cancer by targeting the highly expressed GnRHR in tumor cells. YQGN-7 can be used in the research of breast cancer breast-conserving surgery (BCS).

hsa-miR-3939 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-5694 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.

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

EGFR-IN-38 is a potent inhibitor of EGFR. EGFR-IN-38 is an anti-tumor agent with low toxic side effects. EGFR-IN-33 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-38 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 4).

ALK degrader 2 is an orally active ALK HyT degrader that degrades EML4-ALK levels (DC₅₀ = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC₅₀ = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)).

ST13, an ortho-hydroxyanilide, is a selective, slow- and tight-binding HDAC1 and HDAC2 inhibitor with IC₅₀s of 23 nM and 49 nM, respectively. ST13 shows a weak inhibition of HDAC3 (IC₅₀ = 4.30 μM) and HDAC6 (IC₅₀ > 10 μM). The induced fit mechanism of ST13 proceeds through a two-step process: first, the enzyme and inhibitor rapidly form a collision complex (EI), which then slowly transforms into the stable complex E*I. ST13 induces apoptosis in cancer cells. ST13 can be used for the study of melanoma and triple-negative breast.

Nemiralisib Succinate is a potent and highly selective PI3Kδ inhibitor with a pK_i of 9.9.

β-Glucuronidase/hCAII-IN-2 (Compound 12e) is a potent β-glucuronidase and hCA II inhibitor with an IC₅₀ of 670.7 μM and 21.77 μM, respectively.

5’-O-DMTr-N6-ethyl-2’-deoxyadenosine 3’-CED phosphoramidite 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.

mmu-miR-12187-3p 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.

mmu-miR-496a-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.

(E/Z)-MitoTam (iodide, hydriodide) (MitoTam (iodide, hydriodide)) is the E/Z mixture of MitoTam iodide, hydriodide. MitoTam iodide, hydriodide is a Tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells. MitoTam iodide, hydriodide causes apoptosis.