Cancer Targeted Therapy

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

STA-1474 is an orally active and highly selective HSP90 inhibitor, as well as a phosphate prodrug of the HSP90 inhibitor STA-9090 (HY-15205). STA-1474 disrupts the chaperone function of HSP90 and promotes the degradation of client proteins. STA-1474 inhibits the phosphorylation of Met, Akt and STAT3, thereby blocking related signaling pathways. STA-1474 induces apoptosis and inhibits proliferation of osteosarcoma cells, and triggers the up-regulation of HSP70 and HSP90. STA-1474 induces tumor regression and caspase-3 activation in mouse osteosarcoma xenograft models. STA-1474 can be used in the research of osteosarcoma.

Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct.

PDI-IN-5 (compound 30z) is an allosteric-covalent inhibitor targeting protein disulfide isomerase (PDI) with a 2-chloro-pyrrolopyrimidin-4-one scaffold, with an IC₅₀ of 0.4 μM. PDI-IN-5 exhibits selectivity for ERp57 and GPX4, and inhibits glioblastoma. PDI-IN-5 can be used in glioblastoma-related research.

(S)-Embibatinib ((S)-TERN-701), an isomer of TERN-701 (HY-182792), is a selective BCR-ABL allosteric inhibitor. (S)-Embibatinib can be usd for the research of cancer.

Swertiamarin (Standard) is the analytical standard of Swertiamarin. This product is intended for research and analytical applications. Swertiamarin is an orally active iridoid compound with hypoglycemic, hypolipidemic, anti rheumatic and antioxidant activities, which can be used in the research of diabetes and arthritis.

hsa-miR-1202 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.

Benzyl-PEG9-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

PROTAC HPK1 Degrader-4 is an orally active HPK1 PROTAC degrader and immune activator, with DC₅₀ values of 3.16 nM and 72.59 nM in Jurkat cells and PBMCs, respectively. PROTAC HPK1 Degrader-4 induces degradation via the ubiquitin-proteasome system, downregulates the HPK1-SLP76 signaling pathway, reduces the phosphorylation level of SLP76 (S376), and promotes immune activation. PROTAC HPK1 Degrader-4 can be used in the research of colorectal cancer and B-cell lymphoma.

Vps34-IN-5 is an orally active VPS34 inhibitor, 98% target inhibition, and an IC₅₀ categorized as B. Vps34-IN-5 induces additive or synergistic anti-proliferative activity with EGFR inhibitors in cancer cells. Vps34-IN-5 is administered orally alone or with Erlotinib (HY-50896) in mouse xenograft models. Vps34-IN-5 can be used for the research of non-small cell lung cancer.

CNTO-860 is a humanized anti-tissue factor monoclonal antibody. CNTO-860 can improve tumor control when combined with Paclitaxel (HY-B0015) in colon cancer model and significantly increase tumor-free survival.

NSC 330770, a demethylated hydrogenated molecule, is a potent tubulin polymerization inhibitor (IC₅₀ of 2 μM). NSC 330770 elicites GTPase activity and the formation of abnormal polymers.

LSD1-IN-16 (compound 4b) is a potent LSD1 inhibitor. LSD1-IN-16 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC₅₀ values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 displays cell growth arrest in prostate cancer LNCaP cells, with an IC₅₀ of 15.2 μM.

TA-DOTA-GA is a radionuclide conjugate (RDC), which is capable of binding to a radionuclide. RDC has the ability to specifically target biomolecules and can be used in medical imaging or therapy.

VEGFR-2-IN-61 (Compound 7b) is an inhibitor for VEGFR-2 with an IC₅₀ of 2.83 µM. VEGFR-2-IN-61 inhibits the proliferation of multi cancer cells (IC₅₀ for MCF-7 is 2.12 μM). VEGFR-2-IN-61 inhibits the cell migration, induces oxidative stress and apoptosis in MCF-7.

hsa-miR-199b-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-4423-3p 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.

hsa-miR-548ai 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-6850-3p 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-298-3p 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.