Cancer Targeted Therapy

hsa-miR-328-3p 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-1290 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.

HSD1590 is potent ROCK inhibitor, with IC₅₀s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (K_ds<2 nM). HSD1590 displays low cytotoxicity.

HLX-22 is a humanized monoclonal antibody targeting HER2. HLX-22 induces apoptosis in HER2-overexpressing breast and gastric cancer cells combined with Trastuzumab (HY-P9907). HLX-22 has potent antitumor activity against advanced solid tumors.

E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.

BC-1258，an F-box/LRR-repeat protein 2 (FBXL2) activator，can stabilize and upregulate FBXL2 levels. BC-1258 induces apoptosis of tumorigenic cells，and profoundly inhibits tumor formation in mice.

BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research.

Dihydrobaicalein is a PLK1 Inhibitor with an IC₅₀ of 6.3 μM. Dihydrobaicalein also inhibits VRK2 and PLK2. Dihydrobaicalein is a natural product that can be isolated from Scutellaria scandens.

NSC647889 is an apoptosis and autophagy inducer. NSC647889 induces apoptosis, inhibits mTOR pathway and abrogates DNA synthesis. NSC647889 triggers LC3-positive vesicle formation, modulates AKT and 4EBP1 phosphorylation and shows heightened caspase-3 activation in multicellular spheroids. NSC647889 can be used for the research of solid cancer tumour, head-neck carcinoma, and colorectal cancer.

N-(Amino-PEG3)-N-bis(PEG4-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

(7S)-BAY-593 is the S-enantiomer of BAY-593 (HY-161573). BAY-593 is an orally active GGTase-I inhibitor. BAY-593 can block YAP1/TAZ signaling in animals and has antitumor activity.

NVP-EVS459 is a Folate Receptor (FR)-targeting radioconjugate. NVP-EVS459 labeled with 177Lu can be used for tumor diagnosis and research.

mmu-miR-345-5p 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.

AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).

Piperacillin (Standard) is the analytical standard of Piperacillin. This product is intended for research and analytical applications. Piperacillin is a semisynthetic broad-spectrum β-lactam antibiotic which exhibits potent bactericidal activity against Gram-negative bacteria as well as select Gram-positive strains through penicillin-binding proteins. Piperacillin is most commonly used in combination with the β-lactamase inhibitor Tazobactam.

ARL-17477 is a dual inhibitor of NOS1and the autophagy-lysosomal system with anticancer activity and can inhibit tumor growth in KRAS-mutated cancers.

m-PEG15-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Shikonin (Standard) is the analytical standard of Shikonin. This product is intended for research and analytical applications. Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC₅₀ of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.

PTACH (NCH-51) is a potent HDAC inhibitor with IC₅₀s of 48 nM, 32 nM, and 41 nM for HDAC1, HDAC4, and HDAC6, respectively. PTACH exerts potent growth inhibition against various cancer cells (EC₅₀s of 1.1-9.1 μM) .

(2-Pyridyldithio)-PEG4-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.