Cancer Targeted Therapy

MDM2-p53-IN-15 is a MDM2-p53 inhibitor with an IC₅₀ value of 26.1 nM. MDM2-p53-IN-15 inhibits the proliferation of various cancer cells and induces cell apoptosis. MDM2-p53-IN-15 can be used for the research of cancer.

5’-Azido-5’-deoxy-2’-O-methyluridine 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. 5’-Azido-5’-deoxy-2’-O-methyluridine 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.

(R)-ICMT-IN-3 (compound ent 2-27) is an inhibitor of ICMT (IC₅₀=0.01 μM).

Haspin-IN-4 (Compound 60) is a selective inhibitor of Haspin with an IC₅₀ value of 0.01 nM. Haspin-IN-4 possesses anticancer activity and can be used in cancer research.

IGF-1R inhibitor-5 (compound 19) is a potent inhibitor of IGF-1R, with the IC₅₀ of 6 μM. IGF-1R inhibitor-5 has the potential for the research of cancer.

VEGFR-2/P-gp-IN-1, a Licochalcone A (HY-N0372) derivative, is an orally active VEGFR-2 (IC₅₀ = 0.885 μM) and P-gp inhibitor. VEGFR-2/P-gp-IN-1 achieves anti-tumor proliferation and overcomes chemotherapy resistance by synchronously inhibiting VEGFR-2 kinase activity and P-gp drug efflux pump function. VEGFR-2/P-gp-IN-1 inhibits phosphorylation of VEGFR-2 and downstream PI3K/AKT signaling pathway proteins, induces apoptosis, blocks cells in the S phase, and inhibits invasive migration. VEGFR-2/P-gp-IN-1 exerts potent in vivo anti-tumor effects in the HeLa/DDP cell xenograft tumor model. VEGFR-2/P-gp-IN-1 is used in cervical cancer research.

HDAC6-IN-66 is a potent and selective histone deacetylase (HDAC) 6 inhibitor with an IC₅₀ of 1.8 nM. HDAC6-IN-66 induces α-tubulin acetylation over histone H3. HDAC6-IN-66 can be used for the research of cancer.

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

Abiraterone N-oxide-d₄ is the deuterium labeled Abiraterone N-oxide (HY-148376). Abiraterone N-oxide is a metabolite of Abiraterone (HY-148377). Abiraterone is a potent and irreversible?CYP17A1 inhibitor?with antiandrogen activity.

Benzyl-PEG14-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth.

POI ligand-6 is a target protein ligand targeting HDAC6. POI ligand-6 can be used to synthesize the hydrophobic tag (Hyt) degrader HDAC6 degrader-6 (HY-189299). POI ligand-6 can be used for research on leukemia.

FGFR3 kinase mutations are associated with a variety of malignancies. FGFR3 V555L mutation leads to resistance to FGFR inhibitors. FGFR3 V555L Recombinant Human Active Protein Kinase is a recombinant FGFR3 V555L protein that can be used to study FGFR3 V555L-related functions.

hsa-miR-196a-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-545-3p 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-6843-3p 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.

mmu-miR-292b-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.

mmu-miR-6769b-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-7684-3p 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.

Telomerase-IN-4 is a potent telomerase inhibitor. Telomerase-IN-4 has antiproliferative activity and induces apoptosis.