Cancer Targeted Therapy

PI3K-IN-46 (Intermediate 4) is an intermediate in the synthesis of PI3K inhibitor (2-imino-azolinone-vinyl fused-benzene derivative) that can be used for the research of autoimmune disorders, cardiovascular diseases, and neurodegenerative diseases.

DSPE-PEG1000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors.

Tubulin polymerization-IN-80 (Compound 32) is a potent tubulin polymerization inhibitor with antiproliferative activity. Tubulin polymerization-IN-80 disrupts microtubule formation and leads to cell cycle arrest and apoptosis. Tubulin polymerization-IN-80 is promising for research of cancers.

P22D is a BCR-ABL PROTAC degrader based on Dasatinib (HY-10181), with a DC₅₀ value of approximately 10 nM for the wild-type BCR-ABL protein. P22D cannot degrade the BCR-ABL T315I mutant. P22D has inhibitory activity against K562 cells (wild type), but is ineffective against BaF3-BCR-ABL (T315I) cells. P22D can be used for research on chronic myeloid leukemia and acute lymphocytic leukemia.

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

MDL-27048, a tubulin inhibitor, binds competitively, reversibly to the Colchicine (HY-16569)-binding site on tubulin heterodimers. MDL-27048 inhibits microtubule assembly, induces slow depolymerization of preassembled microtubules, disrupts microtubule polymerization-depolymerization dynamics, and disrupts cytoplasmic microtubule networks. MDL-27048 exerts growth inhibitory effects on human cancer cells, induces mitotic arrest, and does not disrupt actin filaments at microtubule-depolymerizing concentrations. MDL-27048 can be used for the research of malignant tumors.

mmu-miR-8111 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.

Theophylline-triazole-estrone is an α-glucosidase inhibitor with an IC₅₀ of 123.9 μM. Theophylline-triazole-estrone interacts with the catalytic site of α-glucosidase and binds to the anti-apoptotic protein BCL-2. Theophylline-triazole-estrone reduces cancer cell viability and can be used in research related to type 2 diabetes and breast cancer.

Notum-IN-1 (compound 6b) is an orally active, selective and brain penetrant inhibitor of Notum. Notum-IN-1 blocks the Wnt signaling in vivo in mouse.

CCT368772 (compound 35) is a selective kinesin HSET inhibitor (HSET ADP-Glo IC₅₀ = 0.019 μM). CCT368772 exhibits selectivity over Eg5 (Eg5 ADP-Glo IC₅₀ >200 μM). CCT368772 (compound 152) can be used for the study of hyperproliferative diseases and disorders such as cancer.

Pixantrone (BBR 2778 (free base)) hydrochloride, a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.

hsa-miR-4636 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-575 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-344b-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-6969-5p 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.

ZINC08792229 is a potent SIRT1 inhibitor. ZINC08792229 has the potential for research on SIRT1 related diseases, such as ageing, diabetes, cancers.

hsa-miR-3150b-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.

Propargyl-PEG7-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Propargyl-PEG7-amine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

CBP/p300 ligand 5 is the target protein ligand of XYD129 (HY-161710). CBP/p300 ligand 5 can be used to study the acute myelogenous leukemia.

Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG3-C2-OTs can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.