Cancer Targeted Therapy

hsa-miR-520a-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.

E3 ligase Ligand 30 is a ligand for E3 ligase.

EX05 is a potent KIF18A inhibitor with an IC₅₀ value of 8.2 nM. EX05 has the potential for the research of cancer.

DSPE-PEG5000-CREKA is a PEG compound which composed of DSPE and a fibrin-targeting peptide (CREKA). CREKA peptide can be used to target tumor cells and tumor vasculature, exhibiting antitumor activity. DSPE-PEG5000-CREKA can be used for drug delivery.

Sarkomycin is a glutathione-targeting cytotoxic agent and antibacterial agent. Sarkomycin forms an addition product with glutathione, thereby reducing intracellular glutathione levels. Sarkomycin can induce cytoplasmic vacuolation, mitochondrial damage, cytoplasmic deformation, metaphase arrest, chromosomal abnormalities, nuclear degeneration, and nuclear fragmentation; it also modulates amino acid metabolism. Sarkomycin also inhibits anaerobic fermentation in affected cells in mice and inhibits cell growth in tissue culture, leading to the disappearance of mitotic cells, cell degeneration, and cell detachment from the glass surface. Sarkomycin can be used in research related to Yoshida ascites tumor, Ehrlich ascites tumor, Ehrlich carcinoma, and Yoshida rat sarcoma.

PF-06747143 is recombinant anti-human antibody targeting CXCR4. PF-06747143 blocks CXCL12-induced calcium flux, F-actin polymerization, chemotaxis, cell migration, and leukemic cell bone marrow homing. PF-06747143 reduces tumor burden and improves survival in mouse models of hematologic malignancies. PF-06747143 can be used for the research of chronic lymphocytic leukemia, acute myeloid leukemia, and hematologic malignancies.

hsa-miR-197-3p 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-433-3p 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.

3’-Deoxy-N6-methyladenosine 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.

PROTAC BRD4 Degrader-22 is a BRD4 PROTAC degrader with a DC₅₀ of 0.59 nM. At high concentrations, PROTAC BRD4 Degrader-22 induces partial degradation of BRD3 and BRD2, but exhibits selectivity for IKZF3. PROTAC BRD4 Degrader-22 can be used in leukemia-related research.

PROTAC Bcl-xL degrader-4 is a Bcl-xL PROTAC degrader. PROTAC Bcl-xL degrader-4 exhibits cytotoxicity against hepatocellular carcinoma cells, inhibits their migration and colony formation, and shows low cytotoxicity toward normal cells. PROTAC Bcl-xL degrader-4 induces apoptosis by reducing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTAC Bcl-xL degrader-4 significantly suppresses tumor growth in xenograft tumor mouse models. PROTAC Bcl-xL degrader-4 can be used in hepatocellular carcinoma-related research.

PROTAC EZH2 Degrader-45 (compound 61) is a PROTAC protein degrader targeting EZH2 with an IC₅₀ of 22.97 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-45 can be used for the research of diffuse large b-cell lymphoma.

Trastuzumab-DM4 is an antibody-drug conjugate (ADC) formed by conjugating Trastuzumab (HY-P9907) with DM4 (sulfo-SPDB-DM4) (HY-101141) via a cleavable linker. DM4 is a tubulin inhibitor that suppresses cell division. Trastuzumab-DM4 significantly inhibits tumor growth in Trastuzumab-resistant HER2 xenograft tumor models. Trastuzumab-DM4 can be used for the research of HER2-positive breast cancer.

Pimozide-d₄-1 is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with K_is of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a K_i of 39 nM; Pimozide also inhibits STAT3 and STAT5.

hsa-miR-7844-5p 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.

mmu-miR-344d-2-5p 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.

Hydroxy-PEG24-CH2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

mmu-miR-6971-5p 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.

rno-miR-205 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.

CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC₅₀s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.