Cancer Targeted Therapy

TK4g is a Janus kinase (JAK) inhibitor with the IC₅₀ values of 12.61 nM and 15.80 nM for JAK2 and JAK3, respectively. TK4g can be used in lymphoid-derived diseases and leukemia cancer research.

1-(5-O-Methoxytrityl-2-deoxy-β-D-xylofuranosyl)uracil 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.

ICMT-IN-49 (compound 2) is an inhibitor of ICMT (IC₅₀=0.12 μM).

MIF-IN-5 (compound 1d) is a potent and reversible macrophage migration inhibitory factor (MIF) competitive inhibitor with an IC₅₀ of 4.8 μM and a K_i value of 3.3 μM, respectively.

RGS2–Galpha-q interaction-IN-1 (Compound AJ-3) is an inhibitor of the RGS2-G_alpha-q interaction. RGS2–Galpha-q interaction-IN-1 can inhibit the growth of cancer cell lines expressing RGS2 and exhibits anti-cell migration properties.

Mcl-1-IN-17 (Compound 25) is an orally active Myeloid Cell Leukemia 1 (Mcl-1) inhibitor with a K_i < 0.08  nM. Mcl-1-IN-17 has a significant antiproliferative activity (GI₅₀s of 39 and 105  nM for H929 and A427 cells, respectively) and inhibits cell apoptosis. Mcl-1-IN-17 can be used for hematological and solid cancers research.

DSPE-PEG2000-DHLASLWWGTEL is a PEG compound which composed of DSPE and a GPC3 targeting peptide DHLASLWWGTEL. The DHLASLWWGTEL peptide partially and specifically binds to GPC3-positive cells, achieving precise targeting. DSPE-PEG2000-DHLASLWWGTEL can be used for drug delivery.

DOPE-PEG2000-K237 (DOPE-PEG2000-Mal-Cys-HTMYYHHYQHHL) is an amphiphilic lipid-PEG-peptide conjugate composed of DOPE (1,2-dioleoyl-sn-glycero-3-phosphoethanolamine), PEG2000, and the K237 peptide (sequence: HTMYYHHYQHHL). K237 peptide is a tumor-homing peptide identified by phage display that specifically binds to vasculature in tumor tissues. DOPE-PEG2000-K237 is used for tumor-targeted drug delivery via functionalization of liposomes and nanoparticles.

Y-29794 (Compound 2) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a K_i of 0.95 nM. Y-29794 can be used for studying neurodegenerative diseases and cancer.

CCT239065 is an orally available, effective inhibitor of the mutant protein kinase ^V600EBRAF (RAF) with anti-tumor activity. CCT239065 inhibits downstream signaling of ^V600EBRAF in cancer cells, blocking DNA synthesis and suppressing proliferation.

A-1155905 is a MCL-1 inhibitor (IC₅₀=33.5 nM; K_i=0.58 nM) with anticancer activity. A-1155905 selectively binds to MCL-1 with sufficient affinity to disrupt the MCL-1-bim complex in living cells. A-1155905-induced death of MCL-1-dependent cell lines is caspase-dependent and occurs via apoptosis.

ER ligand-6 is a target protein ligand of PROTAC ER Degrader-14 (HY-170340).

MRC-G-001 is a Genipin (HY-17389) derivative with an IC₅₀ of 117 μM against A549 cancer cells. MRC-G-001 inhibits the phosphorylation of EGFR, JAK1, and STAT3, and modulates epithelial-mesenchymal transition (EMT)-related protein expression, thereby attenuating cell migration and invasion. MRC-G-001 induces cell cycle arrest and cell apoptosis. MRC-G-001 can be used for the study of cancers such as non-small-cell lung cancer.

Anticancer agent 280 TFA (Compound 65) is an anti-cancer agent targeting triple-negative breast cancer (TNBC). Anticancer agent 280 TFA exhibits IC₅₀ values of Anticancer agent 280 TFA for MDA-MB-231, MDA-MB-231/LM2-4, Jurkat, and MCF-7 of 7.1, 11.65, 6.99, and 21.51 μM respectively. Anticancer agent 280 TFA can cause significant arrest of cells in the S phase and induce cell apoptosis. Anticancer agent 280 TFA can be used for the study of TNBC.

Fmoc-Val-Ala-Gly (compound 58a) is a cleavable ADC linker, can be conjugated to the antibody Trastuzumab (HY-P9907) to form an antibody-drug conjugate (ADC).

cIAP1 Ligand-Linker Conjugates 3 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 3 can be used to design SNIPERs.

hsa-miR-1207-5p 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.

hsa-miR-342-5p 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-4730 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-10b-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.