Cancer Targeted Therapy

ASS1 activator 1 (Compound 10f) is a ASS1 activator with an EC₅₀ of 1.90 μM. ASS1 activator 1 enhances the activity of ASS1 and promotes AMPK phosphorylation. ASS1 activator 1 induces cell Apoptosis. ASS1 activator 1 exhibits anticancer activity against triple-negative breast cancer, colorectal cancer and liver cancer.

KDM2A/7-IN-1 is a lysine demethylase 2A (KDM2A) inhibitor with a human IC₅₀ of 11 nM. KDM2A/7-IN-1 requires co-factor 2-oxoglutarate (2OG) for binding and occupies the H3K36me2 substrate pocket via a dimethylated lysine 36-mimicking group. KDM2A/7-IN-1 represses E2F-regulated genes, induces epithelial-mesenchymal transition, DNA repair, and mTOR pathways in specific cells, and selectively inhibits proliferation of ALT-positive cancer cell lines. KDM2A/7-IN-1 can be used for the research of ALT-positive cancers.

2’-Deoxy-2’-fluoroinosine 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.

hsa-miR-873-5p 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-375-5p 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-6958-5p 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.

rno-miR-190b-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.

EZH2-IN-25 is an EZH2 inhibitor that inhibits the catalytic subunit of PRC2. EZH2-IN-25 can be used for the research of diffuse large B cell lymphoma.

ICMT-IN-31 (compound 68) is an inhibitor of ICMT (IC₅₀=0.0038 μM).

(S)-HTS-3 is a Lysophosphatidylcholine acyltransferase 3 (LPCAT3/MBOAT5) inhibitor with a human IC₅₀ of 4.1 μM. (S)-HTS-3 inhibits the acyltransferase activity of LPCAT3. (S)-HTS-3 modestly reduces incorporation of deuterated arachidonic acid into C20:4 phosphatidylserine in myeloid leukemia cells.

Thalidomide-O-C5-piperidine-NH-Boc is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-O-C5-piperidine-NH-Boc can be used to synthesize PROTAC PIN1 degrader-1 (HY-168037).

HPK1-IN-56 (Compound A29) is a HPK1 inhibitor (IC₅₀: 2.70 nM). HPK1-IN-56 inhibits downstream p-SLP76 (IC₅₀: 8.1 nM in Jurkat T cells). HPK1-IN-56 induces the production of IL-2 in human PBMCs. HPK1-IN-56 has anticancer effect, enhances T-cell killing ability and the antitumor efficacy of anti-PD-1 antibody.

HP1142 is a potent and selective inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1142 is a benzoimidazole scaffold-based compound. HP1142 has the potential for the research of FLT3/ITD leukemia.

HIF-1α-IN-6 (compound 3s) is a HIF-1α inhibitor with IC₅₀ values of 0.6 and 53.3 nM observed in MiaPaCa-2 and MDA-MB-231 cells. HIF-1α-IN-6 can inhibit HIF-1α expression by decreasing the level of HIF-1α mRNA.

PB830 (compound 41) is a potent receptor interacting protein 1 kinase (RIP1) Inhibitor with an IC₅₀ of <100 nM for human RIP1. PB830 has an EC₅₀ of 1-100 nM in the cell necrosis assay.

L-731735 is a selective FPTase inhibitor that can inhibit ras-dependent cell transformation. L-731735 can be used in cancer research.

hsa-miR-4648 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-585-5p 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.

E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC₅₀ value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase.

(S,R,R,R)-AHPC-Me is a von Hippel-Lindau (VHL) Ligands for E3 Ligase and a diastereomer of (S,R,S)-AHPC-Me. (S,R,R,R)-AHPC-Me can be used in studies related to PROTAC synthesis, such as MS4322 (isomer) (HY-141877B).