Cancer Targeted Therapy

1,2-Di-O-acetyl-3,5-di-O-benzyl-D-xylofuranose 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.

Propargyl-PEG3-methyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Propargyl-PEG3-methyl ester is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

E3 ligase Ligand 26 (part of Compd 10) is a ligand for E3 ligase, used for the synthesis of PROTAC SOS1 degrader (HY-161636).

NH2-NODAGA is an amino-modified NODAGA-type bifunctional chelator, specifically designed for amidation coupling with targeting ligands via squaric acid (SA), followed by coordination with radionuclides (e.g., ⁶⁸Ga, ¹⁷⁷Lu). NH2-NODAGA can be coupled with diethyl squarate to form a PSMA inhibitor conjugate, which is used in prostate cancer research.

Topoisomerase IIα-IN-10 (Compound 13r) is an inhibitor of Topoisomerase IIα. It binds to the active site of DNA when complexed with Topoisomerase IIα, and this binding is stabilized through interactions with DNA base pairs and amino acid residues. Topoisomerase IIα-IN-10 can induce Apoptosis by intercalating DNA and inhibiting Topoisomerase IIα, thereby disrupting the mitochondrial membrane potential and inhibiting the growth of HCT116 cell lines, with an IC₅₀ of 4.37 μM against HCT116 cells. Topoisomerase IIα-IN-10 can be used for research in the field of cancer treatment.

P-gp-IN-30 (Compound 13) is a P-glycoprotein (P-gp) inhibitor by targeting YB-1. P-gp-IN-30 significantly enhances sensitivity to Paclitaxel by reducing total YB-1 and nucleus YB-1 protein expression, inhibiting the expression and function of downstream P-gp, further suppressing the efflux rate of Paclitaxel. P-gp-IN-30 potently inhibits tumor growth in A549/Taxol xenografts mice model with combination of Paclitaxel (HY-B0015). P-gp-IN-30 can be used for non-small cell lung cancer (NSCLC) research.

hsa-miR-4314 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-526a-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.

Nitrovin (Difurazon) is an orally active inhibitor of thioredoxin reductase 1 (TrxR1) with both antibacterial and anticancer activities. Nitrovin induces ROS generation and endoplasmic reticulum stress by targeting and inhibiting TrxR1, which in turn induces cytoplasmic vacuolation, activates MAPK, and inhibits Alix. Nitrovin induces paraptosis-like non-apoptotic cell death, thereby exerting significant cytotoxicity against cancer cells. Nitrovin is used for research on glioblastoma, liver cancer, and bacterial infections.

CDK2-IN-11 (compound 9d) is a potent CDK2 inhibitor with an IC₅₀ of 6.4 μM, and K_I values of 23.4 nM, 56.3 nM and 44.3 nM for hCA II, hCA IX and hCA XII, respectively. CDK2-IN-11 can be used for researching anticancer.

PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC₅₀s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells.

CDK9-IN-41 is a potent CDK9, EGFR, HER2, and COX-2 kinases inhibitor with IC₅₀s of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM. COX-2-IN-18 exhibits remarkable antitumor activity against leukemia cancer cells, colon cancer cells, melanoma cells, ovarian cells and breast cells.

hsa-miR-8052 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-3473b 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-6980-5p 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-222-5p 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.

RIPK1-IN-37-CO-Ph-alkynyl-Py-Pip is a Ligand-Linker conjunction, targeting RIPK1. RIPK1-IN-37-CO-Ph-alkynyl-Py-Pip can be used to synthesize PROTAC LD5097 (HY-179234).

eALM1192 is a selective mTOR kinase inhibitor (IC₅₀ = 2.3 nM) that also inhibits DNA-PK (IC₅₀ = 84 nM), PI3Kα, and PKN3, with 37-fold selectivity for mTOR over DNA-PK. eALM1192 exhibits antiproliferative activity against cancer cell lines and colorectal cancer cell lines. eALM1192 can be used for colorectal cancer research.

Procainamide-d₄ (Procaine amide-d₄) is the deuterium labeled Procainamide (HY-A0084A). Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research.

AKT is the oncogenic protein kinase that regulates essential cellular functions such as migration, proliferation, differentiation, apoptosis, and metabolism. Mammalian cells are characterized by the expression of three different Akt isoforms, Akt1, Akt2, and Akt3. Biotin-AKT2 Recombinant Human Active Protein Kinase is obtained by expressing AKT2 proteins and is biotinylated.