Cancer Targeted Therapy

CaMKK2-IN-1 is a selective, ligand-efficient inhibitor of CaMKK2, with IC₅₀ of 7 nM.

Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.

4-trans-Hydroxycyclohexylamine (trans-4-Aminocyclohexan-1-ol) is an intermediate. 4-trans-Hydroxycyclohexylamine is used in the synthesis of the PGK1 inhibitor Compd 25-4. 4-trans-Hydroxycyclohexylamine is used in research on EGFR-positive esophageal squamous cell carcinoma.

Vicenin 2, a flavonoid, is an orally active angiotensin-converting enzyme (ACE) inhibitor (IC₅₀ of 43.83 μM). Vicenin 2 has radioprotective, anti-nociceptive effects, anti-glycation anti-inflammatory, antioxidant, anticancer, antiangiogenic properties.

D-Ala-Lys-AMCA hydrochloride is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA hydrochloride may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA hydrochloride can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm).

SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC₅₀s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively.

Phleomycin is a copper-dependent DNA damaging agent and antibiotic with antitumor activity. Phleomycin binds to DNA and produces ROS in the presence of reducing agents (such as dithiothreitol and glutathione), inducing single-strand and double-strand breaks in DNA. Phleomycin can induce cell apoptosis or mutation and is widely used in cancer inhibition, microbial genetic transformation (as a screening marker to improve fungal transformation efficiency) and DNA repair mechanism research.

Mal-Val-Ala-PAB-N(SO2Me)-Exatecan (Compound LE14) is a conjugate of an ADC toxin Exatecan (HY-13631) and a linker Mal-Val-Ala-PAB-N(SO2Me). Mal-Val-Ala-PAB-N(SO2Me)-Exatecan can be used for synthesis of ADC FZ-AD005. FZ-AD005 is a delta-like ligand 3 (DLL3, K_D=58.3 pM) targeting ADC, that exhibits antitumor efficacy against SCLC cancer.

Columbamine (Columbamin; Dehydroisocorypalmine) chloride is an organic heterotetracyclic alkaloid extracted from plants. Columbamine chloride is a metabolite of Berberine (HY-N0716). Columbamine chloride inhibits the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 30.6 µM). Columbamine chloride induces apoptosis in cancer cells. Columbamine chloride can be used for antioxidant, anti-inflammatory, antitumor, antifungal, antiparasite, hepatoprotective, neuroprotective, hypolipidemic and hypoglycemic study.

Tanerasertib (Compound 456) is an AKT1 inhibitor, targerting to AKT1^E17K with the EC₅₀ of 15-60 nM. Tanerasertib can be used in the study of cancer.

m-PEG2-Amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. m-PEG2-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Keracyanin chloride inhibits NF-κB/FAK/MAPK signaling pathway. Keracyanin chloride exhibits antioxidant, anti-inflammatory and hypoglycemic effects, and is orally active.

Oleuropein Aglycone (3,4-DHPEA-EA) is a secoiridoid that exerts antioxidant, anti-inflammatory, and anti-apoptotic effects by promoting ERK/AMPK/eNOS phosphorylation and inhibiting JNK/p38 MAPK and inflammation-related signaling pathways. Oleuropein Aglycone is used in research on acute kidney injury induced by ischemia-reperfusion injury, pleurisy, osteoporosis, Alzheimer's disease, neurodegenerative diseases, and triple-negative breast cancer.

RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC₅₀=46.3 nM), stabilizes the interaction between RECQL5-RAD51 proteins, causes RAD51 aggregation and homologous recombination repair (HRR) inhibition, thereby exhibiting selective cytotoxicity in RECQL5-expressing cancer cells.

2-Deoxy-D-glucose 6-phosphate disodium is an ATP-competitive, 2-deoxy-D-glucose non-competitive Hexokinase inhibitor, with a K_i value of 1.45 mM against bovine heart hexokinase. 2-Deoxy-D-glucose 6-phosphate disodium exerts ATP-competitive and 2-deoxy-D-glucose non-competitive inhibitory effects on bovine heart hexokinase. 2-DG inhibits glycolysis via the production and intracellular accumulation of 2-Deoxy-D-glucose 6-phosphate disodium, thereby inhibiting the functions of hexokinase and Glucose-6-phosphate isomerase, and inducing cell death. 2-Deoxy-D-glucose 6-phosphate disodium can be used in cancer-related research.

Dibromomaleimide-C5-COOH (DBM-C5-COOH) is a bifunctional dibromomaleimide (DBM) linker. Dibromomaleimide-C5-COOH can be used to connect MMAF and to synthesize ADC.

IL4I1-IN-1 (Compound Ex 232 pg 200) is a selective interleukin 4-induced protein 1 (IL4I1) inhibitor with an EC₅₀ of 2 nM. IL4I1-IN-1 inhibits IL4I1-mediated oxidative deamination of phenylalanine, reducing the production of phenylpyruvate, H₂O₂ and NH₃. IL4I1-IN-1 is promising for research of cancers with high IL4I1 expression, such as endometrial carcinoma, ovarian cancer, and triple-negative breast cancer.

Taurohyocholic acid is a taurine-conjugated hyocholic acid. Taurohyocholic acid is predictor of the efficacy of tyrosine kinase inhibitors combined withPD-1 inhibitors in hepatocellular carcinoma (HCC).

Boc-NH-C4-acid is a PROTAC linker, which belongs to a Alkyl/ether linker. Boc-NH-C4-acid can be used in the synthesis of the compound PROTAC1, and specifically degrades EED, EZH2, and SUZ12 in the PRC2 Complex.

DBM-MMAF is a agent-linker conjugate composed of a potent antitubulin agent MMAF and a linker DBM to make antibody agent conjugate (ADC).