Cancer Targeted Therapy

LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with high affinity (K_d: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn²⁺ respectively). LDV-FITC can be used to detect α4β1 integrin affinity.

Apixaban (Standard) is the analytical standard of Apixaban. This product is intended for research and analytical applications. Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with K_i of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is in development for the prevention and treatment of various thromboembolic diseases.

7-Bromohept-1-yne is a PROTAC linker that can be used to synthesize AK-1690 (HY-169179).

Desamino lenalidomide-6-OH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-6-OH can be linked to a target protein ligand via a linker to form a PROTAC.

2,4,6-Trihydroxybenzaldehyde is an orally active NF- B inhibitor. 2,4,6-Trihydroxybenzaldehyde shows anti-tumor activity, anti-cancer cell proliferative activity and anti-obesity activity.

4-Phenyl-1H-1,2,3-triazole is a selective IDO1 inhibitor with an IC₅₀ of 83 μM against human IDO1. 4-Phenyl-1H-1,2,3-triazole binds to the heme iron of IDO1 and occupies its active site, thereby inhibiting tryptophan catabolism. 4-Phenyl-1H-1,2,3-triazole can serve as a precursor for the synthesis of HIV-1 capsid protein inhibitors. 4-Phenyl-1H-1,2,3-triazole is applicable to research related to cancer and organic synthesis.

tert-Butyl N-(3-hydroxypropyl)-N-methylcarbamate is a PROTAC linker that can be used in the synthesis of PROTACs.

3’-Azido-3’-deoxyuridine is a purine nucleoside analogue. 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. 3’-Azido-3’-deoxyuridine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

Meridianin C is a marine natural product with anticancer activity. Meridianin C has significant inhibitory effects on four different human tongue cancer cells (YD-8, YD-10B, YD-38 and HSC-3). Meridianin C most strongly reduced the growth of YD-10B cells, the most aggressive and tumorigenic of the cell lines tested. Meridianin C also induced significant accumulation of large vesicles in YD-10B cells, validating its function through macrophagocytosis. Meridianin C reduces cellular levels of Dickkopf-related protein-3 (DKK-3), a known negative regulator of macrophagy. Meridianin C affects macrophagocytosis by downregulating DKK-3, thereby affecting cell proliferation.

Taltobulin intermediate-4 is an intermediate in the synthesis of Taltobulin (HY-15584). Taltobulin is a common toxin component in ADC preparation (ADC Cytotoxin), and it is also a powerful tubulin (Microtubule/Tubulin) inhibitor. Taltobulin disrupts tubulin polymerization, induces mitotic arrest, and induces apoptosis.

miR-21-IN-2 is a high-affinity miR-21 inhibitor. miR-21-IN-2 binds to the apical loop region of the pre-miR-21 hairpin, inhibits Dicer-mediated processing, and thereby blocks the biosynthesis of mature miR-21. miR-21-IN-2 can be used for the research of microRNA-related diseases.

Exatecan intermediate 9 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM).

Benzyl N-(2-aminoethyl)carbamate hydrochloride is a PROTAC linker that can be used in the synthesis of PROTACs.

4-(4-Hydroxyphenyl)butanoic acid is a PROTAC linker that can be used in the synthesis of PROTACs.

N-methylated pomalidomide (Pomalidomide-methyl), a derivative of Pomalidomide (HY-10984), is a cereblon (CRBN) ligand. N-methylated pomalidomide is unable to recruit CRBN that can be used as a negative control for Pomalidomide. N-methylated pomalidomide can be used to synthesize PROTAC.

5-(Benzyloxy)pentan-1-ol is a PROTAC linker that can be used in the synthesis of PROTACs.

7-Hydroxystaurosporine (UCN-01), a derivative of Staurosporine (HY-15141), is a selective protein kinase C (PKC) inhibitor with antitumor activity. 7-hydroxystaurosporine induces apoptosis and inhibits cell proliferation in colon carcinoma and leukemia cells, suppresses invasion and migration in glioblastoma cells. 7-Hydroxystaurosporine exhibits efficacy in breast cancer xenograft mouse models. 7-Hydroxystaurosporine can be used for colon carcinoma, breast cancer, glioblastoma and leukemia research.

APX2009 is a specific APE1/REF-1 redox inhibitor with anticancer activities which decreases the proliferative, migratory, and invasive properties of breast cancer cell and induces apoptosis in breast cancer cell.

2-(2,6-Dioxopiperidin-3-yl)phthalimidine (EM-12), a teratogenic Thalidomide analogue, is more active than Thalidomide and is much more stable for hydrolysis. 2-(2,6-Dioxopiperidin-3-yl)phthalimidine enhances 1,2-dimethylhydrazine-induction of rat colon adenocarcinomas.

tert-Butyl (11-aminoundecyl)carbamate is an alkane chain with terminal amine and Boc-protected amino groups. tert-Butyl (11-aminoundecyl)carbamate can be used as a PROTAC linker in the synthesis of PROTACs and other conjugation applications. Amine group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. The Boc group can be deprotected under mild acidic conditions to form the free amine.