va 4

VA4 is a novel irreversible TG2 transamidase site-specific inhibitor.

DBCO-PEG4-VA-PBD is a cleavable 4-unit PEG ADC linker utilized in antibody-drug conjugate (ADC) synthesis [1].

Mal-PEG4-VA-PBD is a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), consisting of the antitumor antibiotic Pyrrolobenzodiazepine (PBD) linked via Mal-PEG4-VA.

Mal-PEG4-VA, a noncleavable ADC linker featuring a Maleimide group, is utilized in the synthesis of antibody-drug conjugates.

DBCO-PEG4-VA-PABC-MMAE is a drug-linker conjugate for ADCs, consisting of a tubulin inhibitor (MMAE) and a cleavable linker (DBCO-PEG4-VA-PABC). This compound is applicable for synthesizing ADCs.

OAT-1441 is a hAMCase inhibitor.

Fedovapagon (VA106483) is a selective and potent agonist of the vasopressin V2 receptor (V2R) that inhibits the growth of intersegmental vessels in zebrafish. It can be used to study overactive bladder, nocturia, and painful bladder syndromes.

RSVA405 is an AMPK activator (EC50 = 1 μM), and is STAT3 inhibitor

Adenosine 5'-methylenediphosphate is an inhibitor of ecto-5'-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5'-monophosphate , adenosine 5'-diphosphate , or adenosine 5'-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5'-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) cells in a migration assay.2,3It increases tumor infiltration of CD3+CD8+T cells and reduces tumor growth in a K1735 murine melanoma model when administered at a dose of 400 μg/mouse.4 1.Bruns, R.F.Adenosine receptor activation by adenine nucleotides requires conversion of the nucleotides to adenosineNaunyn Schmiedebergs Arch. Pharmacol.315(1)5-13(1980) 2.Braganhol, E., Tamajusuku, A.S.K., Bernardi, A., et al.Ecto-5′-nucleotidase/CD73 inhibition by quercetin in the human U138MG glioma cell lineBiochim. Biophys. Acta1770(9)1352-1359(2007) 3.Shali, S., Yu, J., Zhang, X., et al.Ecto\5′\nucleotidase (CD73) is a potential target of hepatocellular carcinomaJ. Cell Physiol.234(7)10248-10259(2018) 4.Forte, G., Sorrentino, R., Montinaro, A., et al.Inhibition of CD73 improves B cell-mediated anti-tumor immunity in a mouse model of melanomaJ. Immunol.189(5)2226-2233(2021)

BCN-HS-PEG2-VA-PABC-SG3199 (Compound 4) functions as a pyrrolobenzodiazepine-based agent linker for antibody-drug conjugates (ADC) [1]. This compound also serves as a click chemistry reagent, featuring a BCN group capable of participating in strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules.