va 4

OAT-1441 is a hAMCase inhibitor.

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), comprising the antitumor antibiotic Pyrrolobenzodiazepine (PBD), connected through Mal-PEG4-VA.

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

RSVA405 是一种具有口服活性的AMPK 激活剂，EC50值为 1 μM。它也是一种 STAT3 抑制剂，具有抗炎作用，可研究肥胖症。它通过促进 CaMKKβ 依赖的 AMPK 活化，从而抑制mTOR，并促进自噬以增加 Aβ 的降解。

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) 作为一种吡咯苯二氮卓类化合物，主要用于作为抗体活性分子偶联物 (ADC) 的连接剂。该化合物兼具点击化学试剂的特性，含有BCN基团，能够通过应用菌株促进的炔-叠氮环加成反应 (SPAAC) 与含有Azide基团的分子进行反应。