AKR1B10-IN-1, a powerful AKR1B10 (Aldo-Keto Reductase 1B10) inhibitor, demonstrates an IC50 value of 3.5 nM. This compound effectively curtails the proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells.
AKR1C3-IN-6 (Compound 1) is a powerful and specific inhibitor of AKR1C3, with IC50 values of 0.31 μM and 73.23 μM against AKR1C3 and AKR1C2, respectively. It demonstrates significant antitumor activity [1].
Avatrombopag, also known as AKR-501, YM477, AS 1670542 or E5501, is a novel orally-active thrombopoietin (TPO) receptor agonist. AKR-501 specifically targeted the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as rhTPO did. AKR-501 may be useful in the treatment of patients with thrombocytopenia. Avatrombopag was first approved in 2018.
Avatrombopag hydrochloride (AKR-501) is an orally active, nonpeptide agonist of the thrombopoietin (TPO) receptor with an EC 50 of 3.3 nM. It effectively mimics the biological activities of TPO, stimulating platelet production by activating the intracellular signaling system and facilitating the generation of platelets and megakaryocytes from hemopoietic precursor cells. Additionally, Avatrombopag hydrochloride serves as a substrate for cytochrome P450 (CYP) 2C9 and CYP3A.
KSPWFTTL is an immunodominant epitope derived from the p15E transmembrane protein. It is Kb-restricted and can enhance the susceptibility of a tumor cell line to cytotoxic T lymphocytes targeting anti-AKR/Gross MuLV.