iHCK-37 (ASN05260065) 是一种有效的特异性 Hck 抑制剂，Ki 值为 0.22 μM。iHCK-37 阻断 HIV-1 病毒复制，其 EC50 值为 12.9 μM。iHCK-37 可用于慢性髓系白血病(CML)研究。
iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research[1].
iHCK-37 (5.0-20 μM; 24 hours) exhibits a potent in vitro antiproliferative activity. The dose (μM) for growth inhibition (GI50) is 5.0-5.8 μM for AML cell lines (HL60, KG1a and U937) and 9.1-19.2 μM for chronic myeloid leukemia cell lines (HEL and K562)[2].iHCK-37 (3-9 μM; plus Erythropoietin) leads to a decrease in ERK, AKT and P70S6K phosphorylation of in lentivirus HCK silenced K562 and U937 cell lines[2].iHCK-37 (3-9 μM) results in a decrease of p-HCK, p-ERK, p-AKT, p-70S6 in the cell line KG1a (AML/CD34+), in a dose-dependent manner[2].
[1]. Cristina Tintori, et al. Identification of Hck inhibitors as hits for the development of antileukemia and anti-HIV agents. ChemMedChem. 2013 Aug;8(8):1353-60.
[2]. Fernanda Marconi Roversi, et al. Hematopoietic cell kinase (HCK) is a potential therapeutic target for dysplastic and leukemic cells due to integration of erythropoietin/PI3K pathway and regulation of erythropoiesis: HCK in erythropoietin/PI3K pathway. Biochim Biophys Acta Mol Basis Dis. 2017 Feb;1863(2):450-461.
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