| Description | iHCK-37 (ASN05260065) is a high-potency, selective inhibitor of Hck with a Ki value of 0.22 μM. It effectively inhibits HIV-1 viral replication, exhibiting an EC50 value of 12.9 μM. Primarily employed in chronic myeloid leukemia (CML) research, iHCK-37 demonstrates promising potential for studying and understanding this disease. |
| In vitro | iHCK-37 (5.0-20 μM; 24 hours) exhibits a potent in vitro?antiproliferative activity. The dose (μM) for growth inhibition (GI 50 ) 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]. Cell Viability Assay[1]Cell Line: U937,?HL60, KG1a, HEL and K562 cells Concentration: 5.0-20 μM Incubation Time: 24 hours Result: Exhibited a reduction of growth in a dose-dependent manner. |
| Target activity | Hck:0.22 μM (Ki) |
| Synonyms | iHCK-37, ASN05260065 |
| molecular weight | 544.73 |
| Molecular formula | C30H32N4O2S2 |
| CAS | 516478-09-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 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. |