biostudies-literatureFetisov TIRussian Science Foundation230https://www.ebi.ac.uk/biostudies/studies/S-EPMC9856019biostudies-literatureUnknown11(1)The anticancer activity of Curaxin CBL0137, a DNA-binding small molecule with chromatin remodulating effect, has been demonstrated in different cancers. Herein, a comparative evaluation of CBL0137 activity was performed in respect to acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), chronic myeloid leukemia and multiple myeloma (MM) cultured in vitro. MTT assay showed AML and MM higher sensitivity to CBL0137's cytostatic effect comparatively to other hematological malignancy cells. Flow cytometry cell cycle analysis revealed an increase in subG1 and G2/M populations after CBL0137 cell treatment, but the prevalent type of arrest varied. Apoptosis activation by CBL0137 measured by Annexin-V/PI dual staining was more active in AML and MM cells. RT2 PCR array showed that changeBiomedicinesTargeting Features of Curaxin CBL0137 on Hematological Malignancies In Vitro and In Vivo.PMC985601921-75-10163Antoshina EEGurova KAntipova ASZuevskaya SNLesovaya EAMaslov AKirsanov KIYakubovskaya MGFetisov TIGudkov ABorunova AABelitsky GAGorkova TGTrukhanova LSfalseTargeting Features of Curaxin CBL0137 on Hematological Malignancies In Vitro and In Vivo.The anticancer activity of Curaxin CBL0137, a DNA-binding small molecule with chromatin remodulating effect, has been demonstrated in different cancers. Herein, a comparative evaluation of CBL0137 activity was performed in respect to acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), chronic myeloid leukemia and multiple myeloma (MM) cultured in vitro. MTT assay showed AML and MM higher sensitivity to CBL0137's cytostatic effect comparatively to other hematological malignancy cells. Flow cytometry cell cycle analysis revealed an increase in subG1 and G2/M populations after CBL0137 cell treatment, but the prevalent type of arrest varied. Apoptosis activation by CBL0137 measured by Annexin-V/PI dual staining was more active in AML and MM cells. RT2 PCR array showed that change2023-01-01T00:00:00Z2023 Jan2025-04-26T00:38:29.582Z2025-04-06T09:47:21.324ZS-EPMC98560193667273810.3390/biomedicines11010230