ICCB280

ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc)[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

C/EBPα[1]

ICCB280 (0.1-50 μM; 48 h) suppresses the HL-60 cell growth, with an IC50 of 8.6 μM[1]. ICCB280 (10 μM; 2-8 d) increases the C/EBPα expression (mRNA and protein) and modulates its target genes in HL-60 cells[1]. ICCB280 (10 μM; 7 d) induces granulocytic differentiation and subsequent apoptosis in HL-60 cells[1]. Cell Viability Assay[1] Cell Line: HL-60 cells Concentration: 0.1, 0.5, 1, 5, 10, 50 μM Incubation Time: 48 hours Result: Induced cell growth arrest, with an IC50 of 8.6 μM. Western Blot Analysis[1] Cell Line: HL-60 cells Concentration: 10 μM Incubation Time: 2, 4, 6, 8 days Result: Upregulated the C/EBPα protein on day 4. Increased the C/EBPε expression on day 6. No changes in C/EBPβ expression through the 8 days of the experiment.

[1]. Radomska HS, et, al. A Cell-Based High-Throughput Screening for Inducers of Myeloid Differentiation. J Biomol Screen. 2015 Oct;20(9):1150-9.

[2]. Sridhar R, et, al. Styryl Quinazolinones as Potential Inducers of Myeloid Differentiation via Upregulation of C/EBPα. Molecules. 2018 Aug 3;23(8):1938.