For research use only. Not for therapeutic Use.
BETd-260 (CAT: I020058), also known as ZBC 260, is a potent PROTAC BET degrader with exceptional activity against BRD4 protein in RS4;11 leukemia cells (IC50 as low as 30 pM). It effectively suppresses cell viability and induces apoptosis in hepatocellular carcinoma (HCC) cells. BETd-260 induces degradation of BRD2, BRD3, and BRD4 proteins in leukemia cells, inhibits leukemia cell growth (IC50 51 pM), and promotes apoptosis. It modulates the expression of apoptotic genes and causes rapid tumor regression (over 90% regression) in RS4;11 xenograft mice models. BETd-260 shows promise as a therapeutic agent for leukemia and hepatocellular carcinoma.
| Catalog Number | I020058 |
| CAS Number | 2093388-62-4 |
| Molecular Formula | C₄₃H₄₆N₁₀O₆ |
| Purity | ≥95% |
| Reference | [1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.<br>[2]. Zhang H, et al. Targeting BET Proteins With a PROTAC Molecule Elicits Potent Anticancer Activity in HCC Cells. Front Oncol. 2020;9:1471. Published 2020 Jan 14. |
