Bioactivity | WH244 is a second generation BCL-2 and BCL-xL dual depressant (PROTAC). The primary activity of WH244 is the specific degradation of BCL-2 and BCL-xL proteins (BCL-xL: DC50=0.6 nM, BCL-2: DC50=7.4 nM). WH244 promotes their ubiquitination and subsequent proteasome degradation by targeting these proteins, thereby restoring the cell's apoptosis pathway. WH244 has good antitumor activity. (Pink: BCL-2/BCL-xL ligand (HY-161415); Blue: E3 ligase ligand (HY-112078); Black: linker)[1]. |
CAS | 2941088-96-4 |
Formula | C83H105ClF3N13O11S4 |
Molar Mass | 1681.51 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Nayak D, et al. Development and crystal structures of a potent second-generation dual degrader of BCL-2 and BCL-xL[J]. Nature communications, 2024, 15(1): 2743. |