WH244 

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].

1681.51

C₈₃H₁₀₅ClF₃N₁₃O₁₁S₄

2941088-96-4

CC1=C(C2=CC=C([C@@H](NC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(CN4CCN(CC(N5CCN(C[C@]6(C)CCC(C7=CC=C(Cl)C=C7)=C(CN8CCN(C9=CC=C(C(NS(C%10=CC(S(C(F)(F)F)(=O)=O)=C(N[C@@H](CSC%11=CC=CC=C%11)CCN%12C[C@@H]%13OC[C@H]%12C%13)C=C%10)(=O)=O)=O)C=C9)CC8)C6)CC5)=O)CC4)=O)C(C)(C)C)=O)=O)C)C=C2)SC=N1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]