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].

Product Specifications

CAS Number

[2941088-96-4]

UNSPSC

12352005

Target

Apoptosis; Bcl-2 Family; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/wh244.html

Purity

99.82

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C83H105ClF3N13O11S4

Molecular Weight

1681.51

References & Citations

[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.