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WH244

Chemical Structure : WH244

CAS No.: 2941088-96-4

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WH244 (WH-244, BCL-xL/BCL-2 degrader)

Catalog No.: PC-22097Not For Human Use, Lab Use Only.

WH244 is a potent second-generation dual PROTAC degrader of BCL-2 and BCL-xL with DC50 of 0.6  nM (BCL-xL) and 7.4  nM (BCL-2) in Jurkat cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

WH244 is a potent second-generation dual PROTAC degrader of BCL-2 and BCL-xL with DC50 of 0.6  nM (BCL-xL) and 7.4  nM (BCL-2) in Jurkat cells.
WH244 exhibits binding Kd for 6.14  nM and 3.1  nM, respectively, for WT BCL-xL and WT BCL-2 in binary binding assays.
WH244 shows enhanced potency to degrade BCL-xL/BCL-2 in cells compare to Dual BCL-xL/BCL-2 degrader 753b (Cat#PC-21928).

Physicochemical Properties

M.Wt 1681.52
Formula C83H105ClF3N13O11S4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(2S,4R)-1-((S)-2-(2-(4-(2-(4-(((R)-6-((4-(4-(((4-(((R)-4-((1R,4R)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)carbamoyl)phenyl)piperazin-1-yl)methyl)-4'-chloro-4-methyl-2,3,4,5-tetrahydro-[1,1'-biphenyl]-4-yl)methyl)piperazin-1-yl)-2-oxoethyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

References

1. Digant Nayak, et al. Nat Commun. 2024 Mar 29;15(1):2743.

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