Chemical Structure : WH244
CAS No.:
2941088-96-4
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
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M.Wt
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1681.52
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Formula
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C83H105ClF3N13O11S4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Digant Nayak, et al. Nat Commun. 2024 Mar 29;15(1):2743.
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