2694057-55-9
Chemical Structure
XF056-132
Synonym(s): MS132N TFA
- CAS No.: 2694057-55-9
- Formula:C53H58F7N9O9S
- Molecular Weight:1130.14
InChIKey: QZLCTMRLBULGEK-KCFOSPOJSA-N
SMILES: O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=C(N3C[C@H](N([C@H](C3)C)C)C)C=CC(C4=CC(C(NCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O)=O)=CC=C4F)=C2.O=C(O)C(F)(F)F
Biological Activity: XF056-132 (MS132N TFA) is an inactive WDR5 PROTAC degrader with a Kd value of 106 nM against human targets, and exhibits no significant binding to the VHL complex, serves as a negative control for MS132. XF056-132 binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 can be used in the research of pancreatic ductal adenocarcinoma[1][2].
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XF056-132 | XF056-132 (MS132N TFA) is an inactive WDR5 PROTAC degrader with a Kd value of 106 nM against human targets, and exhibits no significant binding to the VHL complex, serves as a negative control for MS132. XF056-132 binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 can be used in the research of pancreatic ductal adenocarcinoma. | |||||||||||||||||||||
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- [1]. Yu X, et al. Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer. Journal of medicinal chemistry. 2023 Dec 14;66(23):16168-16186. [Content Brief]
- [2]. Jian Jin, et al. Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use. WO2019246570A1.
Keywords
