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Chemical Structure| 1005342-46-0 Chemical Structure| 1005342-46-0

Structure of LCL161
CAS No.: 1005342-46-0

Chemical Structure| 1005342-46-0

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LCL161 is an IAP inhibitor that inhibits XIAP in HEK293 cells and cIAP1 in MDA-MB-231 cells with IC50s of 35 and 0.4 nM, respectively.

Synonyms: NVP-LCL161

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Product Citations

Product Citations

Rathje, Oliver H. ; Perryman, Lara ; Payne, Richard J. ; Hamprecht, Dieter W. ;

Abstract: Mixed Lineage Kinase domain-Like pseudokinase (MLKL) is implicated in a broad range of diseases due to its role as the ultimate effector of necroptosis and has therefore emerged as an attractive drug target. Here, we describe the development of PROteolysis TArgeting Chimeras (PROTACs) as a novel approach to knock down MLKL through chem. means. A series of candidate degraders were synthesized from a high-affinity pyrazole carboxamide-based MLKL ligand leading to the identification of a PROTAC mol. that effectively degraded MLKL and completely abrogated cell death in a TSZ model of necroptosis. By leveraging the innate ability of these PROTACs to degrade MLKL in a dose-dependent manner, the quant. relationship between MLKL levels and necroptosis was interrogated. This work demonstrates the feasibility of targeting MLKL using a PROTAC approach and provides a powerful tool to further our understanding of the role of MLKL within the necroptotic pathway.

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Product Details of LCL161

CAS No. :1005342-46-0
Formula : C26H33FN4O3S
M.W : 500.63
SMILES Code : C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O
Synonyms :
NVP-LCL161
MDL No. :MFCD23160049
InChI Key :UFPFGVNKHCLJJO-SSKFGXFMSA-N
Pubchem ID :24737642

Safety of LCL161

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • cIAP

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01098838 Advanced Solid Tumors PHASE1 COMPLETED 2025-01-11 UNC/ Lineberger Comprehensive ... More >>Cancer Center Dept. of LinbergerCancerCtr(2), Chapel Hill, North Carolina, 27599-7295, United States|Fox Chase Cancer Center, Philadelphia, Pennsylvania, 19111-2497, United States|Sarah Cannon Research Institute DeptofSarahCannonRes.Inst. (2), Nashville, Tennessee, 37203, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

9.99mL

2.00mL

1.00mL

19.97mL

3.99mL

2.00mL

 

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