3103327-20-1
Chemical Structure
PROTAC MLKL Degrader-2
- CAS No.: 3103327-20-1
- Formula:C36H35N9O9S
- Molecular Weight:769.78
InChIKey: XEKYTQMFAGXTNJ-UHFFFAOYSA-N
SMILES: O=C(NC1=CC=CC(C#CCN(C(N(C2=O)C)=O)C3=C2N(C(S(C)(=O)=O)=N3)C)=C1)CN4CCN(C5=CC6=C(C=C5)C(N(C6=O)C7CCC(NC7=O)=O)=O)CC4
Biological Activity: PROTAC MLKL Degrader-2 is an orally active and highly selective mixed lineage kinase domain-like pseudokinase (MLKL) PROTAC degrader with a DC50 of 0.012 μM. PROTAC MLKL Degrader-2 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, leading to ubiquitination of MLKL and its degradation via a proteasome-dependent pathway. PROTAC MLKL Degrader-2 inhibits necroptosis, reduces ROS production, restores mitochondrial function, and ameliorates lysosomal dysfunction induced by necroptotic stimuli. PROTAC MLKL Degrader-2 degrades MLKL in xenograft mouse models. PROTAC MLKL Degrader-2 can be used in cancer-related research[1].
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PROTAC MLKL Degrader-2 | PROTAC MLKL Degrader-2 is an orally active and highly selective mixed lineage kinase domain-like pseudokinase (MLKL) PROTAC degrader with a DC50 of 0.012 μM. PROTAC MLKL Degrader-2 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, leading to ubiquitination of MLKL and its degradation via a proteasome-dependent pathway. PROTAC MLKL Degrader-2 inhibits necroptosis, reduces ROS production, restores mitochondrial function, and ameliorates lysosomal dysfunction induced by necroptotic stimuli. PROTAC MLKL Degrader-2 degrades MLKL in xenograft mouse models. PROTAC MLKL Degrader-2 can be used in cancer-related research. | |||||||||||||||||||||
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