3095033-62-5
Chemical Structure
Lck degrader-1
- CAS No.: 3095033-62-5
- Formula:C25H25N5O4
- Molecular Weight:459.50
IUPAC Name: 7-(aminomethyl)-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)-3-ethyl-1H-indole-2-carboxamide
InChIKey: KMGBAFLISYQLRW-UHFFFAOYSA-N
SMILES: CCC1=C(NC2=C1C=CC=C2CN)C(NC3=CC4=C(C(N(C5CCC(NC5=O)=O)C4)=O)C=C3)=O
Biological Activity: Lck degrader-1 is a molecular glue degrader that recruits cereblon to target LCK and CK1α. Lck degrader-1 promotes the formation of the LCK/CRBN-DDB1 ternary complex with an EC50 of 77.1 nM, and induces the degradation of LCK and CK1α. LCK degradation induced by Lck degrader-1 depends on the G415-containing helical G-loop degron, and maintains LCK-degrading activity in cells with the LCK T316I gatekeeper mutation. Lck degrader-1 can be used for research related to T-cell acute lymphoblastic leukemia (T-ALL) and LCK inhibitor resistance[1].
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Lck degrader-1 | Lck degrader-1 is a molecular glue degrader that recruits cereblon to target LCK and CK1α. Lck degrader-1 promotes the formation of the LCK/CRBN-DDB1 ternary complex with an EC50 of 77.1 nM, and induces the degradation of LCK and CK1α. LCK degradation induced by Lck degrader-1 depends on the G415-containing helical G-loop degron, and maintains LCK-degrading activity in cells with the LCK T316I gatekeeper mutation. Lck degrader-1 can be used for research related to T-cell acute lymphoblastic leukemia (T-ALL) and LCK inhibitor resistance. | |||||||||||||||||||||
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