2763268-64-8
Chemical Structure
PROTAC LZK degrader 1
- CAS No.: 2763268-64-8
- Formula:C51H64F2N10O5S
- Molecular Weight:967.18
InChIKey: NNOXSMGLIYXSCU-OMSCPKDKSA-N
SMILES: FC(CC1)(F)CN1C2=CC(C3CCN(C(CCCCCCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)=O)=O)CC3)=CC(NC7=CC(C#N)=CC=N7)=N2
Biological Activity: PROTAC LZK degrader 1 is an LZK (MAP3K13) PROTAC degrader. PROTAC LZK degrader 1 binds LZK with a Kd of 35 nM and recruits VHL E3 ubiquitin ligase to induce ubiquitin-proteasome dependent degradation of LZK in MAP3K13-amplified HNSCC cells. PROTAC LZK degrader 1 eliminates both kinase-dependent c-MYC stabilization and kinase-independent GOF p53 accumulation downstream of LZK, suppresses colony formation of LZK-amplified head and neck squamous cell carcinoma (HNSCC) cells. PROTAC LZK degrader 1 can be used for research on LZK-driven HNSCC[1].
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PROTAC LZK degrader 1 | PROTAC LZK degrader 1 is an LZK (MAP3K13) PROTAC degrader. PROTAC LZK degrader 1 binds LZK with a Kd of 35 nM and recruits VHL E3 ubiquitin ligase to induce ubiquitin-proteasome dependent degradation of LZK in MAP3K13-amplified HNSCC cells. PROTAC LZK degrader 1 eliminates both kinase-dependent c-MYC stabilization and kinase-independent GOF p53 accumulation downstream of LZK, suppresses colony formation of LZK-amplified head and neck squamous cell carcinoma (HNSCC) cells. PROTAC LZK degrader 1 can be used for research on LZK-driven HNSCC. | |||||||||||||||||||||
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