2901804-87-1
Chemical Structure
SMARCA2/4 degrader-1
- CAS No.: 2901804-87-1
- Formula:C30H35N7O
- Molecular Weight:509.65
IUPAC Name: 2-(6-amino-5-(8-(2-(3-(azepan-1-yl)prop-1-yn-1-yl)pyridin-4-yl)-3,8-diazabicyclo[3.2.1]octan-3-yl)pyridazin-3-yl)phenol
InChIKey: GLSFALNCXYWSSD-UHFFFAOYSA-N
SMILES: OC1=CC=CC=C1C2=CC(N3CC4N(C5=CC(C#CCN6CCCCCC6)=NC=C5)C(CC4)C3)=C(N)N=N2
Biological Activity: SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4DCAF16 and CRL1FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer[1].
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SMARCA2/4 degrader-1 | SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4DCAF16 and CRL1FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer. | |||||||||||||||||||||
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