THAL-SNS-032

- Overview
  - THAL-SNS-032 is a novel, potent and selective CDK9 degrader baed on PROTAC technology to degrade CDK9. THAL-SNS-032 is composed of a CDK-binding SNS-032 ligand linked to a thalidomide which is E3 ligase ligand that binds the E3 ubiquitin ligase Cereblon (CRBN). Cyclin-dependent kinase 9 (CDK9), an important regulator of transcriptional elongation, is a promising target for cancer therapy, particularly for cancers driven by transcriptional dysregulation. THAL-SNS-032 induced rapid degradation of CDK9 without affecting the levels of other SNS-032 targets. Moreover, the transcriptional changes elicited by THAL-SNS-032 were more like those caused by NVP-2 than those induced by SNS-032. Notably, compound washout did not significantly reduce levels of THAL-SNS-032-induced apoptosis, suggesting that CDK9 degradation had prolonged cytotoxic effects compared with CDK9 inhibition. Thus, the findings suggest that thalidomide conjugation represents a promising strategy for converting multi-targeted inhibitors into selective degraders and reveal that kinase degradation can induce distinct pharmacological effects compared with inhibition.
    
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- Properties
  - Categories
    
    PROTACs
    
    CAS Number
    
    2139287-33-3
    
    Molecular Formula
    
    C40H52N8O10S2
    
    Molecular Weight
    
    869.02
    
    Purity
    
    ≥98%
    
    Storage
    
    Powder: store in -20°C freezer for up to three years, store in 4°C freezer for up to two years
    In solvent: store in -80°C freezer for up to six months, store in -20°C freezer for up to two months
    
    Shipping
    
    Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
    
    SMILES
    
    O=C(C1CCN(CC(NCCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)CC1)NC5=NC=C(SCC6=NC=C(C(C)(C)C)O6)S5
    
    * For research use only

THAL-SNS-032

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