Name: Tat-braftide
Price: 364.00 USD

- Overview
  - Allosteric BRAF inhibitor.
    Tat-braftide is a BRAF kinase inhibitor consisting of the 10-mer peptide inhibitor, braftide, TRHVNILLFM, linked by PEG to the cell penetrating sequence TAT. Tat-braftide was designed to bind to the dimer interface of the BRAF kinase domain, and accordingly, it inhibits BRAF kinase activity by disrupting BRAF dimers, with an IC50 of 43 nM in kinase assays. Additionally, targeting the dimer interface of BRAF kinase leads to protein degradation of both RAF and MEK, uncovering a novel scaffolding function of RAF in protecting large MAPK complexes from protein degradation. Tat-braftide shows efficient inhibition and degradation of WT BRAF and BRAFG469A in a variety of cells exhibiting either RAS dependence or independence. Tat-braftide treatment causes dose dependent
    inhibition of growth of HCT116 and HCT-15 cells, with EC50 values of 7.1 and 6.6 μM, demonstrating potent inhibition of cell viability in KRAS-mutated colon cancer cells.
    
    Please contact us at for specific academic pricing.
- Properties
  - Categories
    
    Cell Penetrating Peptides
    
    Alternative Name
    
    GRKKRRQRRRPQ-PEG-TRHVNILLFM
    
    Molecular Formula
    
    C128H227N51O30S
    
    Molecular Weight
    
    2990.47
    
    Appearance
    
    Freeze dried solid
    
    Purity
    
    >95% by HPLC
    
    Solubility
    
    Soluble in water
    
    Other Properties
    
    Sequence: H-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Pro-Gln-PEG-Thr-Arg-His-Val-Asn-Ile-Leu-Leu-Phe-Met-OH,GRKKRRQRRRPQXTRHVNILLFM
    Modification: X = PEG = -NH-CH2-CH2-O-CH2-CH2-O-CH2-C=O-
    
    Storage
    
    Store dry, frozen and in the dark
    
    * Please note: this product can only be supplied to registered research and development facilities, and may be used for in vitro research use only, not for administration to humans or animals.

Tat-braftide

Tat-braftide

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