Notch Transcription Factor Inhibitor, SAHM1 – Calbiochem

Descrição detalhada : A cell-permeable, stabilized hydrocarbon-stapled alpha-helical peptide that targets a critical protein-protein interface and prevents assembly in the NOTCH1 trans-activation complex. Soluble FITC-SAHM1 was found to bind the pre-formed RAMANK-CSL complex (Kd = 0.12 µM) competitively with MAML1, whereas the unmodified FITC-MAML1 (21-36) peptide bound the complex with markedly diminished affinity in an in vitro pull down assay. Treatment of KOPT-K1 cell lines with 20 µM of compound results in the suppression of NOTCH1 target genes, HES4, DTX1, and HES1. A consistent repressive effect on NOTCH1-activated gene expression by this compound was observed across a panel of human T-ALL cell lines, containing diverse mutant NOTCH1 alleles. In HeLa cells, this peptide also inhibited the expression of ICN1 (IC50 = 6.56 µM) dose-dependently in a luciferase reporter-gene assay, as well as that of beta-lactamase (IC50<2.5 µM) in a second reporter-gene assay. Furthermore, treatment with this peptide inhibits NOTCH-mediated proliferation in cultured cells at 15 µM, and in a mouse model of T-ALL cells at 30 mg/kg twice daily.
Sinónimos : Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem; AcbetaA1a-ERLRRRI*LCR*HHST (*=S5)
Fórmula molecula r: C94H162N36O23S · 7C2HF3O2 · 13H2O
Armazenamento : -20C
Embalagem : 1X1MG