Notch Transcription Factor Inhibitor, SAHM1, Notch Transcription Factor Inhibitor, SAHM1, is a cell-permeable inhibitor that prevents assembly in the NOTCH1 trans-activation complex.
A cell-permeable, stabilized hydrocarbon-stapled α-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 β-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.
Warning
Toxicity: Standard Handling (A)
Sequence
Acetyl-βAla-ERLRRRI*LCR*HHST
* = Two S5 molecules (a non-natural alkenyl amino acid) stapled together with a double bond
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Moellering, R.E., et al. 2009. Nature462, 182.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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Development (Cambridge, England), 147(17) (2020-08-12)
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Cooperative NF-I?B and Notch1 signaling promotes macrophage-mediated MenaINV expression in breast cancer.
Cancer stem cells (CSCs) play an important role during metastasis, but the dynamic behavior and induction mechanisms of CSCs are not well understood. Here, we employ high-resolution intravital microscopy using a CSC biosensor to directly observe CSCs in live mice
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