491002

Notch Transcription Factor Inhibitor, SAHM1

Notch Transcription Factor Inhibitor, SAHM1, is a cell-permeable inhibitor that prevents assembly in the NOTCH1 trans-activation complex.

• Synonim(y): Notch Transcription Factor Inhibitor, SAHM1, AcβA1a-ERLRRRI*LCR*HHST (*=S5)
• Wzór empiryczny (zapis Hilla): C₉₄H₁₆₂N₃₆O₂₃S · 7C₂HF₃O₂ · 13H₂O
• Masa cząsteczkowa: 3228.95
• Kod UNSPSC: 12352200

Właściwości

• Poziom jakości: 100
• Próba: ≥93% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze
• kolor: off-white
• rozpuszczalność: DMSO: 50 mg/mL
• Warunki transportu: wet ice
• temp. przechowywania: −20°C

Opis

Opis ogólny

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 (K_d = 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.

Ostrzeżenie

Toxicity: Standard Handling (A)

Sekwencja

Acetyl-βAla-ERLRRRI*LCR*HHST

* = Two S5 molecules (a non-natural alkenyl amino acid) stapled together with a double bond

Rekonstytucja

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Inne uwagi

Moellering, R.E., et al. 2009. Nature462, 182.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable