491002

SAHM1

≥93% (HPLC), solid, Notch transcription factor inhibitor, Calbiochem^®

• Sinonimo/i: Notch Transcription Factor Inhibitor, SAHM1, AcβA1a-ERLRRRI*LCR*HHST (*=S5)
• Formula empirica (notazione di Hill): C₉₄H₁₆₂N₃₆O₂₃S · 7C₂HF₃O₂ · 13H₂O
• Peso molecolare: 3228.95
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Nome del prodotto: Notch Transcription Factor Inhibitor, SAHM1, Notch Transcription Factor Inhibitor, SAHM1, is a cell-permeable inhibitor that prevents assembly in the NOTCH1 trans-activation complex.
• Livello qualitativo: 100
• Saggio: ≥93% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: off-white
• Solubilità: DMSO: 50 mg/mL
• Condizioni di spedizione: wet ice
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

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.

Attenzione

Toxicity: Standard Handling (A)

Sequenza

Acetyl-βAla-ERLRRRI*LCR*HHST

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

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable