491002

SAHM1

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

• Synonym(s): Notch Transcription Factor Inhibitor, SAHM1, AcβA1a-ERLRRRI*LCR*HHST (*=S5)
• Empirical Formula (Hill Notation): C₉₄H₁₆₂N₃₆O₂₃S · 7C₂HF₃O₂ · 13H₂O
• Molecular Weight: 3228.95
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• product name: Notch Transcription Factor Inhibitor, SAHM1, Notch Transcription Factor Inhibitor, SAHM1, is a cell-permeable inhibitor that prevents assembly in the NOTCH1 trans-activation complex.
• Quality Level: 100
• Assay: ≥93% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: off-white
• solubility: DMSO: 50 mg/mL
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

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.

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable