506154

Pifithrin-α, p-Nitro, Cyclic

A cell-permeable p53 inhibitor that exhibits 10-fold higher potency and 50% longer half-life than Pifithrin-α.

• Synonim(y): Pifithrin-α, p-Nitro, Cyclic, 2-(4-Nitrophenyl)imidazo[2,1-b]-5,6,7,8-tetrahydrobenzothiazole
• Wzór empiryczny (zapis Hilla): C₁₅H₁₃N₃O₂S
• Numer CAS: 60477-38-5
• Masa cząsteczkowa: 299.35
• MDL number: MFCD05670249
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Właściwości

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: yellow
• solubility: DMSO: 2.5 mg/mL, ethanol: 250 μg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: [s]1c2[n](c4c1CCCC4)cc(n2)c3ccc(cc3)[N+](=O)[O-]
• InChI: 1S/C15H13N3O2S/c19-18(20)11-7-5-10(6-8-11)12-9-17-13-3-1-2-4-14(13)21-15(17)16-12/h5-9H,1-4H2
• InChI key: XMFNSEDROOHGBY-UHFFFAOYSA-N

Opis

General description

A cell-permeable p53 inhibitor that exhibits 10-fold higher potency (ED₅₀ = 30 nM in protecting etoposide-induced cortical neuron death) and 50% longer half-life (t_1/2 = 6h in neuron culture medium at 37°C) than Pifithrin-α (Cat. No. 506132). However, despite its in vitro efficacy, this inhibitor is not effective when adminstered in rats in vivo. For in vivo applications, please consider Pifithrin-α, p-Nitro (Cat. No. 506152).

Biochem/physiol Actions

Cell permeable: yes

ED50 = 30 nM in protecting etoposide-induced cortical neuron death

Primary Target
p53

Product does not compete with ATP.

Reversible: no

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

Pietrancosta, N., et al. 2006. J. Med. Chem.49, 3645.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• wgk: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable