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.

• Synonym(s): Pifithrin-α, p-Nitro, Cyclic, 2-(4-Nitrophenyl)imidazo[2,1-b]-5,6,7,8-tetrahydrobenzothiazole
• Empirical Formula (Hill Notation): C₁₅H₁₃N₃O₂S
• CAS Number: 60477-38-5
• Molecular Weight: 299.35
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 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

Description

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).

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

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