Pifithrin-β hydrobromide

SKU: orb1303972

Description

Pifithrin-β hydrobromide is a cell-permeable inhibitor of p53 that reversibly blocks its transcriptional activity and apoptosis. It functions as an aryl hydrocarbon receptor (AHR) agonist and is applied in research on neuroprotection, cancer therapy side-effects, and stem cell biology, utilizing both in vivo stroke models and in vitro assays.

Research Area

Cell Biology

Images & Validation

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Key Properties

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CAS Number	511296-88-1
MW	349.29
Purity	99.74%
Formula	C₁₆H₁₇BrN₂S
SMILES	Br.Cc1ccc(cc1)-c1cn2c3CCCCc3sc2n1
Target	Ferroptosis,p53,MDM-2/p53
Solubility	DMSO:13.75 mg/mL (39.37 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.86 mM)

Bioactivity

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Target IC50

p53:23 μM(EC50)

In Vitro

PFTα molecule could not take a planar conformation required for AhR activation whereas Pifithrin-β hydrobromide showed a conformation similar to those of the prototypical AhR ligand β-naphthoflavone. In both cell lines, PFTα and Pifithrin-β hydrobromide provoked different responses related with AhR activation. However, when cyclization of PFTα to Pifithrin-β hydrobromide was hampered by acetylation of the exocyclic nitrogen, all these responses were not observed. These results lead to the conclusion that the activation of the AhR is probably caused by Pifithrin-β hydrobromide instead of PFTα.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Pifithrin β hydrobromide, Pifithrin-b, Pifithrin-b Hydrobromide, Pifithrin-beta, Pifithrin-beta Hydrobromide, Pifithrin-β, Pifithrinβ hydrobromide, Pifithrin-β Hydrobromide, PFT-b, PFT-beta, PFT-β, PFT b, PFT beta, PFT β, PFT β (hydrobromide), MDM-2/p53, Ferroptosis, p53, Cyclic PFT-a, Cyclic PFT-alpha, Cyclic PFT-α, Cyclic PFT-α, Cyclic Pifithrin-a Hydrobromide, Cyclic Pifithrin-alpha Hydrobromide, Cyclic Pifithrin-α, Cyclic Pifithrin-α hydrobromide, Cyclic Pifithrin-α hydrobromide

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Compound Identifiers

PubChem CID

11515812 ↗

Key Properties

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No computed properties available.

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