Structure of Pifithrin-α HBr
CAS No.: 63208-82-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Pifithrin-α hydrobromide is a p53 inhibitor that blocks its transcriptional activity and prevents cell apoptosis. Additionally, it acts as an aryl hydrocarbon receptor (AhR) agonist.
Synonyms: Pifithrin hydrobromide; PFTα hydrobromide; PFT-alpha
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 63208-82-2 |
Formula : | C16H19BrN2OS |
M.W : | 367.30 |
SMILES Code : | CC1=CC=C(C(CN2C(SC3=C2CCCC3)=N)=O)C=C1.[H]Br |
Synonyms : |
Pifithrin hydrobromide; PFTα hydrobromide; PFT-alpha
|
MDL No. : | MFCD00417851 |
InChI Key : | HAGVCKULCLQGRF-UHFFFAOYSA-N |
Pubchem ID : | 9929138 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
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In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
HEK293-OATP1B3 cells | 30 µM | 5 h | To investigate the effect of Pifithrin-α on microcystin-LR-induced cytotoxicity, results showed that Pifithrin-α concentration-dependently attenuated the susceptibility of HEK293-OATP1B3 cells to microcystin-LR. | PMC2944092 |
sheep fetal fibroblasts (SFFs) | 10 μM | 48 h | To evaluate the effect of pifithrin-β on CRISPR-Cas9-mediated homology-directed repair (HDR) efficiency, results showed that pifithrin-β significantly decreased HDR efficiency. | PMC9883270 |
Human Coronary Artery Smooth Muscle Cells (HCASMC) | 10 μM | To investigate the effect of Pifithrin-α on the p53 signaling pathway in CDKN2B-deficient cells, results showed that Pifithrin-α inhibited the p53 signaling pathway and reduced apoptosis. | PMC3569043 | |
HepG2 cells | 20 µM | 24 h | Inhibition of p53 activation, reduction of caspase-3 cleavage, and significant reduction of OH-ME-induced cell death | PMC9708695 |
HK2 cells | 10μM | 48 h | Inhibit p53 protein levels and activity, and evaluate its impact on TGFβ1 mRNA and protein levels as well as mesenchymal transition. The results showed that PFT-α treatment partially reversed the increases in TGFβ1 mRNA and protein levels, as well as the expression of mesenchymal markers α-SMA and Vimentin induced by Bmi1 knockdown or H2O2 treatment, while partially restoring the expression of the epithelial marker E-Cadherin. | PMC11008269 |
A172 cells | 10 μM | Pifithrin-α (p53 inhibitor) was used to perform the rescue experiment, but the results indicated that pifithrin-α (PFT-a) could not significantly affect the impact of p62 overexpression on SLC7A11 in A172 (p53 wild-type) cells. | PMC8881833 |
In Vivo:
Species
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Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | Piezo1scKO mouse model | Intraperitoneal injection | 2 mg/kg | Every second day until sample isolation | Inhibition of P53 activity, reduction of senescent muscle stem cell formation, and improvement of muscle regeneration | PMC9005960 |
Mice | Carotid Artery Ligation (CAL) model and Elastase-induced Abdominal Aortic Aneurysm (AAA) model | Intraperitoneal injection | 2.2 mg/kg | Every 48 hours until sacrifice | To investigate the effect of Pifithrin-α on vascular remodeling and aneurysm formation in Cdkn2b-deficient mice, results showed that Pifithrin-α inhibited the p53 signaling pathway, reduced apoptosis, and reversed the vascular remodeling phenotype. | PMC3569043 |
Mice | MYC-induced T-cell acute lymphocytic lymphoma model | Intraperitoneal injection | 4 mg/kg | Thrice weekly for two weeks | Inhibit p53 to study its effect on CSC self-renewal | PMC6701948 |
Tags: Pifithrin-α | Pifithrin | PFTα | MDM-2/p53 | Aryl Hydrocarbon Receptor | Ferroptosis | Apoptosis | AhR | p53 inhibitor | neuroprotection | p53 transcription factor | cell cycle arrest | DNA repair | 63208-82-2
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