5,6,7,8-Tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazolehydrobromide
Synonym(s):2-(4-Methylphenyl)imidazo[2,1-b]-5,6,7,8-tetrahydrobenzothiazole hydrobromide;Cyclic PFT-α hydrobromide;Pifithrin-α, cyclic;QB102
- CAS NO.:511296-88-1
- Empirical Formula: C16H16N2S.HBr
- Molecular Weight: 349
- MDL number: MFCD02683960
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-09 19:38:33
What is 5,6,7,8-Tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazolehydrobromide?
Description
Pifithrin-
The Uses of 5,6,7,8-Tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazolehydrobromide
Cyclic Pifithrin-α hydrobromide has been used as p53 inhibitor to study its role in cigarette smoke?induced apoptosis of pulmonary endothelial cells.
What are the applications of Application
Cyclic Pifithrin-α hydrobromide is a cyclic analog of pifithrin-α
Biochem/physiol Actions
A stable analog of Pifithrin-α (Product Code P4359) with similar biological activities and lower cellular toxicity.
in vitro
pifithrin-α blocks p53-dependent transactivation of p53-responsive genes in cona cells. pifithrin-α (10 μm) inhibits apoptotic death of c8 cells guided by etoposide, taxol, dox, cytosine arabinoside. pifithrin-α has significant effect on the inhibition of p53-dependent growth arrest of human diploid fibroblasts in response to dna damage but not on p53-deficient fibroblasts. pifithrin-α may monitor the nuclear import or export (or both) of p53 or may make nuclear p53 instability [2].
in vivo
pifithrin-α-mice (2.2 mg/kg i.p.) were completely survival with both strains from 60% killing doses of gamma irradiation (8 gy for c57bl and 6 gy for balb/c). mice pretreated with pfithrin-α lost less weight than irradiated mice without the pifithrin-α. pifithrin-α (2.2 mg/kg) eliminates p53-dependent regulation of dna replication after whole-body gamma irradiation in mice [2].
storage
Desiccate at RT
References
[1] komarova ea and gudkov a v. could p53 be a target for therapeutic suppression semin. cancer biol. 1998, 8: 389-400.
[2] komarov pg, komarova ea, kondratov rv, christov-tselkov k, coon js, chernov mv, gudkov av. a chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. science. 1999 sep 10; 285(5434):1733-7.
Properties of 5,6,7,8-Tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazolehydrobromide
storage temp. | -20°C |
solubility | DMSO: soluble20mg/mL |
form | powder to crystal |
color | White to Almost white |
Merck | 14,7421 |
Safety information for 5,6,7,8-Tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazolehydrobromide
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for 5,6,7,8-Tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazolehydrobromide
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