| Identification | Back Directory | [Name]
PU-141 | [CAS]
168334-34-7 | [Synonyms]
PU-141
Isothiazolo[5,4-b]pyridin-3(2H)-one, 2-[[4-(trifluoromethyl)phenyl]methyl]- | [Molecular Formula]
C14H9F3N2OS | [MOL File]
168334-34-7.mol | [Molecular Weight]
310.29 |
| Hazard Information | Back Directory | [Description]
PU141 is a novel histone acetyltransferase (HAT) inhibitor. | [Uses]
PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity[1]. | [in vivo]
PU141 (25 mg/kg; administered once intraperitoneally for 24 days) exhibits a significant antitumor effects against neuroblastoma xenografts in vivo[1]. | Animal Model: | Male NMRI:nu/nu mice bearing a xenograft model[1] | | Dosage: | 12.5 and 25 mg/kg | | Administration: | Administered once intraperitoneally (i.p.) as a detergent containing saline microemulsion; for 24 days | | Result: | Led to significant tumor volume reduction (19%) at 25 mg/kg. |
| [References]
[1] M Gajer,et al. Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogenesis.2015 Feb 9;4(2):e137. DOI:10.1038/oncsis.2014.51 |
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