For research use only. Not for therapeutic Use.
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].
PU141 inhibits cell growth at micromolar concentrations in A431 (epidemoid carcinoma), A549 (alveolar basal epithelial adenocarcinoma), A2780 (ovarian carcinoma), HCT116 (epithelial colon carcinoma), HepG2 (hepatocellular carcinoma), MCF7 (breast carcinoma), SK-N-SH (neuroblastoma), SW480 (colon adenocarcinoma) and U-87MG (epithelial-like glioblastoma-astrocytoma)[1].
PU141 causes both histone hypoacetylation and growth inhibition in vitro. PU141 (25 µM) leads to a decrease in SAHA-induced H3K14 and H4K8 hyperacetylation, whereas H3K9 and H4K16 acetylation levels remaine stable after co-treatment of HDAC and HAT inhibitor. The impact on histone acetylation is similar in both SK-N-SH and HCT116 cells[1].
PU141 (25 mg/kg; administered once intraperitoneally for 24 days) exhibits a significant antitumor effects against neuroblastoma xenografts in vivo[1].
| Catalog Number | I035198 |
| CAS Number | 168334-34-7 |
| Synonyms | 2-[[4-(trifluoromethyl)phenyl]methyl]-[1,2]thiazolo[5,4-b]pyridin-3-one |
| Molecular Formula | C14H9F3N2OS |
| Purity | ≥95% |
| InChI | InChI=1S/C14H9F3N2OS/c15-14(16,17)10-5-3-9(4-6-10)8-19-13(20)11-2-1-7-18-12(11)21-19/h1-7H,8H2 |
| InChIKey | UQVNCGIZTSUQOC-UHFFFAOYSA-N |
| SMILES | C1=CC2=C(N=C1)SN(C2=O)CC3=CC=C(C=C3)C(F)(F)F |
| Reference | [1]. M Gajer,et al. Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogenesis.2015 Feb 9;4(2):e137. |
