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Biochem/physiol Actions
Potent and type IIa-selective histone deacetylases (HDAC4/5/7/9) inhibitor in vitro and in vivo.
TMP269 is a potent and type IIa-selective histone deacetylases (HDACs) inhibitor (HDAC4/5/7/9 Ki = 126/80/36/19 nM, IC50 = 157/97/43/23 nM; HDAC6/8 IC50 = 8.2/4.2 μM, HADC1/2/3/10/11 IC50 >100 μM) with an active site zinc-targeting trifluoromethyloxadiazole (TFMO). TMP269 inhibits the growth of AsPC-1 by upregulating FOXO3a expression and displays in vivo therapeutic efficacy in animal models of acute kidney injury (50 mg/kg via i.p. in mice) and cerebral ischemia/reperfusion injury (1-16 mg/kg via i.p. in rats).
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to yellow-orange |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | FC(F)(C1=NC(C2=CC(C(NCC3(C4=NC(C5=CC=CC=C5)=CS4)CCOCC3)=O)=CC=C2)=NO1)F |
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