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Merck
CN

SML4101

TMP269

≥98% (HPLC)

Synonym(s):

N-((4-(4-Phenylthiazol-2-yl)tetrahydro-2H-pyran-4-yl)methyl)-3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)benzamide, TMP 269, TMP-269

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About This Item

Empirical Formula (Hill Notation):
C25H21F3N4O3S
CAS Number:
Molecular Weight:
514.52
MDL number:
NACRES:
NA.28
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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SMILES string

FC(F)(C1=NC(C2=CC(C(NCC3(C4=NC(C5=CC=CC=C5)=CS4)CCOCC3)=O)=CC=C2)=NO1)F

assay

≥98% (HPLC)

form

powder

color

white to yellow-orange

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

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).

Regulatory Information

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