All Photos(1)
Synonym(s):
ARE expression modulator 1, N-(1,3-Benzodioxol-5-ylmethyl)-5-(4-fluorophenyl)-thieno[2,3-d]pyrimidin-4-amine
Empirical Formula (Hill Notation):
C20H14FN3O2S
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to light brown
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
AEM1 (ARE expression modulator 1) is also a selective inhibitor of sirtuin 2, which is a protein deacetylase mediated by NAD+. Sirtuin 2 supports tumor cell proliferation, thus its inhibition stimulates cell death in tumors.
AEM1 is a potent inhibitor of deregulated Nrf2 transcriptional activity. AEM1 broadly decreases the expression of NRF2 controlled genes and sensitizes A549 cells to various chemotherapeutic agents.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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AK-1, a specific SIRT2 inhibitor, induces cell cycle arrest by downregulating Snail in HCT116 human colon carcinoma cells.
Cheon M G, et al.
Cancer Letters, 356(2), 637-645 (2015)
Gesine Hoffmann et al.
The Journal of biological chemistry, 289(8), 5208-5216 (2014-01-01)
Sirtuin 2 (SIRT2) is an NAD(+)-dependent protein deacetylase whose targets include histone H4 lysine 16, p53, and α-tubulin. Because deacetylation of p53 regulates its effect on apoptosis, pharmacological inhibition of SIRT2-dependent p53 deacetylation is of great therapeutic interest for the
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