XCT 790

Names

[ Name ]:
XCT 790

[Synonym ]:
XCT790
(2E)-3-(4-{[2,4-Bis(trifluoromethyl)benzyl]oxy}-3-methoxyphenyl)-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]acrylamide
2-Propenamide, 3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]-, (2E)-
(2E)-3-(4-{[2,4-bis(trifluoromethyl)benzyl]oxy}-3-methoxyphenyl)-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]prop-2-enamide
hms3263n08

Biological Activity

[Description]:

XCT-790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα); induces cell death in chemotherapeutic resistant cancer cells.IC50 value:Target: ERRαERRalpha inverse agonist XCT-790 induced cell death in HepG2 hepatocarcinoma and its multi-drug resistance (MDR) sub-line R-HepG2. Using a dye Mitotracker Green which stains mitochondrion independent of mitochondrial membrane potential (DeltaPsi(m)), XCT-790 dose-dependently decreased mitochondrial mass. Intriguingly, XCT-790 increased DeltaPsi(m) upon short term treatment but decreased DeltaPsi(m) upon longer term treatment. XCT-790 synergized with paclitaxel to induce cell death in multi-drug resistance sub-line R-HepG2 [1].XCT790 is a potent and specific inverse agonist of ERRα. XCT790 shows no significant antagonist activity on related nuclear receptors, such as ERR or ERα at concentrations below 10 μM. This also inhibits the constitutive activity of ER (Estrogen Receptor) [2].

[Related Catalog]:

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

[References]

[1]. Wu F, et al. Estrogen-related receptor alpha (ERRalpha) inverse agonist XCT-790 induces cell death in chemotherapeutic resistant cancer cells. Chem Biol Interact. 2009 Oct 7;181(2):236-42.

[2]. Busch BB, et al. Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha. J Med Chem. 2004 Nov 4;47(23):5593-6.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.544g/cm3

[ Molecular Formula ]:
C₂₃H₁₃F₉N₄O₃S

[ Molecular Weight ]:
596.42500

[ Exact Mass ]:
596.05600

[ PSA ]:
125.37000

[ LogP ]:
6.80078

[ Index of Refraction ]:
1.55

[ Storage condition ]:
2-8℃

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Statements ]:
H413

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Estrogen-related receptor α is required for efficient human cytomegalovirus replication.

Proc. Natl. Acad. Sci. U. S. A. 111(52) , E5706-15, (2014)

An shRNA-mediated screen of the 48 human nuclear receptor genes identified multiple candidates likely to influence the production of human cytomegalovirus in cultured human fibroblasts, including the ...

Mitochondrial biogenesis is required for the anchorage-independent survival and propagation of stem-like cancer cells.

Oncotarget 6 , 14777-95, (2015)

Here, we show that new mitochondrial biogenesis is required for the anchorage independent survival and propagation of cancer stem-like cells (CSCs). More specifically, we used the drug XCT790 as an in...