K-8012 

K-8012 is a Sulindac (HY-B0008) analog and RXRα antagonist with an IC₅₀ of 9.2 µM. K-8012 inhibits the activation of AKT. K-8012 induces Apoptosis, redirecting the TNFα signaling pathway from survival to death. K-8012 exerts anticancer activity against lung cancer, prostate cancer, and breast cancer. K-8012 can be used in research related to lung cancer, prostate cancer, breast cancer, and hepatocellular carcinoma^[1].

K-8012 (0.1-100 μM) acts as an RXRα antagonist in HCT-116 colon cancer cells, and inhibits 9-cis-RA-induced RXRα transactivation with an IC₅₀ of 9.2 μM^[1].
K-8012 (0-50 μM; 48 h) potently inhibits the growth of A549 lung cancer cells, PC3 prostate cancer cells, ZR-75-1 breast cancer cells, and MB231 breast cancer cells in vitro^[1].
K-8012 (1 h) inhibits TNFα-induced AKT activation in A549 lung cancer cells and other cancer cell lines in vitro^[1].
K-8012 (40 μM; 4 h) redirects the TNFα signaling pathway from survival to death in A549 lung cancer cells, and induces significant apoptosis when combined with TNFα^[1].
K-8012 (0.1-100 μM) inhibits the binding of 9-cis-RA-induced coactivator peptide to purified RXRα LBD, with an IC₅₀ of 14.5 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

374.45

C₂₃H₂₃FN₄

1346513-17-4

Solid

Light yellow to yellow

CC1=C(CCC2=NN=NN2)C3=CC(F)=CC=C3/C1=C\C4=CC=C(C=C4)C(C)C

Room temperature in continental US; may vary elsewhere.

• [1]. Chen L, et al. Sulindac-derived RXRα modulators inhibit cancer cell growth by binding to a novel site. Chem Biol. 2014;21(5):596-607.  [Content Brief]