K-8012
K-8012, a sulindac (HY-B0008) analog, is a potent antagonist of RXRa. The IC50 value for K-8012 to inhibit 9-cis-RA-induced Gal4-RXRa-LBD trans-activation were about 9.2 μM. K-8012 exerts improved anticancer activity over sulindac in a RXRa-dependent manner. K-8012 exhibits activity in inhibiting the tRXRa-mediated PI3K/AKT signaling pathway. K-8012 induces apoptosis and inhibits AKT activation by preventing tRXRa from binding to p85a[1].
Product Specifications
CAS Number
[1346513-17-4]
UNSPSC
12352005
Target
Akt; Apoptosis; PI3K; RAR/RXR
Type
Reference compound
Related Pathways
Apoptosis; Metabolic Enzyme/Protease; PI3K/Akt/mTOR; Vitamin D Related/Nuclear Receptor
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/k-8012.html
Purity
99.46
Solubility
10 mM in DMSO
Smiles
CC1=C(CCC2=NN=NN2)C3=CC(F)=CC=C3/C1=C\C4=CC=C(C=C4)C(C)C
Molecular Formula
C23H23FN4
Molecular Weight
374.45
References & Citations
[1]Chen L, et al. Sulindac-derived RXRα modulators inhibit cancer cell growth by binding to a novel site. Chem Biol. 2014 May 22;21 (5) :596-607.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
RXRα
Available Sizes
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