K-8012
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 1346513-17-4
- Formula: C23H23FN4
- Molecular Weight:374.45
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
RXR α 9.2 μM (IC50) |
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.
-
Cell Line:A549 lung cancer cells, PC3 prostate cancer cells, ZR-75-1 breast cancer cells, MB231 breast cancer cells
-
Concentration:0 μM, 0.2 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM
-
Incubation Time:48 h
-
Result:Inhibited the growth of all tested cancer cell lines in a concentration-dependent manner.
Was significantly more effective than Sulindac at reducing cell viability.
-
Cell Line:A549 lung cancer cells
-
Concentration:40 μM; 10 ng/mL TNFα (co-incubated with K-8012)
-
Incubation Time:4 h
-
Result:Slightly induced PARP cleavage when treated alone.
Caused significant induction of PARP cleavage when combined with TNFα, indicating apoptosis.
Chemical Information
-
CAS No. 1346513-17-4
-
Appearance Solid
-
Molecular Weight 374.45
-
Formula C23H23FN4
-
Color Light yellow to yellow
-
SMILES
CC1=C(CCC2=NN=NN2)C3=CC(F)=CC=C3/C1=C\C4=CC=C(C=C4)C(C)C
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
-
Data Sheet (274 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
K-8012 Related Classifications
HY-121435 Related Classifications
Powered by Bioz