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.
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- Purity: 99.51%
- CAS No.: 1346513-17-4
- 화학식: C23H23FN4
- 분자량:374.45
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보관: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]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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.
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Cell Line:A549 lung cancer cells, PC3 prostate cancer cells, ZR-75-1 breast cancer cells, MB231 breast cancer cells
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Concentration:0 μM, 0.2 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM
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Incubation Time:48 h
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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.
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Cell Line:A549 lung cancer cells
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Concentration:40 μM; 10 ng/mL TNFα (co-incubated with K-8012)
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Incubation Time:4 h
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Result:Slightly induced PARP cleavage when treated alone.
Caused significant induction of PARP cleavage when combined with TNFα, indicating apoptosis.
Chemical Information
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CAS No. 1346513-17-4
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Appearance Solid
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분자량 374.45
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화학식 C23H23FN4
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Color Light yellow to yellow
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SMILES
CC1=C(CCC2=NN=NN2)C3=CC(F)=CC=C3/C1=C\C4=CC=C(C=C4)C(C)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
순도&문서
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Data Sheet (274 KB)
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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)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
K-8012 Related Classifications
HY-121435 Related Classifications
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