2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor PI3K/Akt/mTOR Apoptosis
  3. RAR/RXR PI3K Akt Apoptosis
  4. 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.

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K-8012 Chemical Structure

K-8012 Chemical Structure

CAS No. : 1346513-17-4

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K-8012 Related Antibodies

Top Publications Citing Use of Products

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RXRα RXRβ RXRγ

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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Description

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].

IC50 & Target

RXR α

 

Molecular Weight

374.45

Formula

C23H23FN4
CAS No.
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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Purity & Documentation
References
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K-8012 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

K-80121346513-17-4K8012K 8012RAR/RXRPI3KAktApoptosisRetinoic acid receptorsRetinoid X receptorsPhosphoinositide 3-kinasePKBProtein kinase Banti-cancerRetinoid X receptor-alphaInhibitorinhibitorinhibit

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