1. PI3K/Akt/mTOR
  2. Akt
  3. K-80003

K-80003 (Synonyms: TX-803)

Cat. No.: HY-U00458
Handling Instructions

K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.

For research use only. We do not sell to patients.

K-80003 Chemical Structure

K-80003 Chemical Structure

CAS No. : 1292821-90-9

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Description

K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.

IC50 & Target[1]

Akt

 

In Vitro

When MCF-7 cells are cotreated with K-80003, TNFα-induced colocalization of tRXRα with p85α in the cytoplasm is inhibited, resulting in tRXRα nuclear localization. Western blotting shows that K-80003-stabilized tetrameric form of tRXRα is found exclusively in the nuclear fraction, while tRXRα monomer is distributed both in the nuclear and cytoplasmic fractions[2].

In Vivo

K-80003 is a potent inhibitor of AKT activation by all-trans-retinoic acid. K-80003 displays enhanced efficacy in inhibiting tRXRα-dependent AKT activation and tRXRα tumor growth in animals. K-80003 has high affinity to RXRα but lacks COX inhibitory activity[1].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Cell Assay
[2]

MCF-7 cells cotransfected with Myc-RXRα, Myc-tRXRα, tRXRα/L433D and p85α are pretreated with or without K-80003 (5 μM) for 3 h before exposed to TNFα (10 ng/mL) for 30 min. Cells are immunostained with anti-Myc and anti-p85α antibody, and their subcellular localization revealed by confocal microscopy. HEK293T cells cotransfected with Myc-tRXRα are treated with or without K-80003 (5 μM) for 6 h. Nuclear (N) and cytoplasmic (C) fractions are prepared, subjected to BS3 crosslinking, and analysed by western blotting using anti-Myc antibody. The purity of fractions is examined by analysing the expression of nuclear PARP and cytoplasmic α-tubulin in non-crosslinked fractions. One of three similar experiments is shown[2].

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

Animal Administration
[1]

Mice[1]
Nude mice (BALB/c, 4-5-week old) are injected subcutaneously with 100 μL of cells (2×106). For drug treatment, mice (n=6) are treated intraperitoneally after 7 days of transplantation with Corn oil, Sulindac (60 mg/kg), or K-80003 (60 mg/kg) once every other day (six injections). Body weight and tumor sizes are measured every 4 days.

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

References
Molecular Weight

336.40

Formula

C₂₂H₂₁FO₂

CAS No.

1292821-90-9

SMILES

CC1=C(C2=CC(F)=CC=C2/C1=C(C3=CC=C(C=C3)C(C)C)/[H])CC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere

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Cat. No.: HY-U00458