Home Metabolism Retinoid Receptor agonist TTNPB

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TTNPB Retinoid Receptor agonist

Cat.No.S4627

TTNPB is a potent RAR agonist, and inhibits binding of [3H]tRA with IC50 of 5.1 nM, 4.5 nM, and 9.3 nM for human RARα, β, and γ, respectively.
TTNPB Retinoid Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 348.48

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Quality Control

Batch: Purity: 99.67%
99.67

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells Function assay Agonist activity at human RARalpha expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.18 nM
CV-1 cells Function assay Binding affinity against retinoic Acid gamma receptors co-transfected into CV-1 cells, EC50=0.002 Μm
HL60 cells Cytotoxicity assay In vitro cytotoxicity against HL60 cells, IC50=46 μM
HeLa cells Function assay Agonist activity at human RARalpha expressed in human HeLa cells assessed as relative luminescence units at >=10 uM by luciferase assay relative to control
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 15 mg/mL (43.04 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 348.48 Formula

C24H28O2

 Storage (From the date of receipt)
CAS No. 71441-28-6 Download SDF Storage of Stock Solutions

Synonyms Arotinoid Acid, Ro 13-7410, AGN-191183 Smiles CC(=CC1=CC=C(C=C1)C(=O)O)C2=CC3=C(C=C2)C(CCC3(C)C)(C)C

Mechanism of Action

Targets/IC50/Ki
RARβ
(cell-free assay)
4.5 nM
RARα
(cell-free assay)
5.1 nM
RARγ
(cell-free assay)
9.3 nM
In vitro
TTNPB binds to nuclear retinoic acid receptors with high affinity, inhibits binding of [3H]tRA with IC50 of 3.8 nM, 4.0 nM, and 4.5 nM for mRARα, β, and γ, respectively. This compound increases transcriptional activation of Mouse RARs in JEG-3 cells after 72 h using conditioned media with EC50 of 2.0 nM, 1.1 nM and 0.8 nM for mRARα, β, and γ, respectively. It inhibits the growth of normal human mammary epithelial cells (HMECs) and estrogen receptor-positive (ER-positive) breast cancer cells by inducing G1 cell cycle blockade. This chemical causes a concentration-dependent decrease in ES-D3 cell differentiation.
Kinase Assay
Binding assays
Binding assays are performed as previously described (Allenby et al., 1993, 1994). Briefly, labeled and unlabeled retinoids are added to nucleosol or cytosolic fractions in ethanol so that the total amount of ethanol added is constant in all tubes and did not exceed 2% of the incubation volume. The receptor preparations are incubated with retinoids at 4°C for 4–6 hr. Sephadex PD-10 desalting columns are used to separate bound radioligand from free radioligand after equilib- rium is achieved. For competitive binding assays, varying concentrations of unlabeled competing ligand are incubated with the appropriate nucleosol or cytosol in the presence of a fixed concentration of [3H]tRA (sp. act. 49.3 Ci/mmol) or [3H]9-cis RA (sp. act. 24.0 Ci/mmol). Final concentrations of [3H] tRA and [3H]9-cis RA for nuclear receptor binding assays are 5nM. Final concentrations of [3H] tRA for CRABP binding assays is 30 nM. The IC50s are calculated as described above (DeLean et al., 1978). For saturation kinetics, increasing concentrations of radiolabeled ligand ([3H]tRA sp. act. 49.3 Ci/mmol, [3H]this compound sp. act. 5.5 Ci/ mmol) are added to the nucleosol of the appropriate receptor subtype in the presence (nonspecific binding) or absence (total binding) of a 100-fold molar excess of the corresponding unlabeled retinoid. Specific binding is defined as the total binding minus nonspecific binding. Saturation kinetics are calculated as previously described (Scatchard, 1949; Grippo and Gudas, 1987; Levin et al., 1992).
In vivo
TTNPB (0.25 mg/kg) causes growth inhibition in both MXT-HS and MXT-HI models by inducing cell apoptosis.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/21362465/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9877028/

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