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TTNPB

Catalog No. T1288   CAS 71441-28-6
Synonyms: AGN191183, Arotinoid acid, Ro 13-7410,AGN-191183, Ro 13-7410

TTNPB (Ro 13-7410,AGN-191183), a potent RAR agonist, inhibits binding of [3H]tRA of human RARα (IC50: 5.1 nM), β (IC50: 4.5 nM), and γ (IC50: 9.3 nM), respectively.

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TTNPB Chemical Structure
TTNPB, CAS 71441-28-6
Pack Size Availability Price/USD Quantity
2 mg In stock $ 33.00
5 mg In stock $ 52.00
10 mg In stock $ 79.00
25 mg In stock $ 165.00
50 mg In stock $ 323.00
100 mg In stock $ 488.00
500 mg In stock $ 1,060.00
1 mL * 10 mM (in DMSO) In stock $ 54.00
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Purity: 98.84%
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Biological Description
Chemical Properties
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Description TTNPB (Ro 13-7410,AGN-191183), a potent RAR agonist, inhibits binding of [3H]tRA of human RARα (IC50: 5.1 nM), β (IC50: 4.5 nM), and γ (IC50: 9.3 nM), respectively.
Targets&IC50 RARβ:4.5 nM, RARγ:9.3 nM, RARα:5.1 nM
In vitro By inducing apoptosis, TTNPB (0.25 mg/kg) can inhibit the growth of the MXT-HI and MXT-HS models.
In vivo After 72-hour cultivation in a conditioned medium, TTNPB increases the transcriptional activities of mouse mRARα (EC50: 2.0 nM), β (EC50: 1.1 nM), and γ (EC50: 0.8 nM) in JEG-3 cells. TTNPB exhibits high binding affinity to retinoic acid receptors, thereby inhibiting the binding of [3H]tRA to mRARα (IC50: 3.8 nM), β (IC50: 4.0 nM), and γ (IC50: 4.5 nM). TTNPB inhibits the growth of estrogen receptor-positive breast cancer cells and normal human mammary epithelial cells by inducing a G1 cell cycle arrest. Additionally, TTNPB concentration-dependently reduces the differentiation of ES-D3 cells.
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 5 nM. 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]TTNPB 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).
Cell Research Human mammary epithelial cells are maintained in Mammary Epithelial Basal Medium (MEBM) supplemented with the Mammary Epithelial Growth Media (MEGM) bullet kit. 184 and 184B5 cells are maintained in MEBM sodium-bicarbonate free (MEBM-SBF) supplemented with the MEGM bullet kit, isoproterenol (10 μM), and transferrin (5 μg/ml). MCF10A cell lines are maintained in DME/F12 containing 5% heat inactivated horse serum, penicillin/streptomycin (100 μg/ml and 100 μg/ml), hydrocortisone (1.4 μM), insulin (10 μg/ml), choleratoxin (100 ng/ml), and EGF (20 ng/ml). Breast cancer cell lines are maintained in Improved MEM Zinc Option containing 10% fetal bovine serum, 1% glutamine, and 1% penicillin/streptomycin. For growth assays, cells are treated with the different retinoids for the specified number of days with media and treatment changes every other day in T47D cells and every 2 days in 184 cells. Cell proliferation is measured according to the protocol for the CellTiter 96 Aqueous Non-Radioactive Cell Proliferation Assay. This colorimetric assay determines the number of viable cells in a sample. Each point represents samples done in quadruplicate.(Only for Reference)
Synonyms AGN191183, Arotinoid acid, Ro 13-7410,AGN-191183, Ro 13-7410
Molecular Weight 348.48
Formula C24H28O2
CAS No. 71441-28-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.5 mg/mL (10 mM)

TargetMolReferences and Literature

1. Pignatello MA, et al. Toxicol Appl Pharmacol. 1997, 142(2), 319-327. 2. Pignatello MA, et al. Toxicol Appl Pharmacol. 1999, 159(2), 109-116. 3. Wu K, et al. Breast Cancer Res Treat. 2006, 96(2), 147-157. 4. Louisse J, et al. Toxicol Lett. 2011, 203(1), 1-8. 5. Darro F, et al. Breast Cancer Res Treat. 1998, 51(1), 39-55.

Related compound libraries

This product is contained In the following compound libraries:
NO PAINS Compound Library Nuclear Receptor Compound Library Target-Focused Phenotypic Screening Library Stem Cell Differentiation Compound Library Lipid Metabolism Compound Library Bioactive Compound Library Neuronal Differentiation Compound Library Autophagy Compound Library Bioactive Compounds Library Max Metabolism Compound Library

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Keywords

TTNPB 71441-28-6 Apoptosis Autophagy Metabolism Retinoid Receptor Inhibitor Retinoic acid receptors RAR/RXR AGN191183 Arotinoid acid Ro 13-7410,AGN-191183 Ro 13-7410,AGN 191183 Retinoid X receptors Ro 13-7410,AGN191183 AGN 191183 Ro 13-7410 inhibit AGN-191183 inhibitor

 

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