TTNPB

Catalog No.S4627 Batch:S462701

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Technical Data

Formula

C24H28O2
Molecular Weight 348.48 CAS No. 71441-28-6
Solubility (25°C)* In vitro DMSO 15 mg/mL (43.04 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
RARβ [1]
(cell-free assay)		 RARα [1]
(cell-free assay)		 RARγ [1]
(cell-free assay)
4.5 nM 5.1 nM 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. [1] TTNPB 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. [2] TTNPB 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. [3] TTNPB causes a concentration-dependent decrease in ES-D3 cell differentiation. [4]
In vivo TTNPB (0.25 mg/kg) causes growth inhibition in both MXT-HS and MXT-HI models by inducing cell apoptosis. [5]

Protocol (from reference)

Kinase Assay:[1]
  • 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]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 Assay:[3]
  • Cell lines

    T47D cells and 184 cells

  • Concentrations

    ~1 μM

  • Incubation Time

    8-12 days

  • Method

    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 (1.4μM), 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.
Animal Study:[5]
  • Animal Models

    Mouse models bearing hormone-sensitive (HS) and hormone-insensitive (HI) strains of the MXT murine mammary carcinoma.

  • Dosages

    ~0.25 mg/kg

  • Administration

    i.p.

Selleck's TTNPB has been cited by 11 publications

Intrafollicular Retinoic Acid Signaling Is Important for Luteinizing Hormone-Induced Oocyte Meiotic Resumption [ Genes (Basel), 2023, 14(4)946] PubMed: 37107703
Induction of mouse totipotent stem cells by a defined chemical cocktail [ Nature, 2022, 10.1038/s41586-022-04967-9] PubMed: 35728625
Generation of mitochondria-rich kidney organoids from expandable intermediate mesoderm progenitors reprogrammed from human urine cells under defined medium [ Cell Biosci, 2022, 12(1):174] PubMed: 36243732
Direct Reprograming of Mouse Fibroblasts into Dermal Papilla Cells via Small Molecules [ Int J Mol Sci, 2022, 23(8)4213] PubMed: 35457029
ATRA-mediated-crosstalk between stellate cells and Kupffer cells inhibits autophagy and promotes NLRP3 activation in acute liver injury [ Cell Signal, 2022, 93:110304] PubMed: 35278669
Identification of hepatic fibrosis inhibitors through morphometry analysis of a hepatic multicellular spheroids model [ Sci Rep, 2021, 11(1):10931] PubMed: 34035369
GATA6-AS1 Regulates GATA6 Expression to Modulate Human Endoderm Differentiation [ Stem Cell Reports, 2020, S2213-6711(20)30291-5] PubMed: 32795420
Bmi1 inhibitor PTC-209 promotes Chemically-induced Direct Cardiac Reprogramming of cardiac fibroblasts into cardiomyocytes. [ Sci Rep, 2020, 28;10(1):7129] PubMed: 32346096
The modification of mitochondrial energy metabolism and histone of goat somatic cells under small molecules compounds induction [ Reprod Domest Anim, 2019, 54(2):138-149] PubMed: 30098220
Chemical reprogramming of mouse embryonic and adult fibroblast into endoderm lineage. [Cao S, et al. J Biol Chem, 2017, 10.1074/jbc.M117.812537] PubMed: 28935668

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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