In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO
40%PEG300
5%Tween80
50%ddH2O
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
5.000mg/ml
(14.35mM)
Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
* <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.)
Preparing Stock Solutions
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 (cell-free assay)
RARα (cell-free assay)
RARγ (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. 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.
In Vivo
TTNPB (0.25 mg/kg) causes growth inhibition in both MXT-HS and MXT-HI models by inducing cell apoptosis.
Binding assays are performed as previously described (Allenby et al., 1993, 1994). Briefly, labelled and unlabelled 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 equilibrium is achieved. For competitive binding assays, varying concentrations of unlabelled 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 radiolabelled 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 (non-specific binding) or absence (total binding) of a 100-fold molar excess of the corresponding unlabelled retinoid. Specific binding is defined as the total binding minus non-specific binding. Saturation kinetics are calculated as previously described (Scatchard, 1949; Grippo and Gudas, 1987; Levin et al., 1992).
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 this compound 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.
Chemoresistance-motility signature of molecular evolution to chemotherapy in non-muscle-invasive bladder cancer and its clinical implications
[ Cancer Lett, 2025, 610:217339]
[C6TSEDRVAJZ, a combination of small-molecule compounds, induces differentiation of human placental fibroblasts into epithelioid cells in vitro]
[ Nan Fang Yi Ke Da Xue Xue Bao, 2025, 45(2):322-330]
A noncoding variant confers pancreatic differentiation defect and contributes to diabetes susceptibility by recruiting RXRA
[ Nat Commun, 2024, 15(1):9771]
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]
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
