| 名稱 | TTNPB |
| 描述 | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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). |
| 體外活性 | 通過誘導(dǎo)細(xì)胞凋亡,TTNPB（0.25 mg/kg）可抑制MXT-HI和MXT-HS模型的生長. |
| 體內(nèi)活性 | 在條件培養(yǎng)基培養(yǎng)72 h,TTNPB可使JEG-3細(xì)胞中小鼠mRARα（EC50：2.0 nM）、β（EC50：1.1 nM）以及γ（EC50：0.8 nM）轉(zhuǎn)錄活性增加。TTNPB與核視黃酸受體的結(jié)合親和力較高,從而抑制[3H]tRA與mRARα（IC50：3.8 nM）、 β（IC50：4.0 nM）以及γ（IC50：4.5 nM）的結(jié)合。通過誘導(dǎo)G1細(xì)胞周期阻滯,TTNPB對雌激素受體-陽性乳腺癌細(xì)胞和正常人體乳腺上皮細(xì)胞的生長具有抑制作用。TTNPB濃度依賴性地減少ES-D3細(xì)胞分化。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.18 mg/mL (0.52 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 3.5 mg/mL (10 mM)
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| 關(guān)鍵字 | Autophagy | Inhibitor | Apoptosis | Retinoic acid receptors | RAR/RXR | Ro 13-7410,AGN 191183 | Retinoid X receptors | Ro 13-7410,AGN191183 | TTNPB | AGN 191183 | inhibit | AGN-191183 |
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