rarβ antagonist le135  (Tocris)

Journal: Journal of translational medicine

Article Title: Notch3 enhances the synergistic effect of all-trans retinoic acid and calcipotriol in pancreatic stellate cell activation.

doi: 10.1186/s12967-025-06666-1

Figure Lengend Snippet: Fig. 9 ATRA and calcipotriol are independent of RARβ and VDR to regulate Notch3. Western blot analysis of the expression of Notch3 and the nuclear receptors RARβ and VDR after LE135 binding to ATRA or calcipotriol. A LE135 binding to ATRA for incubation of quiescent or activated PSCs (n = 3, *p < 0.05, **p < 0.01, ***p < 0.001). B Results of LE135 binding to calcipotriol for the incubation of quiescent or activated PSCs (n = 3, *p < 0.05, **p < 0.01, ***p < 0.001)

Article Snippet: The LE135 RAR antagonist was purchased from MedChemExpress (MCE), dissolved in DMSO at 50 mg/ml, and stored at − 80 °C.

Techniques: Western Blot, Expressing, Binding Assay, Incubation

Journal: Frontiers in Pharmacology

Article Title: Canagliflozin alleviates progestin resistance by suppressing RARβ/CRABP2 signaling in THRB knockout endometrial cancer cells

doi: 10.3389/fphar.2025.1573032

Figure Lengend Snippet: Interaction and regulation of TRβ, RARβ and CRABP2. (A) The interaction between TRβ and the RARβ promoter assayed by EMSA. The “bound band” was a key indicator. It represented the complex where TRβ attaches to the RARβ promoter DNA, migrating sluggishly in the gel due to the increased molecular mass from this union. In contrast, the “free band” meant the unbound RARβ promoter DNA, i.e., a smaller size protein migrated more rapidly through the gel, providing a baseline to confirm the specific binding event. (B,C) Relative fluorescence intensity between TRβ and RARβ promoter binding assayed by dual luciferase reporter gene. The value of Luc/RLuc was the relative fluorescence intensity. EV represented empty vector. The stronger fluorescence intensity indicated the stronger binding ability of TRβ to the RARB promoter. (D,E) Inhibitory effects of LE135, the RARβ inhibitor, on the expression of CRABP2 in a concentration-dependent manner. (F) Effects of RARβ regulated the CRABP2 promoter via EMSA assay. The results were presented as the mean ± SEM from three independent experiments with triplet repeat of each data. ** p < 0.01, **** p < 0.0001 compared with control group.

Article Snippet: Canagliflozin (CANA), acarbose, atorvastatin and LE135 were purchased form MCE (Monmouth Junction, United States).

Techniques: Binding Assay, Fluorescence, Luciferase, Plasmid Preparation, Expressing, Concentration Assay, Control

Journal: EMBO Reports

Article Title: Rarγ-Foxa1 signaling promotes luminal identity in prostate progenitors and is disrupted in prostate cancer

doi: 10.1038/s44319-024-00335-y

Figure Lengend Snippet: Reagents and tools table

Article Snippet: RARβ antagonist (LE135) , Cayman , 14415.1.

Techniques: Recombinant, Sequencing, Software