cd2665  (Tocris)

Journal: Clinical and Translational Medicine

Article Title: ZSH‐2208: A novel retinoid with potent anti‐tumour effects on ESCC stem cells via RARγ–TNFAIP3 axis

doi: 10.1002/ctm2.70148

Figure Lengend Snippet: ZSH‐2208 inhibits the transcription of TNFAIP3 through reducing the expression of protein of RARγ. (A) Pattern diagram of molecular docking simulation of ZSH‐2208 to RARγ protein. (B–D) Effect of ZSH‐2208 on RARγ protein and gene expression levels in ESCC‐TRCs. (E) Heatmap of the significantly upper (lower)—modulated differentially expressed gene (DEGs) Top50 after ZSH‐2208 treatment. (F) Combined analysis of sequencing by RNA‐seq and ChIP‐seq identified TNFAIP3, a key effector molecule for ZSH‐2208. (G) ZSH‐2208 treatment significantly reduced the binding peak of RARγ protein in the promoter region of TNFAIP3 gene. (H) Three possible binding sites for the RARγ protein on the TNFAIP3 gene promoter. (I) Effect of ZSH‐2208 on TNFAIP3 and TNIP1 at protein level in ESCC‐TRCs. (J) Immunofluorescence staining of TNFAIP3 protein was performed in subcutaneous tumour tissues of nude mice to observe the effect of ZSH‐2208 on TNFAIP3 protein expression. DOX, doxorubicin; red, TNFAIP3: blue. (K–M) Effect of CD2665 on TNFAIP3 and TNIP1 at gene and protein level in ESCC‐TRCs (* p < .05, ** p < .01, *** p < .001, **** p < .0001; ns, not significant).

Article Snippet: Additionally, we treated ESCC‐TRCs with CD2665 (MCE, HY‐107437, USA), a selective antagonist of RARγ, and observed a reduction in the expression levels of both TNFAIP3 and TNIP1 at the gene level.

Techniques: Expressing, Sequencing, RNA Sequencing Assay, ChIP-sequencing, Binding Assay, Immunofluorescence, Staining

Journal: bioRxiv

Article Title: Retinoid-impregnated nanoparticles enable control of bone growth by site-specific modulation of endochondral ossification in mice

doi: 10.1101/2024.11.08.622655

Figure Lengend Snippet: RARγ agonists strongly affect cultured chondrocyte function. Epiphyseal chondrocytes isolated from neonatal mice were treated with vehicle ethanol, retinoic acid (100 nM, RA), RARα agonist (AGN195183, 300 nM), RARβ agonist (BMS453, 300 nM) or RARγ agonist (NRX204647, 100 nM) 2 days after plating. A, Phase contrast images 4 days after treatment. B, Total RNAs were prepared 4 days after treatment and subjected to qPCR to examine expression levels of Sox 9 , Acan , Col9a1 , Ihh , C ol10a1 , Mmp3 and Tnfs11 ( Rankl ). n=3/group. Individual values, average and standard deviation (SD) are shown.

Article Snippet: Retinoic acid, BMS453 (RARβ agonist, CAS166977-43-1) and CD2665 (RARβ/γ antagonist, CAS 170355-78-9) were purchased from Tocris Biosciences (Bristol, UK).

Techniques: Cell Culture, Isolation, Expressing, Standard Deviation

Journal: bioRxiv

Article Title: Retinoid-impregnated nanoparticles enable control of bone growth by site-specific modulation of endochondral ossification in mice

doi: 10.1101/2024.11.08.622655

Figure Lengend Snippet: RARγ signaling dominantly affects skeletal growth. A-C, C57BL/6J female mice were treated with corn oil (Control), selective agonists of RARα (AGN195183, 4 mg/kg), RARβ (BMS453, 4 mg/Kg), RARγ (NRX204647, 1 mg/Kg) or antagonist for RARγ (CD2665 and 7C, 4 mg/kg) via peritoneal injections (11 days of age) or gavage (over 14 days of age) starting at 11 days of age every other day. The hind limbs were harvested at and subjected to radiological examination. (A) Gross appearance 8 days after initial treatment (19 days of age). (B) Radiological views of the knee joints 8 days after initial treatment (19 days of age). Arrows indicate the proximal tibial growth plate. Note RARγ-agonist treated group (right panel) showed closure of growth plate. (C) Body length was measured 8 days after initial treatment (19 days of age). D, C57BL/6J female and male mice were treated with corn oil (Control) or selective agonists of RARγ (NRX204647, 1 mg/Kg) via peritoneal injections starting at 14 days of age every other day. The hind limbs were harvested at 22 days of age and subjected to radiological examination. The tibia and femur lengths were measured by ImageJ. Individual values, average and standard deviation (SD) are shown.

Article Snippet: Retinoic acid, BMS453 (RARβ agonist, CAS166977-43-1) and CD2665 (RARβ/γ antagonist, CAS 170355-78-9) were purchased from Tocris Biosciences (Bristol, UK).

Techniques: Control, Standard Deviation