Nuclear Receptors
The nuclear receptor superfamily describes a related but diverse array of transcription factors (nuclear hormones). Upon activation by glucocorticoids, mineralocorticoids, sex steroids (estrogen, progesterone, and androgen), thyroid hormones, or vitamin D3, the nuclear receptors can bind a highly specific DNA sequence[1]. As a result, they regulate the expression of adjacent genes, thereby controlling the development, homeostasis, and metabolism of the organism. In the human genome, 48 different nuclear receptors are encoded, which can be classified into 6 evolutionary groups, based on their sequence alignment and phylogenetic tree[2]. All NR proteins exhibit a characteristic modular structure that consists of five to six domains of homology on the basis of regions (A-F) of conserved sequence and function. The DNA-binding domain (DBD, region C), absent in DAX-1 and SHP, and the ligand-binding domain (LBD; region E) are the most highly conserved domains. These two regions are the most important and can function independently.
[1] Nuclear Receptor Minireview Series. J.M. Olefsky. J. Biol. Chem. 2001, 276, 36863-36864.
[2] Overview of Nomenclature of Nuclear Receptors. P. Germain et al. Pharmacol Rev 2006, 58, 685-704.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2239 | (+)-ZK 216348 | Selective nonsteroidal glucocorticoid receptor (GR) agonist | €125.00 | |
| 3928 | (R)-SKBG-1 | Covalent RNA-binding protein NONO ligand | €160.00 | |
| 3704 | (S)-ErSO | Inactive enantiomer of ErSO | €180.00 | |
| 3929 | (S)-SKBG-1 | Inactive enantiomer of (R)-SKBG-1 | €150.00 | |
| 4093 | (Z)-4-Hydroxytamoxifen | The more active metabolite of Tamoxifen (SERM; Axon 3252) | €110.00 | |
| 2221 | (Z)-Endoxifen | The more active (Z)-isomer of Endoxifen (SERM; Axon 2190) | €150.00 | |
| 4081 | 4A7C-301 | Brain-penetrant Nurr1 agonist | €130.00 | |
| 2948 | AM 580 | RAR-α agonist | €95.00 | |
| 3742 | Apararenone | Potent and highly selective nonsteroidal mineralocorticoid receptor (MR) antagonist | €130.00 | |
| 2679 | AR7 | RARα antagonist that stimulates chaperone-mediated autophagy | €90.00 | |
| 1979 | ARN 509 | Antagonist of androgen receptor (AR) | €95.00 | |
| 1675 | Asoprisnil | Progesterone receptor (PR) modulator | €130.00 | |
| 3904 | BAY-0069 | Potent covalent PPARγ inverse agonist | €90.00 | |
| 3809 | BAY-4931 | Potent covalent PPARγ inverse agonist | €120.00 | |
| 2051 | Bazedoxifene acetate | Selective estrogen receptor modulator (SERM) | €80.00 | |
| 1748 | Bazedoxifene hydrochloride | Selective estrogen receptor modulator (SERM) | €70.00 | |
| 3882 | Beclomethasone dipropionate | Glucocorticoid | €50.00 | |
| 1700 | Bexarotene | Retinoid X Receptor antagonist | €65.00 | |
| 2790 | BHPI | ER-α antagonist | €125.00 | |
| 1940 | BI 6015 | Potent hepatocyte nuclear factor 4α (HNF4α) antagonist | €120.00 | |
| 3313 | Bicalutamide | Androgen receptor (AR) antagonist | €50.00 | |
| 1194 | BMS 189961 | RAR-γ agonist | €145.00 | |
| 1173 | BMS 270394 | RAR-γ agonist | €165.00 | |
| 4232 | BMS-986365 | Highly potent and selective androgen receptor (AR) degrader | Recently added | €150.00 |
| 1676 | BXL 628 | Vitamin D receptor (VDR) agonist | €150.00 | |
| 2575 | C-DIM12 | Nurr1 activator that stimulates apoptosis in bladder cancer cells | €85.00 | |
| 2828 | C-DIM5 | Nur77 agonist | €95.00 | |
| 2827 | C-DIM8 | Nur77 antagonist | €95.00 | |
| 2964 | CD12681 | Potent RORγ inverse agonist | €135.00 | |
| 1950 | CDDO | A potent multifunctional anti-tumor agent. PPAR-γ agonist | €80.00 | |