Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C28H27NO2S |
| Molecular Weight | 441.584 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1(C)CCC(C)(C)C2=C1C=C3SC4=CC=CC=C4N=C(C5=CC=C(C=C5)C(O)=O)C3=C2
InChI
InChIKey=PFGCWQPTOKPRRK-UHFFFAOYSA-N
InChI=1S/C28H27NO2S/c1-27(2)13-14-28(3,4)21-16-24-19(15-20(21)27)25(17-9-11-18(12-10-17)26(30)31)29-22-7-5-6-8-23(22)32-24/h5-12,15-16H,13-14H2,1-4H3,(H,30,31)
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/9435893 | https://www.ncbi.nlm.nih.gov/pubmed/26883505Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26714014 https://www.ncbi.nlm.nih.gov/pubmed/24916544
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9435893 | https://www.ncbi.nlm.nih.gov/pubmed/26883505
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26714014 https://www.ncbi.nlm.nih.gov/pubmed/24916544
HX630 is a synthetic RXR pan-agonist. HX-630 has bein shown to exert anti-proliferative and pro-apoptotic effects in murine pituitary corticotroph tumor AtT20 cells, making HX-630 a new therapeutic candidate for Cushing’s disease. It might also serve as potential pharmacological tool for treating retina degenerative diseases and Alzheimer's disease.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2363070 |
|||
Target ID: CHEMBL2061 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9435893 |
900.0 nM [Ki] | ||
Target ID: CHEMBL1870 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9435893 |
400.0 nM [Ki] | ||
Target ID: CHEMBL2004 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9435893 |
620.0 nM [Ki] | ||
Target ID: CHEMBL2008 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9435893 |
320.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| The ATRA-dependent overexpression of the glutamate transporter EAAC1 requires RARbeta induction. | 2009-09 |
|
| 9-cis-Retinoic acid (9cRA), a retinoid X receptor (RXR) ligand, exerts immunosuppressive effects on dendritic cells by RXR-dependent activation: inhibition of peroxisome proliferator-activated receptor gamma blocks some of the 9cRA activities, and precludes them to mature phenotype development. | 2007-05-15 |
|
| Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. | 1997-12-19 |
|
| Action mechanism of retinoid-synergistic dibenzodiazepines. | 1997-04-07 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26714014
Mice: 5 mg/kg/day, injected intraperitonealy 3 times a week for 3 weeks
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26714014
HX-630 significantly suppressed AtT20 cell proliferation at 10 uμM
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ACTIVE MOIETY