| S2833 |
UVI 3003
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UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR) with IC50 of 0.24 μM against human RXR.
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Cell Rep, 2023, 10.1016/j.celrep.2023.113369
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Genes (Basel), 2023, 14(4)946
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| S6605 |
AR7
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AR7 is a retinoic acid receptor α (RARα) antagonist. This compound is a potent and selective inhibitor of RARα, demonstrating high affinity and specificity for this receptor subtype. It effectively blocks the binding of retinoic acid to RARα, thereby inhibiting downstream signaling pathways. In cellular assays, this chemical has been shown to suppress the proliferation of various cancer cell lines that are dependent on RARα signaling. Additionally, it induces apoptosis in these cells, highlighting its potential as a therapeutic agent. The pharmacological profile of this antagonist supports its use in studying RARα-mediated processes and in developing treatments for related diseases.
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Phytomedicine, 2024, 136:156286
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| E6637New |
YCT529
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YCT-529 is a selective antagonist of retinoic acid receptor alpha (RARα) developed as a pyrrole-linked analog that potently inhibits RARα with an IC50 of 1.2 nM and greater than 300-fold selectivity over RARβ and RARγ. It also serves as oral non-hormonal male contraceptive effectively reduces sperm counts in mice and non-human primates by targeting the retinoid signaling pathway essential for spermatogenesis.
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| E1767New |
HX531
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HX531 is an orally active antagonist of RXR. This compound enhances activation of the p53–p21Cip1 pathway and abrogates the anti-apoptotic effects of all-trans-retinoic acid (t-RA). It exhibits anti-obesity, anti-diabetic, and anti-melanoma properties.
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