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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC73848 MBX-102 acid MBX-102 acid is the active form of JNJ39659100 (MBX-102), a selective partial PPAR-γ agonist with EC50 of 23.34 uM (hPPAR-γ), enhances insulin sensitivity in vitro in 3T3-L1 adipocytes, binds to the PPAR-γ LBD in a manner that is distinct from but overla
DC73849 MMT-160 MMT-160 is a novel selective peroxisome proliferator-activated receptor γ (PPARγ) antagonist with IC50 of 0.17 uM, covalently binds to the PPARγ ligand binding domain (LBD) via Cys285.
DC73850 SR10221 SR10221 is a potent, selective PPARγ inverse agonist with IC50 of 13 nM in biochemical peptide recruitment assays, represses downstream PPARγ target genes leading to growth inhibition in bladder cancer cell lines.
DC73851 FKK6 FKK6 (Felix Kopp Kortagere 6) is a specific human pregnane X receptor (hPXR) agonist with IC50 of 1.56 uM in a cell-free competitive hPXR TR-FRET-binding assays.
DC73852 SJPYT-318 SJPYT-318 is a highly selective pregnane X receptor (PXR) agonist, targets PXR ligand-binding domain (LBD), exhibits selectivity for PXR LBD over LXR LBDs for recruiting SRC-1.
DC73853 AG-205 A small molecule inhibitor of progesterone receptor membrane component 1 (PGRMC1) that alters the spectroscopic properties of the PGRMC1-heme complex.
DC73854 AGN196996 AGN 196996 (IRX6696) is a potent selective RARα antagonist with Ki of 2 nM, shows little to no activity against RARβ and RARγ.
DC73855 BPA-B9 Featured BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.
DC73856 CD666 CD666 is a potent, selective RARgamma (RARγ) agonist.
DC73857 E6060 E6060 is a potent, selective retinoic acid receptor subtype α (RAR-α) agonist with Ki of 0.2 nM, IC50 of 0.2 nM for RAR-α-mediated reporter transactivation assays.
DC73858 IRX4647 IRX4647 is a selective RARγ agonist, regulates T cell biology and reduces syngeneic tumor growth of immune checkpoint-resistant lung cancer cell line (344SQ) when combined with anti-PD-L1.
DC73859 LG101506 LG101506 (LG1506) is a potent, selective and orally active RXR modulator with Ki of 2.6 nM.
DC73860 XS-060 XS-060 is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=1.3 uM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.
DC73861 STL1267 STL1267 is a specific, high affinity synthetic agonist of nuclear receptor REV-ERB with EC50 of 0.13 uM and Ki of 0.16 uM, binds directly to the ligand binding domain (LBD) of REV-ERB.
DC73862 BMS-336 BMS-336 is a potent, selective, orally active RORγt (RORC2) inverse agonist with EC50 of 39 nM in RORγt reporter assays.
DC73863 ODH-08 ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect.
DC73864 PCCR-1 PCCR-1 is a potent, specific RORγ inhibitor with binding IC50 of 34.45 nM and 778.1 nM for human and mouse RORγ, respectively, > 300-fold selectivity over other isoforms of ROR.
DC73865 W6134 W6134 (RORγ covalent inhibitor 29) is a first-in-class, potent and selective RORγ covalent inhibitor with IC50 of 0.21 uM, targets the Cys320 of RORγ.
DC73866 CS27109 Featured CS27109 is a potent, selective thyroid hormone receptor-β (THR-β) agonist with AC50 value of 1.98 uM, 12.6-fold selectivity over THR-α.
DC73867 EN171 Featured EN171 covalently targets both C38 and C96 on 14−3−3 to enhance 14−3−3 interactions with ERα, YAP, and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity.
DC73868 CNB-001 CNB-001 is a pyrazole derivative of curcumin with neuroprotective properties, inhibits extracellular Aβ toxicity in hippocampal neurons with EC50 of 400 nM.
DC73869 DDQ DDQ is a small molecule inhibitor of binding sites of Amyloid beta (Aβ) and Drp1, reduces interaction between Aβ and Drp1, shows anti-aging effects.
DC73870 MeSC-04 MeSC-04 is a potent α-Syn amyloid formation inhibitor, reduces the number and size of amyloid fibrils in vitro.
DC73871 NPT200-11 NPT200-11 is an orally bioavailable and brain penetrating alpha-synuclein (ASYN) misfolding and aggregation inhibitor.
DC73872 SRI-42667 SRI-42667 is a selective small-molecule Tau-SH3 interaction inhibitor with IC50 of 0.91 uM (Tau-FynSH3 interaction), prevents amyloid-β toxicity and network hyperexcitability.
DC73873 CC-8977 CC-8977 is a hgihly potent, selective inhibitor of calcium/calmodulin-dependent kinase kinase II (CaMKK2) with binding IC50 of 7 nM.
DC73874 SMP-114 SMP-114 (Rimacalib) is a potent, specific and orally available CaMKII inhibitor with potential for treatment of rheumatoid arthritis.
DC73875 BMS-332 BMS-332 (BMS332) is a potent, selective dual DGKα/ζ inhibitor with IC50 of 9/8 nM respectively.
DC73876 BMS-684 BMS-684 (BMS684) is a potent, selective inhibitor of diacylglycerol kinase α(DGKα) with IC50 of 15 nM, weakly inhibist DGKβ and DGKγ, does not inhibit other DGK lipid kinases.
DC73877 JNJ-3790339 JNJ-3790339 is a potent and selective inhibitor of diacylglycerol kinase α (DGKα), demonstrates similar cytotoxicity in GBM and melanoma cells as ritanserin.

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