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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
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.
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DC73862 BMS-336
BMS-336 is a potent, selective, orally active RORγt (RORC2) inverse agonist with EC50 of 39 nM in RORγt reporter assays.
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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.
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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.
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DC73859 LG101506
LG101506 (LG1506) is a potent, selective and orally active RXR modulator with Ki of 2.6 nM.
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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.
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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.
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DC73856 CD666
CD666 is a potent, selective RARgamma (RARγ) agonist.
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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.
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DC73853 AG-205
A small molecule inhibitor of progesterone receptor membrane component 1 (PGRMC1) that alters the spectroscopic properties of the PGRMC1-heme complex.
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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.
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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.
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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.
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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.
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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
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DC73847 XCT0135908
XCT0135908 (BRF001) is a highly selective activator of Nurr1-RXR heterodimers, stimulates dopamine (DA) neuron survival.
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DC73846 SA00025
SA00025 is a potent, specific and brain penetrant agonist of Nurr1 (NR4A2) with EC50 of 2.5 nM in HEK293 cells transfected with full length human Nurr1.
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DC73845 BRF110
BRF110 is a potent, selective, brain penetrant and vivo active agonist of Nurr1-RXRα heterodimers with EC50 of 900 nM.
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DC73844 4A7C-301
4A7C-301 is a potent, selective, brain-penetrant agonist of nuclear receptor Nurr1 with EC50 of 6.53 uM, binds to Nurr1 ligand binding domain (LBD) with IC50 of 50 nM.
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DC73843 NC114
NC114 is a small molecule targeting cancer-associated KLF5 transcription factor, decreases the KLF protein but not mRNA levels of KLF in vitro.
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DC73842 sAKZ692
sAKZ692 (sAKZ-692) is a small molecule activator of NRF2 transcriptional activity (EC50=2.2 uM) in cells by inhibiting the glycolytic enzyme pyruvate kinase.
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DC73841 S217879
S217879 (S 217879) is a highly potent and selective NRF2 activator, binds to KEAP1 Kelch domain (SPR Kd=4.15 nM), disrupts the KEAP1-NRF2 interaction leading to robust NRF2 pathway activation.
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DC73840 BC-1901S
BC-1901S is a potent small molecule NRF2 activator that stabilizes NRF2 and increases NRF2 activity, activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner.
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DC73839 TC-D-F07
TC-D-F07 is a novel prodrug of the covalent IRE-1 inhibitor D-F07, inhibits IRE-1/XBP-1s pathway in cancer cells.
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DC73838 PAIR1
PAIR1 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=220 nM) but only partially inhibit its RNase activity.
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DC73837 D-F07
D-F07 is a novel fluorescent, covalent IRE-1 inhibitor, potently inhibits XBP-1s expression in MM cells.
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DC73836 MO-2097
MO-2097 is a small molecule hnRNPA2B1-binding compound (ITC KD=43.1 uM) that suppresses hnRNPA2B1-induced HIF-1α protein expression under hypoxic and mimetic hypoxia.
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DC73835 FG-0041
FG-0041 (FG0041) is a small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 of 2 uM for collagen prolyl hydroxylase.
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DC73834 ER-400583-00
ER-400583-00 is a small-molecule HIF-1α inhibitor, inhibits the induction of HIF-1 reporter activity in response to hypoxia with IC50 of 7.9 nM.
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DC73833 3i-1262
3i-1262 is a small molecule GATA4-acting compound that inhibit the GATA4-NKX2-5 interaction, enhances cardiomyocyte identity and maturity.
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