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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC11865 DS-5272 A potent and orally active p53-MDM2 interaction inhibitor with IC50 of 2.4 nM.
DC11743 BMS-681 A potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.
DC22772 ANI-7 A potent and selective (up to 263-fold) inhibitor of breast cancer cells with GI50 of 0.5 uM (MCF-7), via activation the aryl hydrocarbon receptor (AhR) pathway.
DC22622 WAY-100635 A potent and selective 5-HT1A receptor antagonist.
DC21471 PF-03246799 A potent and selective 5-HT2C receptor agonist with EC50 of 190 nM, with excellent selectivity for 5-HT2C over 5-HT2A.
DC22368 Alosetron A potent and selective 5-HT3 receptor antagonist has been shown to be beneficial in the treatment of irritable bowel syndrome..
DC23952 GR-79236 Featured GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.
DC20655 AM-1221 A potent and selective agonist for the cannabinoid receptor CB1 with Ki of 0.28 nM, 180-fold selectivity over CB2..
DC22498 A-443654 Featured A potent and selective Akt inhibitor with Ki of 0.16 nM for Akt1.
DC23832 ALK5-IN-16i A potent and selective ALK5 inhibitor with IC50 of 5.5 nM, displays 300-fold selecitvity over ALK3.
DC22583 AMD-070 hydrochloride(Mavorixafor) Featured A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.
DC22376 Pitolisant oxalate A potent and selective antagonist of H3 receptor with Ki/EC50 of 0.16/1.5 nM.
DC22377 Pitolisant A potent and selective antagonist of H3 receptor with Ki/EC50 of 0.16/1.5 nM.
DC24108 CCT241533 A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM.
DC11654 VRX-0466617 A potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM.
DC22382 SB-277011 A potent and selective dopamine D3 receptor antagonist with pKi of 8.0.
DC22691 MK-4618 Featured A potent and selective full β3 adrenergic receptor agonist with EC50 of 1.1 nM.
DC22340 Linaclotide Featured A potent and selective GC-C agonist (Ki=1.23-1.64 nM) that elicits pharmacological effects locally in the gastrointestinal tract.
DC24162 Bitopertin R enantiomer A potent and selective GlyT1 inhibitor with EC50 of 54 nM.
DC24100 LY2365109 hydrochloride Featured A potent and selective GlyT1 inhibitor with IC50 of 15.8 nM, displays no activity for GlyT2 (IC50>30 uM).
DC11705 GPR30 inhibitor G1 Featured A potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.
DC11672 G-9791 A potent and selective group I PAK (pan-PAK1/2/3) inhibitor with Ki of 0.95/2 nM for PAK1/2, respectively.
DC21716 T247 A potent and selective HDAC3 inhibitor with IC50 of 0.24 uM, >75-fold selectivity over HDAC1 and no activity against HDAC4/6/8.
DC21717 T326 A potent and selective HDAC3 inhibitor with IC50 of 0.26 uM, with no activity against HDAC1/4/6/8.
DC11596 SB-379278A A potent and selective HDAC8 inhibitor with IC50 of 0.5 uM..
DC11595 NCC-149 A potent and selective HDAC8 inhibitor with IC50 of 70 nM.
DC23214 ABT-239 A potent and selective Histamine H3 receptor antagonist with Ki of 0.1-5.8 nM (human, rat H3).
DC23723 BMS-711939 A potent and selective human PPARα agonist with EC50 of 4 nM, >1,000-fold selectivity over human PPARγ (EC50=4.5 uM) and PPARδ (EC50 >100 uM) in PPAR-GAL4 transactivation assays.
DC23452 TAK-259 hydrochloride A potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM.
DC23428 TAK-259 A potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM.

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