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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC21600 S1P Lyase inhibitor 31 A potent, selective and orally bioavailable S1P lyase (S1PL) inhibitor with enzyme IC50 of 44 nM, cell IC50 of 110 nM.
DC21464 Eribaxaban A potent, selective and orally efficacious factor Xa (FXa) inhibitor with IC50 of 0.32 nM.
DC25047 Calphostin C A potent, selective and photo-dependent inhibitor of PKC with IC50 of 50 nM.
DC11511 A-485 Featured A potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM.
DC20602 5F 203 Featured A potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway.
DC21576 RO-5508887 A potent, selective BACE inhibitor with IC50 of 30 nM for BACE1, equally potent against BACE2 (IC50=40 nM) but >1,000-fold selectivity over cathepsin D, cathepsin E, pepsin and renin.
DC21103 GW405833 hydrochloride A potent, selective cannabinoid receptor CB2 agonist with Ki of 3.6 nM, 1200-fold selectivity over CB1.
DC20658 AM1241 Featured A potent, selective cannabinoid receptor CB2 agonist with Ki of 7.1 nM, >80-fold selectivity over CB1 receptors in radioligand binding assay.
DC21376 NESS-0327 A potent, selective CB1 cannabinoid receptor antagonist with Ki of 350 fM, >60,000-fold selective for the CB1 receptor versus CB2 receptor (Ki=21 nM).
DC23357 CBP bromodomain inhibitor a potent, selective CBP bromodomain inhibitor with IC50 of 69 nM, displays exquisite selectivity over BRD4(1) (IC50=18 uM) and the broader bromodomain family..
DC22697 PF-04756956 A potent, selective CCK1 receptor agonist with EC50 of 0.47 nM.
DC21393 nNOS-IN-25 A potent, selective cell permeable neuronal nitric oxide synthase (nNOS) inhibitor with Ki of 30 nM.
DC11519 Ceclazepide A potent, selective cholecystokinin receptor CCK2 antagonist for treatment of gastroesophageal reflux disease (GERD)..
DC20633 ACG-548B A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.12 uM, >400-fold selectivity over ChoKβ.
DC20632 ACG-416B A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.13 uM, >385-fold selectivity over ChoKβ.
DC21741 RSM-932A A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.0 uM, 33-fold selectivity over ChoKβ.
DC22917 SCH 79797 dihydrochloride Featured A potent, selective competitive and nonpeptide PAR-1 antagonist with IC50 of 70 nM.
DC20580 Vitacoxib A potent, selective COX-2 inhibitor with IC50 of 0.34 ug/mL, >50-fold selectivity over COX-1 (IC50=19.4 ug/mL).
DC11675 Synta-66 A potent, selective CRAC channel Orai1 blocker with IC50 of 3 uM.
DC22418 CCX-771 A potent, selective CXCR7 antagonist with IC50 of 4.1 nM.
DC22912 SCH39166 A potent, selective D1 dopamine receptor antagonist with Ki of 3.6 nM, >300-fold selectivity over D2 and 5-HT2 receptors.
DC11897 Garvagliptin A potent, selective dipeptidyl peptidase-4 (DPP-4) inhibitor for treatment for type 2 diabetes..
DC12015 SKF 83566 hydrobromide A potent, selective dopamine D1 receptor antagonist with Ki of 0.56 nM.
DC22910 ABT-724 A potent, selective dopamine D4 receptor agonist that activates human dopamine D4 receptors with EC50 of 12.4 nM, with no effect on dopamine D1, D2, D3, or D5 receptors.
DC22909 ABT-724 trihydrochloride A potent, selective dopamine D4 receptor agonist that activates human dopamine D4 receptors with EC50 of 12.4 nM, with no effect on dopamine D1, D2, D3, or D5 receptors.
DC11973 A-412997 A potent, selective dopamine D4 receptor agonist with Ki of 12.1 and 7.9 nM for rat and human D4 receptors, respectively.
DC11866 AZD 3147 Featured A potent, selective dual mTORC1 and mTORC2 inhibitor with enzyme IC50 of 1.5 nM.
DC22586 AZD9496 maleate A potent, selective estrogen receptor downregulator (SERD) with ER downregulation pIC50 of 9.68.
DC20378 FABP4 inhibitor 1 A potent, selective FABP4 inhibitor with Ki of 30 nM..
DC11956 CCG 258748 A potent, selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 8 nM.

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