EP3

EP3 antagonist 4 is an EP3 antagonist that inhibits hEP with a Ki of 2 nM. EP3 antagonist 4 showed low in vivo clearance, high oral AUC and good bioavailability in complete PK studies in rats. EP3 antagonist 4 can be used to study diabetes and cellular dysfunction.

EP3, an antimicrobial peptide, exhibits both antibacterial and antifungal activities, effectively inhibiting E. gallinarum, P. pyocyanea, A. baumanii, and K. terrigena with a minimum inhibitory concentration (MIC) of 12.85 μg/mL. Additionally, EP3 demonstrates antitumor activity against cancer cells, inducing cell apoptosis [1].

AH 6809 is an antagonist of EP and DP receptors, with Ki values of 1217, 1150, 1597, and 1415 nM for the cloned human EP1, EP2, EP3-III, and DP receptors, respectively, and a Ki of 350 nM for the mouse EP2 receptor.

DG-041 is an antagonist of high-affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively). DG-041 inhibits PGE2 facilitation of platelet aggregation and has the blood-brain barrier permeability.

L-798106 (CM9) is a selective and potent prostaglandin-like EP3 receptor antagonist that inhibits EP4, EP1, and EP2 receptors, suppresses levels of pro-inflammatory cytokines in atherosclerosis, and attenuates PGE2-induced cough.

Prostaglandin E1 (Alprostadil) is the naturally occurring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Prostaglandin E1 is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

Treprostinil Sodium (UT-15) is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM).

Travoprost (Fluprostenol isopropyl ester) is used to treat glaucoma and ocular hypertension,is a potent and selective FP prostaglandin receptor agonist.

EP3 antagonist 3, a potent and selective EP3 antagonist with the advantage of oral activity, significantly inhibited GR63799- or acetic acid-induced reduction in bladder capacity and PGE2-induced overactive bladder model in spontaneously hypertensive rats (SHR).

Compound 22, known as EP3 antagonist 5, serves as an antagonist to the EP3 receptor, exhibiting an IC50 value of 67 nM [1].

EP3 antagonist 7 (Compound II), an EP3 receptor antagonist, is applicable in researching conditions such as itching, pain, dysuria, or stress disorders [1].

EP3 antagonist 6 (compound 5), a selective and orally active EP3 receptor antagonist, exhibits potent activity with an IC 50 of 1.9 nM. It effectively inhibits PGE2-induced uterine contractions in pregnant rats [1].

KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing,

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor.

EP39, a potent HIV-1 maturation inhibitor, binds to the QVT motif within the SP1 domain of Gag, reducing the dynamics at the CA-SP1 junction and disrupting the coil-helix equilibrium adjacent to the SP1 domain by stabilizing the transient alpha-helical structure. This action arrests HIV-1 maturation, effectively blocking its infectivity.

Ep300/CREBBP-IN-8 (Example 37), a potent and orally active inhibitor of Ep300 and CREBBP, shows IC50 values of 0.014 μM and 0.018 μM, respectively, and is utilized in cancer research [1].

Ep300/CREBBP-IN-2 (Example 73) is a potent, orally bioavailable inhibitor of Ep300 and CREBBP, with IC50 values of 0.052 μM and 0.148 μM, respectively, and is used in cancer research [1].

Ep300/CREBBP-IN-3 (Example 61), a potent inhibitor of Ep300 and CREBBP with IC50 values of 0.056 μM and 0.095 μM, respectively, is applicable in cancer research [1].

Ep300/CREBBP-IN-4 (Example 56), a potent inhibitor of both Ep300 and CREBBP, shows IC50 values of 0.024 μM and 0.064 μM, respectively, and is employed in cancer research [1].

EP300/CBP ligand 1, classified as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), serves a primary role in synthesis applications.

EP300/CBP ligand 2 (compound S19) serves as a specific ligand for the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). It plays a critical role in PROTAC technology by acting as a target protein ligand. By linking to an E3 ubiquitin ligase ligand via the PROTAC Linker, it facilitates the synthesis of PROTAC molecules capable of targeted protein degradation. For instance, when EP300/CBP ligand 2 is connected to the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc, it results in the formation of the PROTAC molecule dCE-2.

AtPep3 is a hormone-like peptide that plays a role in the salinity stress tolerance of plants.

AtPep3 TFA is a hormone-like peptide that plays a role in the salinity stress tolerance of plants.