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].

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).

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).

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].

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

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

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

CBP EP300 bromodomain receptor-IN-1 (Compound 10) is an inhibitor targeting the bromodomain receptors of CBP EP300, demonstrating nanomolar-level binding affinity with proteins possessing bromodomains.

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.

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

EP300 CBP-IN-1 (compound 172), a potent inhibitor of EP300 CBP, exhibits IC 50 values of 2.1 nM for EP300 BRD and 2.3 nM for CBP BRD. It effectively inhibits the proliferation of prostate cancer CWR22RV1 cells [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-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 CBP ligand 1, classified as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), serves a primary role in synthesis applications.

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-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].

Prostaglandin E2 (PGE2) is a naturally occurring hormone involved in various physiological processes, such as smooth muscle contraction and relaxation, vasodilation and constriction, blood pressure regulation, and inflammatory regulation.

ONO-AE3-208 (AE 3-208) is an EP4 antagonist. It suppresses cell migration, invasion, and metastasis of prostate cancer.

PF-04418948 is a potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).

Treprostinil diethanolamine (UT-15C) is a potent agonist of EP2, DP1, and IP, with values of 3.6, 4.4, and 32.1 nM for EP2, DP1, and IP, respectively, and 212, 826, 2505, and 4680 nM for EP1, EP4, EP3, and FPKi, respectively. Treprostinil diethanolamine contributes to the upregulation of cAMP, maintaining vascular homeostasis and causing vasodilation in human pulmonary arteries.