pde3a

BAY 2666605 is an orally active inhibitor of PDE3A (IC50 = 87 nM) and PDE3B (IC50 = 50 nM) with noted anticancer effects.

Sp-cAMPS sodium salt is an analog of cAMP that serves as a potent activator of cAMP-dependent PKA I and PKA II, and as a competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 μM. It also binds the PDE10 GAF domain with an EC50 of 40 μM [1] [2] [3].

PF-04822163 is a potent inhibitor of PDE1 with IC50 value of 0.0024 μM.

Vesnarinone HCl (OPC-8212 HCl) is an orally active phosphodiesterase 3 (PDE3) inhibitor.Vesnarinone HCl modulates calcium and potassium ions, increasing calcium flux and decreasing potassium flux.Vesnarinone HCl is a new positive inotropic compound that enhances myocardial contractility and can be be used in heart failure studies.

Cilostamide (OPC3689) is a selective phosphodiesterase (PDE)3A and PDE3B inhibitor(IC50 values of 27 and 50 nM, respectively)

(R)-DNMDP is a potent and selective cancer cytotoxic agent that directly binds PDE3A and has an EC50 500-fold lower than that of (S)-DNMDP against HeLa.

DNMDP is a phosphodiesterase 3A inhibitor with clear cell-selective cytotoxicity. DNMDP binding to PDE3A promotes interaction between PDE3A and Schlafen 12.

K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 μM, respectively.

PDE1-IN-8 (Compound 3f) acts as an inhibitor of PDE1, with an IC50 of 11 nM. It hinders cAMP and cGMP signaling pathways, impeding the differentiation and proliferation of cells into myofibroblasts, and demonstrates antifibrotic effects in the Bleomycin-induced rat model of pulmonary fibrosis.

PDE10A inhibitor

Rp-cAMPS TEA salt is a cAMP-dependent protein kinase (PKA) activator.

BRD9500 is an orally active inhibitor of phosphodiesterases 3 (PDE3) with IC 50 s of 10 and 27 nM for PDE3A and PDE3B, respectively. BRD9500 is active in an SK-MEL-3 xenograft model of cancer [1].

PDE1-IN-4 is a potent and selective inhibitor of PDE1 (phosphodiesterase-1), acting on PDE1C (IC50: 10 nM), PDE1A (IC50: 145 nM) and PDE1B (IC50: 354 nM). PDE1-IN-4 regulates cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate) and exhibits antifibrotic effects. PDE1-IN-4 can inhibit TGF-β1-induced differentiation of human lung fibroblasts, and can be used to study idiopathic pulmonary fibrosis (IPF).

Sp-cAMPS triethylamine, a cAMP analog, serves as a potent activator of cAMP-dependent PKA I and II, and acts as a competitive inhibitor of phosphodiesterase (PDE3A) with a K i of 47.6 µM. Additionally, it binds the PDE10 GAF domain with an EC 50 of 40 μM [1] [2] [3].

4'-Methoxyisoagarotetrol, a chromone derivative, exhibits moderate phosphodiesterase 3A (PDE3A) inhibitory activity with an IC50 value of 54 μM [1].

Antitumor Agent-100 (compound A6) is a molecular gel and apoptosis inducer targeting PDE3A-SLFN12 with an IC50 of 0.3 μM, demonstrating potent antitumor activity. This orally available agent binds to the PDE3A enzyme pocket, recruiting and stabilizing SLFN12 which disrupts protein translation and induces apoptosis [1].

OPB-171775 is a molecular glue that forms a ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). This compound induces cell death mediated by SLFN12 RNase, activates the SLFN12 RNase-associated GCN2 signaling pathway, and demonstrates antitumor activity.

Nauclefine (Parvine) is a plant indole alkaloid natural product and induces apoptosis of diverse cancer cells via a PDE3A-SLFN12 dependent death pathway. Nauclefine binds PDE3A but does not inhibit the PDE3A's phosphodiesterase activity.