pdeδ

K-Ras-PDEδ-IN-1 is a potent inhibitor of competitive K-Ras-PDEδ that binds to the farnesyl binding pocket of PDEδ (Kd of 8 nM).

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

Deltasonamide 2 is a competitive, high-affinity PDEδ inhibitor with a dissociation constant (Kd) of approximately 385 pM.

Deltasonamide 2 hydrochloride is a competitive high-affinity PDEδ inhibitor with a Kd of approximately 385 pM.

Deltasonamide 2 TFA is a competitive, high-affinity PDEδ inhibitor with a Kd of approximately 385 pM.

PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) with a dissociation constant (KD) of 0.410 nM and nicotinamide phosphoribosyltransferase (NAMPT) with an inhibitory concentration (IC50) of 2.21 nM. It disrupts KRAS-related signaling by inhibiting NAMPT's role in the synthesis of nicotinamide adenine dinucleotide (NAD+), consequently inducing apoptosis in pancreatic cancer cells with KRAS mutations. This compound holds potential for research in KRAS-mutant pancreatic cancer.

PDEδ-IN-1 is a ligand for PDEδ and can be utilized in the synthesis of PDEδ autophagic degrader 1.

PDE IV-IN-1 is a potent phosphodiesterase 4 (PDE4) inhibitor with anti-inflammatory activity for the treatment of asthma, chronic obstructive pulmonary disease and other inflammatory diseases, and is a potential compound for the study of depression.

PDE9-IN-1 is a selective and orally bioavailable Inhibitor of PDE9A(IC50 of 8.7 nM).

PDE-9 inhibitor is used for treatment neurodegenerative diseases.

PDE1-IN-2 is an PDE1 inhibitor(PDE1C, PDE1B and PDE1A with IC50 values of 6, 140 and 164 nM, respectvely).

PDE1-IN-3 is a selective inhibitor of human phosphodiesterase 1 (PDE1).

PDE12-IN-3 is an inhibitor of phosphodiesterase 12 (PDE12) (pXC50 of 7.68),with antiviral activity.

PDE2/PDE10-IN-1 is an inhibitor of phosphodiesterase 2 (PDE2) and PDE10, with IC50 values of 29 nM and 480 nM, respectively.

PDE5-IN-2 is a potent, highly selective, and orally active inhibitor of PDE5 (IC50 of 0.31 nM).

PDE4-IN-19 (compound 1) acts as a PDE4 inhibitor and exhibits potent inhibition with IC 50 values below 10 nM for PDE4B1 and between 10-100 nM for PDE4D3.

PDE5-IN-8 (compound 2) is an inhibitor of PDEs.

PDE1-IN-9 (Compound 7a) is a selective inhibitor of phosphodiesterase 1 (PDE1), targeting PDE1C with an IC50 value of 11 nM. It effectively reduces the mRNA expression of IL-1β, IL-6, TNF-α, and iNOS, while also inhibiting the production of nitric oxide (NO) and reactive oxygen species (ROS). Additionally, PDE1-IN-9 demonstrates good metabolic stability in rat liver microsomes.

PDE4-IN-24 (compound 14h) is a potent inhibitor of PDE4D with an IC50 value of 0.57 nM and exhibits over 4100-fold selectivity compared to other PDE families. It plays a significant role in the treatment of inflammatory diseases.

ADORA2A/PDE4D-IN-1 (Compound 9) is a dual inhibitor of the adenosine A2a receptor (ADORA2A) and phosphodiesterase 4D (PDE4D). This compound is applicable for research in bronchial asthma.

PDE2 inhibitor6 (Compound 1) is an orally active phosphodiesterase (PDE) inhibitor, effectively inhibiting PDE2A, PDE3B, and PDE10A2 with IC50 values of 0.95 nM, 6.17 μM (pIC50=5.21), and 87.1 nM (pIC50=7.06), respectively. It modulates AMPA receptor activity, enhances synaptic plasticity, and improves learning and memory in rat models. Furthermore, PDE2 inhibitor6 possesses blood-brain barrier permeability.

PDE3B-IN-1 is a selective phosphodiesterase PDE3B inhibitor, with an IMAP pIC50 of 6.5 and a PDE3B/A selectivity index exceeding 300.

PDE4-IN-15 (compound 7b-1) is a PDE4 inhibitor with an IC50 of 0.17 μM and exhibits anti-TNF-α activity with an EC50 of 0.19 μM. Additionally, PDE4-IN-15 possesses good skin permeability.

PDE3/4-IN-2 is a potent dual PDE3/PDE4 inhibitor with IC50 values of 0.13 nM for PDE3A and 50 nM for PDE4B1. It is used to investigate PDE-related diseases such as asthma, COPD, sepsis, and nephritis. the dual-target activity of PDE3/4-IN-2 provides a mechanistic basis for dissecting cAMP regulation and inflammatory signaling pathways.