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-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).

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.

PDE5-IN-14 (Compound 14a) is a brain-penetrating competitive inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 16.11 nM. It holds potential for research into Alzheimer's disease (AD), cancer, and cardiovascular diseases.

PDE4-IN-29 (Compound 55) is an orally active and selective inhibitor of PDE4, targeting subtypes such as PDE4A1, PDE4B2, and PDE4D3, with an IC50 value for PDE4D3 of less than 5 nM. It inhibits the degradation of cyclic adenosine monophosphate (cAMP), elevating intracellular cAMP levels and suppressing the release of inflammatory mediators like TNF-α. PDE4-IN-29 holds potential for research in inflammatory diseases such as psoriasis, atopic dermatitis, and chronic obstructive pulmonary disease.

PDE5-IN-15 (compound 21) is a xanthine derivative and PDE5 inhibitor with IC50 values of 0.002 μM for hPDE5, 0.180 μM for bPDE6, 2.85 μM for bPDE1, and 2.22 μM for hPDE3. It exhibits good oral bioavailability in dogs and is applicable in research related to male erectile dysfunction.

PDE4B-IN-6 (Compound 4i) is a potent and highly selective inhibitor of phosphodiesterase 4B (PDE4B) with an IC50 of 7.42 nM. As a roflumilast analogue, it exhibits significantly higher selectivity for PDE4B over PDE4A (IC50 = 1540 nM, ~195-fold) and PDE4C (IC50 = 1260 nM, ~169-fold). PDE4B-IN-6 exerts anti-inflammatory effects by elevating intracellular cAMP levels and suppressing the expression of the pro-inflammatory cytokine TNF-α. Additionally, it demonstrates good antioxidant properties and low cytotoxicity, making it suitable for research on chronic obstructive pulmonary disease (COPD) and related inflammatory conditions.

PDE7-IN-2 is an inhibitor of phosphodiesterase 7 (IC50 = 2.1 µM) and can be used in Parkinson's disease studies.

PDE5-IN-42 is a selective inhibitor of second-generation phosphodiesterase type 5 (PDE5).

PDE4B-IN-2 (A 33) is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 µM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.