|S2131||Roflumilast||<1 mg/mL||81 mg/mL||15 mg/mL|
|S1431||Sildenafil Citrate||<1 mg/mL||20 mg/mL||<1 mg/mL|
|S1512||Tadalafil||<1 mg/mL||78 mg/mL||<1 mg/mL|
|S2515||Vardenafil HCl Trihydrate||10 mg/mL||100 mg/mL||20 mg/mL|
|S1550||Pimobendan||<1 mg/mL||67 mg/mL||5 mg/mL|
|S5836||IBMX||<1 mg/mL||44 mg/mL||7 mg/mL|
|S5806||Cilostamide||<1 mg/mL||6 mg/mL||5 mg/mL|
|S9436||Pinoresinol dimethyl ether||-1 mg/mL||77 mg/mL||-1 mg/mL|
|S4837||Ibudilast||30 mg/mL||46 mg/mL||46 mg/mL|
|S2620||GSK256066||<1 mg/mL||5 mg/mL||<1 mg/mL|
|S2687||PF-2545920||<1 mg/mL||78 mg/mL||78 mg/mL|
|S1430||Rolipram||<1 mg/mL||55 mg/mL||55 mg/mL|
|S8034||Apremilast (CC-10004)||<1 mg/mL||92 mg/mL||<1 mg/mL|
|S1294||Cilostazol||<1 mg/mL||74 mg/mL||6 mg/mL|
|S4019||Avanafil||<1 mg/mL||97 mg/mL||<1 mg/mL|
|S2127||S- (+)-Rolipram||<1 mg/mL||55 mg/mL||55 mg/mL|
|S3172||Anagrelide HCl||<1 mg/mL||14 mg/mL||<1 mg/mL|
|S1504||Dyphylline||51 mg/mL||51 mg/mL||<1 mg/mL|
|S1895||Dipyridamole||<1 mg/mL||101 mg/mL||50 mg/mL|
|S4164||Doxofylline||24 mg/mL||53 mg/mL||2 mg/mL|
|S4090||Fenspiride HCl||59 mg/mL||9 mg/mL||<1 mg/mL|
|S7224||Deltarasin||<1 mg/mL||100 mg/mL||100 mg/mL|
|S8459||TAK-063||<1 mg/mL||85 mg/mL||<1 mg/mL|
|S2291||Diosgenin||<1 mg/mL||<1 mg/mL||5 mg/mL|
|S2312||Icariin||<1 mg/mL||50 mg/mL||<1 mg/mL|
|S4683||Sildenafil Mesylate||100 mg/mL||100 mg/mL||4 mg/mL|
|S4684||Sildenafil||14 mg/mL||<1 mg/mL||<1 mg/mL|
|S2320||Luteolin||<1 mg/mL||57 mg/mL||3 mg/mL|
|S8218||PF-8380||<1 mg/mL||95 mg/mL||<1 mg/mL|
|S2368||Theobromine||<1 mg/mL||<1 mg/mL||<1 mg/mL|
|S9229||Linderane||-1 mg/mL||52 mg/mL||-1 mg/mL|
Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.
Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6).
Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.
ADOR lung cancer cells (a July 2015 PDX model) were transfected with an empty vector plasmid or plasmids to express GRP78 and HSP27 together. Twenty-four hours after transfection cells were treated with vehicle control or with OSU-03012 (2.0mM) sildenafil (2mM) for 6 h after which cells were fixed in place and permeabilized using 0.5% Triton X100. Immuno-fluorescence was performed to detect the expression levels of Calnexin; glucosidase I; and glucosidase IIa at 10 magnification using a Hermes WiScan system.
Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11
(a): E. coli bacteria transformed to be resistant to ampicillin and kayamycin (AMPr KAYAr) were grown in AMPt KAYAt media and cells treated with OSU-03012 (2 μM); sildenafil (2 μM); tadalafil (2 μM), or in combination as indicated. Bacterial cell numbers were determined by assessing the protein concentration of the bacterial cell pellet 3 h, 6h and 12 h after drug exposure * P<0.05 less than corresponding vehicle value. The total protein content of each treatment condition was determined 3 h after addition of antibiotic. Portions of bacteria from each treatment condition were isolated and SDS PAGE and immuno-blotting performed to determine the expression of Dna J, Dna K, RecA and GrpE. (b): E. coli bacteria Gram stained and examined under a X100 oil immersion magnification.
Vardenafil HCl Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
(G) Immunoblot analysis for TAZ and Nanog in PCSC after vardenafil treatments. (H) Cytotoxicity to DDP in PCSC treated with indicated concentrations of vardenafil. **p < 0.01, *p < 0.05 versus PC3 cells, vardenafil at 0 μM, or DDP at 0 μM; ++p < 0.01, +p < 0.05 versus vardenafil at 0 μM.
Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
Isobutylmethylxanthine (IBMX) is a nonspecific inhibitor of phosphodiesterase (PDE) with IC50 values of 6.5±1.2, 26.3±3.9 and 31.7±5.3 μM for PDE3, 4 and 5 respectively. It may enhance the intracellular cAMP levels and also acts as an adenosine (A1) receptor antagonist.
Cilostamide is an inhibitor of type III phosphodiesterases with IC50 values of 27 nM and 50 nM for PDE3A and PDE3B, respectively.
Pinoresinol dimethyl ether, which could be isolated from the wood of the basal tree Humbertieae, show a variety of activities as the inhibitor of cyclic AMP phosphodiesterase.
Ibudilast is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2.
PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.
The PDE4 selective inhibitor, rolipram, inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.
D, average percentage difference of cell growth by PDE4D inhibitors between STK11 mutant and wild-type cell lines. The sensitivity on STK11mt cell lines represents the difference of average percentage growth between STK11-mutant (NCI-H1993 and NCI-H1395) and wild-type cell lines (NCI-H82 and NCI-H524). Average percentage growth of each cell line by a PDE4D inhibitor was based on the DMSO control. Cells were treated with a 20 μmol/L of PDE4D inhibitors for 3, 7, and 10 days incubation, respectively. The cell viability was determined using CellTiter-Blue fluorescence. *, P < 0.01 and **, P < 0.05 in the difference between STK11-mutant and wild-type cell lines. All cells used in the experiment were cultured in normal conditioned RPMI medium with 10% FBS and 1% penicillin/streptavidin.
Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.
Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.
Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.
S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous system, less potent than its R enantiomer.
Anagrelide is a drug used for the treatment of essential thrombocytosis.
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects.
Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
Doxofylline is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.
Fenspiride is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi.
Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
TAK-063 is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.
Diosgenin is a steroid sapogenin and the precursor for the semisynthesis of progesterone which in turn was used in early combined oral contraceptive pills; A weak PDE inhibitor.
Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.
Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.
Sildenafil is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.
mRNA and protein expression levels of Id‑1 following treatment with 5 μM sildenafil for 24 h. (A) Relative mRNA expression levels of Id‑1 in the HemECs were significantly decreased by 44.2%, according to the 2‑ΔΔCq method (***P=0.0006 vs. control). (B) Western blotting revealed that the protein expression levels of Id‑1 markedly decreased following treatment with sildenafil when compared with the negative control. The TCA 8113 cell line was used as a positive control. HemECs, hemangioma endothelial cells; SIL, sildenafil; ID‑1, inhibitor of differentiation 1.
Luteolin is a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively. Phase 2.
Bioactive compounds inhibit recombinant HDAC activity. Recombinant HDACs were incubated with flavonoid Luteolin (C) for 2 h prior to the addition of cell permeable HDAC substrates. Luteolin inhibited activity of most classes I, IIa, and IIb HDAC isoforms.
PF-8380 is a potent autotaxin inhibitor with IC50 of 2.8nM in an in vitro enzyme assay.
Theobromine is a xanthine alkaloid widely consumed as stimulants and snacks in coffee and cocoa based foods and most often as part of ingredients in drugs.
Linderane, isolated from Lindera strychnifolia vill., is an indirect PDE3 activator and possesses multiple biological effects, including superoxide anion radical-scavenging and antioxidative activity and protective activity against gastritis, gastric ulcers and backache.