PDE

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S2131	Roflumilast	<1 mg/mL	81 mg/mL	15 mg/mL
S1431	Sildenafil Citrate	<1 mg/mL	20 mg/mL	<1 mg/mL
S1455	Cilomilast	<1 mg/mL	69 mg/mL	50 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
S5014	Crisaborole (AN2728)	-1 mg/mL	50 mg/mL	-1 mg/mL
S4837	Ibudilast	30 mg/mL	46 mg/mL	46 mg/mL
S1550	Pimobendan	<1 mg/mL	67 mg/mL	5 mg/mL
S2620	GSK256066	<1 mg/mL	5 mg/mL	<1 mg/mL
S2687	Mardepodect (PF-2545920)	<1 mg/mL	78 mg/mL	78 mg/mL
S1430	Rolipram	<1 mg/mL	55 mg/mL	55 mg/mL
S1294	Cilostazol	<1 mg/mL	74 mg/mL	6 mg/mL
S2484	Milrinone	<1 mg/mL	42 mg/mL	<1 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
S1673	Aminophylline	84 mg/mL	53 mg/mL	<1 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

Isoform-specific Inhibitors

PDE Inhibitors (30)
New PDE Products

Catalog No.	Information	Product Use Citations	Product Validations
S2131	Roflumilast Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.	Cell Rep, 2014, 8(5):1265-70 Mol Cancer Ther, 2014, 13(10):2463-73 Int Immunopharmacol, 2016, 35:174-84	Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6).
S1431	Sildenafil Citrate 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.	Cancer Lett, 2016, 370(2):279-85 Mol Pharmacol, 2014, 85(3):408-19 Mol Pharmacol, 2014, 85(3):408-19	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.
S1455	Cilomilast Cilomilast is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.	Mol Cancer Res, 2015, 13(1):149-60 AM J Resp Cell Mol, 2014, 10.1165/rcmb.2014-0344OC Biochimie, 2012, 94(11):2360-5	LNCaP-C4 prostate cancer cells were suspended in matrigel and transplanted under the kidney capsule of male nude mice hosts. Mice were treated with vehicle-only (10% EtOH, 90% olive oil) control, cilomilast or NVP-ABE171 by gavage (n=7-11 for each respective group)The xenografts LNCaP-C4 xenografts were excised, fixed in formalin, and embedded in paraffin blocks. IHC with Ki67 (proliferation), TUNEL (apoptosis), or p21 (senescence) was performed. Representative Ki67 and TUNEL photomicrographs for cilomilast and NVP-ABE171 treatment group are shown.
S1512	Tadalafil 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	Cancer Lett, 2016, 370(2):279-85 Cell Death Dis, 2014, 5:e1544 Mol Pharmacol, 2014, 85(3):408-19	(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.
S2515	Vardenafil HCl Trihydrate Vardenafil HCl Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.	Cancer Lett, 2016, 378(1):38-50 Cell Death Dis, 2014, 5:e1544 J Cell Physiol, 2014, 10.1002/jcp.24919	(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.
S5014^New	Crisaborole (AN2728) Crisaborole is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.
S4837^New	Ibudilast Ibudilast is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.
S1550	Pimobendan Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
S2620	GSK256066 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.
S2687	Mardepodect (PF-2545920) PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.	Oncogene, 2014, 10.1038/onc.2014.94 Front Mol Neurosci, 2017, 10:100 Biol Reprod, 2016, 94(5):110
S1430	Rolipram 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.	Mol Cancer Ther, 2014, 13(10):2463-73 Mol Cancer Ther, 2014, 13(10):2463-73 Mol Nutr Food Res, 2017, 10.1002/mnfr.201600966	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.
S1294	Cilostazol Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.
S2484	Milrinone Milrinone is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.	Mol Pharm, 2017, 10.1021/acs.molpharmaceut.7b00360	Viability of H9c2 cells incubated with MRN-HSA-NPs (black bars) compared with MRN-Lactate (grey bars) at different MRN concentrations, at (a) 4 hours, (b) 24 hours and (c) 48 hours. The graph shows a representative result of mean±SD (n=3). **P<0.0001, P<0.001, P<0.01 and P<0.05 were considered significant based on Sidak’s posthoc analysis.
S4019	Avanafil Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.
S2127	S- (+)-Rolipram 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.
S1673	Aminophylline Aminophylline is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.
S3172	Anagrelide HCl Anagrelide is a drug used for the treatment of essential thrombocytosis.
S1504	Dyphylline Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects.
S1895	Dipyridamole Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
S4164	Doxofylline Doxofylline is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.
S4090	Fenspiride HCl 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.
S7224	Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with K_d of 38 nM for binding to purified PDEδ.
S8459	TAK-063 TAK-063 is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.
S2291	Diosgenin 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.
S2312	Icariin Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.	Shandong University, 2014, Haoran Cui
S4683	Sildenafil Mesylate Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.
S4684	Sildenafil Sildenafil is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.	Exp Ther Med, 2017, 13(6):2645-2650	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.
S2320	Luteolin 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.	Mol Nutr Food Res, 2017, 10.1002/mnfr.201600744	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.
S8218	PF-8380 PF-8380 is a potent autotaxin inhibitor with IC50 of 2.8 nM in an in vitro enzyme assay.
S2368	Theobromine 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.

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By Signaling Pathways

By product type

PDE

Signaling Pathway Map

Research Area

Isoform-specific Inhibitors

Roflumilast

Sildenafil Citrate

Cilomilast

Tadalafil

Vardenafil HCl Trihydrate

Crisaborole (AN2728)

Ibudilast

Pimobendan

GSK256066

Mardepodect (PF-2545920)

Rolipram

Cilostazol

Milrinone

Avanafil

S- (+)-Rolipram

Aminophylline

Anagrelide HCl

Dyphylline

Dipyridamole

Doxofylline

Fenspiride HCl

Deltarasin

TAK-063

Diosgenin

Icariin

Sildenafil Mesylate

Sildenafil

Luteolin

PF-8380

Theobromine