PDE

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S2131	Roflumilast (B9302-107)	<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 (IC351)	<1 mg/mL	78 mg/mL	'<1 mg/mL
S2515	Vardenafil HCl Trihydrate	10 mg/mL	100 mg/mL	20 mg/mL
E0346	Ro 20-1724	<1 mg/mL	56 mg/mL	56 mg/mL
S5957	Vardenafil hydrochloride	100 mg/mL	100 mg/mL	''20 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 (ZK-62711)	<1 mg/mL	55 mg/mL	'55 mg/mL
S8034	Apremilast (CC-10004)	<1 mg/mL	92 mg/mL	<1 mg/mL
S1294	Cilostazol (OPC-13013)	<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
S1929	Irsogladine	<1 mg/mL	2 mg/mL	<1 mg/mL
S1504	Dyphylline	51 mg/mL	51 mg/mL	<1 mg/mL
S1895	Dipyridamole (NSC 515776)	<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
S0501	Enpp-1-IN-1	<1 mg/mL	69 mg/mL	<1 mg/mL
S4837	Ibudilast	30 mg/mL	46 mg/mL	46 mg/mL
S5014	Crisaborole (AN2728)	-1 mg/mL	50 mg/mL	-1 mg/mL
S6844	Zatolmilast (BPN14770)	˂1 mg/mL	81 mg/mL	'81 mg/mL
S8895	Ziritaxestat (GLPG1690)	<1 mg/mL	100 mg/mL	'4 mg/mL
S7224	Deltarasin	<1 mg/mL	100 mg/mL	100 mg/mL
S0039	BI-409306	˂1 mg/mL	62 mg/mL	4 mg/mL
S5806	Cilostamide	<1 mg/mL	6 mg/mL	'5 mg/mL
S5539	Olprinone	-1 mg/mL	50 mg/mL	-1 mg/mL
S6186	3-Methylxanthine	<1 mg/mL	8 mg/mL	<1 mg/mL
S8459	TAK-063	<1 mg/mL	85 mg/mL	'<1 mg/mL
S6576	BW-A78U	<1 mg/mL	51 mg/mL	26 mg/mL
S2291	Diosgenin	<1 mg/mL	<1 mg/mL	5 mg/mL
S2312	Icariin	<1 mg/mL	50 mg/mL	<1 mg/mL
S0127	CP-671305	<1 mg/mL	91 mg/mL	20 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
S4345	Pentoxifylline	55 mg/mL	55 mg/mL	55 mg/mL
S5836	IBMX	<1 mg/mL	44 mg/mL	'7 mg/mL
S9436	Pinoresinol dimethyl ether	-1 mg/mL	77 mg/mL	-1 mg/mL
S5837	BRL-50481	<1 mg/mL	49 mg/mL	49 mg/mL
S6433	Udenafil	<1 mg/mL	100 mg/mL	25 mg/mL
S2368	Theobromine	<1 mg/mL	<1 mg/mL	<1 mg/mL
S7858	Dibutyryl-cAMP (Bucladesine)	98 mg/mL	98 mg/mL	''19 mg/mL
S9229	Linderane	-1 mg/mL	52 mg/mL	-1 mg/mL

亜型選択性的な製品

PDE製品

All (50) PDE阻害剤(49) PDE活性剤(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2131	Roflumilast (B9302-107) Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.	EMBO Rep, 2021, e51329 Free Radic Biol Med, 2021, 163:281-296 Mol Cell, 2020, 80(6):1104-1122.e9	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.	Int J Mol Med, 2022, 49(2)19 J Clin Invest, 2021, 131(1)136779 Cardiovasc Res, 2021, 117(5):1391-1401	T24 cells were treated with vehicle, SIL (2 uM), DOX (200 nM) as indicated. Cells were isolated 6 and 12 hours after exposure, and the phosphorylation of γH2AX was determined, with the fold increase in phosphorylation shown.
S1455	Cilomilast Cilomilast (SB-207499) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.	Am J Physiol Renal Physiol, 2020, 318(3):F576-F588 J Pharm Biomed Anal, 2016, 117:47-60 Mol Cancer Res, 2015, 13(1):149-60	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 (IC351) Tadalafil (IC351) 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	J Clin Invest, 2021, 131(1)136779 Biochim Biophys Acta Mol Basis Dis, 2021, 1867(12):166267 Mol Biochem Parasitol, 2021, 244:111392	β-Catenin levels in 293T cells treated with PDE5 inhibitor in the presence or absence of Wnt3a. (a) Tadalafil reduced β-catenin protein levels. Immunofluorescence and confocal images of 293T cells treated with dimethyl sulfoxide (DMSO) or tadalafil at 10 uM in the presence or absence of recombinant Wnt3a for 24 h.
S2515	Vardenafil HCl Trihydrate Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.	Gastroenterology, 2020, 159(3):1068-1084.e2 Bone, 2020, 10.1016/j.bone.2020.115305 Pulm Pharmacol Ther, 2020, 66:101985	(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.
E0346^新	Ro 20-1724 Ro 20-1724 is a potent inhibitor of PDE IV with Ki value of 3.1 μM and a potent gastric secretagogues.
S5957^新	Vardenafil hydrochloride Vardenafil (BAY38-9456, Levitra, Staxyn) hydrochloride is a selective, orally active, potent inhibitor of phosphodiesterase (PDE) with IC50 of 0.7 nM, 11 nM and 180 nM for PDE5, PDE6 and PDE1, respectively.	Cells, 2021, 10(12)3502
S1550	Pimobendan Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.	Sci Rep, 2020, 10(1):19723 Front Microbiol, 2020, 10:2936 Cell Syst, 2019, 8(2):97-108
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.	J Aerosol Med Pulm Drug Deliv, 2019, 32(6):396-404
S2687	Mardepodect (PF-2545920) Mardepodect (PF-2545920) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.	J Neuroimmune Pharmacol, 2020, 10.1007/s11481-020-09943-6 Front Mol Neurosci, 2017, 10:100 Oncotarget, 2017, 8(41):69264-69280
S1430	Rolipram (ZK-62711) The PDE4 selective inhibitor, Rolipram (ZK-62711, SB 95952), inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.	Antioxidants (Basel), 2021, 10(3)460 Sci Rep, 2021, 11(1):19737 Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00768-4	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.
S8034	Apremilast (CC-10004) Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.	Int J Mol Sci, 2021, 22(23)12878 J Immunotoxicol, 2021, 18(1):154-162 Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.04.007
S1294	Cilostazol (OPC-13013) Cilostazol (OPC-13013) is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.	Front Pharmacol, 2021, 12:749930 Front Cell Infect Microbiol, 2021, 11:783085 Int J Biol Sci, 2020, 27;16(11):2001-2013
S2484	Milrinone Milrinone (Win 47203) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.	Biochem Biophys Res Commun, 2018, 503(3):1409-1414 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.	Cell Rep, 2021, 37(1):109774
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.	Viruses, 2019, 11(12)
S1673	Aminophylline Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.	Gastroenterology, 2020, 159(3):1068-1084.e2
S3172	Anagrelide HCl Anagrelide (BL-4162A) is a drug used for the treatment of essential thrombocytosis.	Nat Cancer, 2020, 1(2):235-248
S1929	Irsogladine Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
S1504	Dyphylline Dyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects.	Biogerontology, 2016, 17(5-6):907-920
S1895	Dipyridamole (NSC 515776) Dipyridamole (NSC-515776, Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.	Stem Cells, 2020, 38(8):1020-1033 Stem Cells, 2020, 28 Am J Hum Genet, 2017, 100(1):5-20
S4164	Doxofylline Doxofylline (Doxophylline) 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.
S0501	Enpp-1-IN-1 Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1).
S4837	Ibudilast Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.	Neuron, 2020, 108(5):876-886.e4 CU Scholar, 2019, N/A
S5014	Crisaborole (AN2728) Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.
S6844	Zatolmilast (BPN14770) Zatolmilast (BPN14770) is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.
S8895	Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM.	Front Cell Dev Biol, 2021, 9:656153
S7224	Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with K_d of 38 nM for binding to purified PDEδ.	Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y Cell Death Differ, 2019, 26(11):2400-2415 Nat Commun, 2018, 9(1):672
S0039	BI-409306 BI 409306 (SUB 166499) is a potent and selective inhibitor of human and rat PDE9A with mean IC50 of 65 nM and 168 nM, respectively. Treatment with BI 409306 increases brain cGMP levels, promotes long-term potentiation, and improves episodic and working memory performance in rodents.
S5806	Cilostamide Cilostamide (OPC 3689) is an inhibitor of type III phosphodiesterases with IC50 values of 27 nM and 50 nM for PDE3A and PDE3B, respectively.
S5539	Olprinone Olprinone is a phosphodiesterase III (PDE3) inhibitor with IC50 values of 0.35 mM, 150 mM and 100 mM for human cardiac PDE III, PDE I and PDE II, respectively.
S6186	3-Methylxanthine 3-Methylxanthine (3-MX), a 3-alkylxanthine, is an inhibitor of cyclic guanosine monophosphate (GMP) phosphodiesterase (PDE) with IC50 of 920 μM on guinea-pig isolated trachealis muscle.
S8459	TAK-063 TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.	Int J Mol Sci, 2021, 22(18)9665
S6576	BW-A78U BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
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.	Neurochem Res, 2020, 10.1007/s11064-020-03093-0
S2312	Icariin Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.	Phytomedicine, 2021, 80:153387 Br J Nutr, 2021, 1-11 J Med Virol, 2019, 91(8):1440-1447
S0127	CP-671305 CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM.
S4683	Sildenafil Mesylate Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.	Cardiovasc Res, 2021, 117(5):1391-1401 Sci Rep, 2020, 10(1):18084 Oncotarget, 2016, 7(11):12975-96
S4684	Sildenafil Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.	Cardiovasc Res, 2021, 117(5):1391-1401 J Cell Physiol, 2020, 10.1002/jcp.29580 Bone, 2020, 10.1016/j.bone.2020.115305	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 (Luteoline, Luteolol, Digitoflavone) 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.	Cancer Lett, 2021, 515:36-48 Molecules, 2021, 26(5)1210 Am J Cancer Res, 2021, 11(2):458-478	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 2.8nM in an in vitro enzyme assay.	Leuk Lymphoma, 2021, 1-12
S4345	Pentoxifylline Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity.	Biogerontology, 2016, 17(5-6):907-920
S5836	IBMX IBMX (Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine) 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.	PLoS One, 2019, 14(3):e0214554 Toxicology, 2018, 394:1-10 Cell Death Dis, 2016, 7:e2152
S9436	Pinoresinol dimethyl ether 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.
S5837	BRL-50481 BRL-50481 is a novel and selective inhibitor of phosphodiesterase (PDE) 7 with a Ki value, derived from secondary (Dixon) plots, of 180±10 nM, being at least 200-fold selective for hrPDE7A1 over all other PDEs.	Oncogene, 2017, 36(23):3252-3262
S6433	Udenafil Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.
S2368	Theobromine Theobromine (3,7-Dimethylxanthine) 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.
S7858	Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.	Nat Commun, 2021, 12(1):4050 EMBO Mol Med, 2021, e12632 Cell Rep, 2021, 37(12):110137
S9229	Linderane 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.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2131	Roflumilast (B9302-107) Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.	EMBO Rep, 2021, e51329 Free Radic Biol Med, 2021, 163:281-296 Mol Cell, 2020, 80(6):1104-1122.e9	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.	Int J Mol Med, 2022, 49(2)19 J Clin Invest, 2021, 131(1)136779 Cardiovasc Res, 2021, 117(5):1391-1401	T24 cells were treated with vehicle, SIL (2 uM), DOX (200 nM) as indicated. Cells were isolated 6 and 12 hours after exposure, and the phosphorylation of γH2AX was determined, with the fold increase in phosphorylation shown.
S1455	Cilomilast Cilomilast (SB-207499) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.	Am J Physiol Renal Physiol, 2020, 318(3):F576-F588 J Pharm Biomed Anal, 2016, 117:47-60 Mol Cancer Res, 2015, 13(1):149-60	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 (IC351) Tadalafil (IC351) 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	J Clin Invest, 2021, 131(1)136779 Biochim Biophys Acta Mol Basis Dis, 2021, 1867(12):166267 Mol Biochem Parasitol, 2021, 244:111392	β-Catenin levels in 293T cells treated with PDE5 inhibitor in the presence or absence of Wnt3a. (a) Tadalafil reduced β-catenin protein levels. Immunofluorescence and confocal images of 293T cells treated with dimethyl sulfoxide (DMSO) or tadalafil at 10 uM in the presence or absence of recombinant Wnt3a for 24 h.
S2515	Vardenafil HCl Trihydrate Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.	Gastroenterology, 2020, 159(3):1068-1084.e2 Bone, 2020, 10.1016/j.bone.2020.115305 Pulm Pharmacol Ther, 2020, 66:101985	(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.
E0346^新	Ro 20-1724 Ro 20-1724 is a potent inhibitor of PDE IV with Ki value of 3.1 μM and a potent gastric secretagogues.
S5957^新	Vardenafil hydrochloride Vardenafil (BAY38-9456, Levitra, Staxyn) hydrochloride is a selective, orally active, potent inhibitor of phosphodiesterase (PDE) with IC50 of 0.7 nM, 11 nM and 180 nM for PDE5, PDE6 and PDE1, respectively.	Cells, 2021, 10(12)3502
S1550	Pimobendan Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.	Sci Rep, 2020, 10(1):19723 Front Microbiol, 2020, 10:2936 Cell Syst, 2019, 8(2):97-108
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.	J Aerosol Med Pulm Drug Deliv, 2019, 32(6):396-404
S2687	Mardepodect (PF-2545920) Mardepodect (PF-2545920) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.	J Neuroimmune Pharmacol, 2020, 10.1007/s11481-020-09943-6 Front Mol Neurosci, 2017, 10:100 Oncotarget, 2017, 8(41):69264-69280
S1430	Rolipram (ZK-62711) The PDE4 selective inhibitor, Rolipram (ZK-62711, SB 95952), inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.	Antioxidants (Basel), 2021, 10(3)460 Sci Rep, 2021, 11(1):19737 Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00768-4	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.
S8034	Apremilast (CC-10004) Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.	Int J Mol Sci, 2021, 22(23)12878 J Immunotoxicol, 2021, 18(1):154-162 Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.04.007
S1294	Cilostazol (OPC-13013) Cilostazol (OPC-13013) is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.	Front Pharmacol, 2021, 12:749930 Front Cell Infect Microbiol, 2021, 11:783085 Int J Biol Sci, 2020, 27;16(11):2001-2013
S2484	Milrinone Milrinone (Win 47203) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.	Biochem Biophys Res Commun, 2018, 503(3):1409-1414 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.	Cell Rep, 2021, 37(1):109774
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.	Viruses, 2019, 11(12)
S1673	Aminophylline Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.	Gastroenterology, 2020, 159(3):1068-1084.e2
S3172	Anagrelide HCl Anagrelide (BL-4162A) is a drug used for the treatment of essential thrombocytosis.	Nat Cancer, 2020, 1(2):235-248
S1929	Irsogladine Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
S1504	Dyphylline Dyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects.	Biogerontology, 2016, 17(5-6):907-920
S1895	Dipyridamole (NSC 515776) Dipyridamole (NSC-515776, Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.	Stem Cells, 2020, 38(8):1020-1033 Stem Cells, 2020, 28 Am J Hum Genet, 2017, 100(1):5-20
S4164	Doxofylline Doxofylline (Doxophylline) 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.
S0501	Enpp-1-IN-1 Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1).
S4837	Ibudilast Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.	Neuron, 2020, 108(5):876-886.e4 CU Scholar, 2019, N/A
S5014	Crisaborole (AN2728) Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.
S6844	Zatolmilast (BPN14770) Zatolmilast (BPN14770) is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.
S8895	Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM.	Front Cell Dev Biol, 2021, 9:656153
S7224	Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with K_d of 38 nM for binding to purified PDEδ.	Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y Cell Death Differ, 2019, 26(11):2400-2415 Nat Commun, 2018, 9(1):672
S0039	BI-409306 BI 409306 (SUB 166499) is a potent and selective inhibitor of human and rat PDE9A with mean IC50 of 65 nM and 168 nM, respectively. Treatment with BI 409306 increases brain cGMP levels, promotes long-term potentiation, and improves episodic and working memory performance in rodents.
S5806	Cilostamide Cilostamide (OPC 3689) is an inhibitor of type III phosphodiesterases with IC50 values of 27 nM and 50 nM for PDE3A and PDE3B, respectively.
S5539	Olprinone Olprinone is a phosphodiesterase III (PDE3) inhibitor with IC50 values of 0.35 mM, 150 mM and 100 mM for human cardiac PDE III, PDE I and PDE II, respectively.
S6186	3-Methylxanthine 3-Methylxanthine (3-MX), a 3-alkylxanthine, is an inhibitor of cyclic guanosine monophosphate (GMP) phosphodiesterase (PDE) with IC50 of 920 μM on guinea-pig isolated trachealis muscle.
S8459	TAK-063 TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.	Int J Mol Sci, 2021, 22(18)9665
S6576	BW-A78U BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
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.	Neurochem Res, 2020, 10.1007/s11064-020-03093-0
S2312	Icariin Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.	Phytomedicine, 2021, 80:153387 Br J Nutr, 2021, 1-11 J Med Virol, 2019, 91(8):1440-1447
S0127	CP-671305 CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM.
S4683	Sildenafil Mesylate Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.	Cardiovasc Res, 2021, 117(5):1391-1401 Sci Rep, 2020, 10(1):18084 Oncotarget, 2016, 7(11):12975-96
S4684	Sildenafil Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.	Cardiovasc Res, 2021, 117(5):1391-1401 J Cell Physiol, 2020, 10.1002/jcp.29580 Bone, 2020, 10.1016/j.bone.2020.115305	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 (Luteoline, Luteolol, Digitoflavone) 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.	Cancer Lett, 2021, 515:36-48 Molecules, 2021, 26(5)1210 Am J Cancer Res, 2021, 11(2):458-478	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 2.8nM in an in vitro enzyme assay.	Leuk Lymphoma, 2021, 1-12
S4345	Pentoxifylline Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity.	Biogerontology, 2016, 17(5-6):907-920
S5836	IBMX IBMX (Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine) 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.	PLoS One, 2019, 14(3):e0214554 Toxicology, 2018, 394:1-10 Cell Death Dis, 2016, 7:e2152
S9436	Pinoresinol dimethyl ether 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.
S5837	BRL-50481 BRL-50481 is a novel and selective inhibitor of phosphodiesterase (PDE) 7 with a Ki value, derived from secondary (Dixon) plots, of 180±10 nM, being at least 200-fold selective for hrPDE7A1 over all other PDEs.	Oncogene, 2017, 36(23):3252-3262
S6433	Udenafil Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.
S2368	Theobromine Theobromine (3,7-Dimethylxanthine) 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.
S7858	Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.	Nat Commun, 2021, 12(1):4050 EMBO Mol Med, 2021, e12632 Cell Rep, 2021, 37(12):110137

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S9229	Linderane 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.

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S9229

Linderane

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.

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PDE

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