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) | ||
|---|---|---|---|---|
| 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 |
| E0423 | (R)-Avanafil | <1 mg/mL | 48 mg/mL | 2 mg/mL |
| E0346 | Ro 20-1724 | <1 mg/mL | 56 mg/mL | 56 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 |
| S5957 | Vardenafil hydrochloride | 100 mg/mL | 100 mg/mL | ''20 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 |
| E0483 | Calmidazolium chloride | <1 mg/mL | 100 mg/mL | 50 mg/mL |
亜型選択性的な製品
PDE製品
| 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. |
Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6). |
|
| S1431 |
Sildenafil CitrateSildenafil 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. |
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 |
CilomilastCilomilast (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. |
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 |
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 TrihydrateVardenafil HCl Trihydrate (BAY38-9456) 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.
|
|
| E0423新 |
(R)-AvanafilR-Avanafil is a strong competitive inhibitor of phosphodiesterase 5 (PDE5) with a demonstrated in vitro IC 50 of 5.2 nM. |
||
| E0346新 |
Ro 20-1724Ro 20-1724 is a potent inhibitor of PDE IV with Ki value of 3.1 μM and a potent gastric secretagogues. |
||
| S1550 |
PimobendanPimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM. |
||
| S2620 |
GSK256066GSK256066 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)Mardepodect (PF-2545920) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. |
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|
| 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. |
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.
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|
| 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. |
||
| 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. |
||
| S2484 |
MilrinoneMilrinone (Win 47203) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility. |
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 |
AvanafilAvanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs. |
||
| S2127 |
S-(+)-RolipramS-(+)-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 |
AminophyllineAminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist. |
||
| S3172 |
Anagrelide HClAnagrelide (BL-4162A) is a drug used for the treatment of essential thrombocytosis. |
||
| S1929 |
IrsogladineIrsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. |
||
| S1504 |
DyphyllineDyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects. |
||
| 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. |
||
| S4164 |
DoxofyllineDoxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma. |
||
| S4090 |
Fenspiride HClFenspiride 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. |
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| S0501 |
Enpp-1-IN-1Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). |
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| S4837 |
IbudilastIbudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities. |
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| 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. |
||
| S7224 |
DeltarasinDeltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
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| S0039 |
BI-409306BI 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. |
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| S5806 |
CilostamideCilostamide (OPC 3689) is an inhibitor of type III phosphodiesterases with IC50 values of 27 nM and 50 nM for PDE3A and PDE3B, respectively. |
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| S5539 |
OlprinoneOlprinone 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. |
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| S6186 |
3-Methylxanthine3-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. |
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| S8459 |
TAK-063TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM. |
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| S5957 |
Vardenafil hydrochlorideVardenafil (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. |
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| S6576 |
BW-A78UBW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity. |
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| S2291 |
DiosgeninDiosgenin 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. |
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| S2312 |
IcariinIcariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4. |
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| S0127 |
CP-671305CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM. |
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| S4683 |
Sildenafil MesylateSildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5. |
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| S4684 |
SildenafilSildenafil (Revatio, UK-92480, Viagra) 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.
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| S2320 |
LuteolinLuteolin (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. |
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-8380PF-8380 is a potent autotaxin inhibitor with IC50 of 2.8nM in an in vitro enzyme assay. |
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| S4345 |
PentoxifyllinePentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity. |
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| S5836 |
IBMXIBMX (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. |
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| S9436 |
Pinoresinol dimethyl etherPinoresinol 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. |
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| S5837 |
BRL-50481BRL-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. |
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| S6433 |
UdenafilUdenafil 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. |
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| S2368 |
TheobromineTheobromine (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. |
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| 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. |
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| S9229 |
LinderaneLinderane, 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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| E0483新 |
Calmidazolium chlorideCalmidazolium chloride (R 24571) is a calmodulin (CaM) antagonist, antagonizing CaM-stimulated fraction of rat brain phosphodiesterase and CaM-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively, also shows a CaM-binding Kd value of 3 nM. |
| 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. |
Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6). |
|
| S1431 |
Sildenafil CitrateSildenafil 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. |
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 |
CilomilastCilomilast (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. |
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 |
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 TrihydrateVardenafil HCl Trihydrate (BAY38-9456) 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.
|
|
| E0423新 |
(R)-AvanafilR-Avanafil is a strong competitive inhibitor of phosphodiesterase 5 (PDE5) with a demonstrated in vitro IC 50 of 5.2 nM. |
||
| E0346新 |
Ro 20-1724Ro 20-1724 is a potent inhibitor of PDE IV with Ki value of 3.1 μM and a potent gastric secretagogues. |
||
| S1550 |
PimobendanPimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM. |
||
| S2620 |
GSK256066GSK256066 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)Mardepodect (PF-2545920) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. |
|
|
| 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. |
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. |
||
| 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. |
||
| S2484 |
MilrinoneMilrinone (Win 47203) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility. |
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 |
AvanafilAvanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs. |
||
| S2127 |
S-(+)-RolipramS-(+)-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 |
AminophyllineAminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist. |
||
| S3172 |
Anagrelide HClAnagrelide (BL-4162A) is a drug used for the treatment of essential thrombocytosis. |
||
| S1929 |
IrsogladineIrsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. |
||
| S1504 |
DyphyllineDyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects. |
||
| 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. |
||
| S4164 |
DoxofyllineDoxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma. |
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| S4090 |
Fenspiride HClFenspiride 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. |
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| S0501 |
Enpp-1-IN-1Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). |
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| S4837 |
IbudilastIbudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities. |
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| S5014 |
Crisaborole (AN2728)Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity. |
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| 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. |
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| S8895 |
Ziritaxestat (GLPG1690)Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM. |
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| S7224 |
DeltarasinDeltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
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| S0039 |
BI-409306BI 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. |
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| S5806 |
CilostamideCilostamide (OPC 3689) is an inhibitor of type III phosphodiesterases with IC50 values of 27 nM and 50 nM for PDE3A and PDE3B, respectively. |
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| S5539 |
OlprinoneOlprinone 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. |
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| S6186 |
3-Methylxanthine3-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. |
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| S8459 |
TAK-063TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM. |
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| S5957 |
Vardenafil hydrochlorideVardenafil (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. |
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| S6576 |
BW-A78UBW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity. |
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| S2291 |
DiosgeninDiosgenin 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. |
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| S2312 |
IcariinIcariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4. |
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| S0127 |
CP-671305CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM. |
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| S4683 |
Sildenafil MesylateSildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5. |
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| S4684 |
SildenafilSildenafil (Revatio, UK-92480, Viagra) 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.
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| S2320 |
LuteolinLuteolin (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. |
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. |
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| S8218 |
PF-8380PF-8380 is a potent autotaxin inhibitor with IC50 of 2.8nM in an in vitro enzyme assay. |
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| S4345 |
PentoxifyllinePentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity. |
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| S5836 |
IBMXIBMX (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. |
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| S9436 |
Pinoresinol dimethyl etherPinoresinol 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. |
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| S5837 |
BRL-50481BRL-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. |
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| S6433 |
UdenafilUdenafil 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. |
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| S2368 |
TheobromineTheobromine (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. |
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| 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. |
| 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 |
|---|---|---|---|
| S9229 |
LinderaneLinderane, 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 |
|---|---|---|---|
| E0483新 |
Calmidazolium chlorideCalmidazolium chloride (R 24571) is a calmodulin (CaM) antagonist, antagonizing CaM-stimulated fraction of rat brain phosphodiesterase and CaM-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively, also shows a CaM-binding Kd value of 3 nM. |
