About 24 results found for searched term "PDE1-IN-5" (0.119 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M42565 | PDE1-IN-5 | PDE |
| PDE1-IN-5 is a selective PDE1C inhibitor (IC50: 15 nM). | ||
| M3447 | PF-2545920 | PDE |
| Mardepodect; CAS# 898562-94-2 | ||
| PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. | ||
| M4851 | TAK-063 | PDE |
| Balipodect | ||
| TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM. | ||
| M7630 | Butein | PDE |
| 2’,3,4,4’-tetrahydroxy Chalcone | ||
| Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator. | ||
| M9347 | ITI-214 phosphate | PDE |
| ITI214 | ||
| ITI-214 phosphate is an orally active, potent and selective inhibitors of PDE1, exhibits potent PDE1 inhibitory activity (Ki = 58 pM). ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. | ||
| M11473 | BAY 2666605 | Others |
| BAY 2666605 is an oral active PDE3A and PDE3B inhibitor with IC50 of 87 nM and 50 nM, respectively. BAY 2666605 is a pDE3A-SLFN12 compound inducer (WO2019025562A1; Example, 135). | ||
| M20402 | Mardepodect (PF-2545920) | PDE |
| PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. | ||
| M21090 | ITI-214 free base | Others |
| ITI-214 free base is a potent inhibitor of CNS activity and an orally bioactive PDE1 inhibitor (Ki of 58 pM) with good selectivity for other PDE family members and a range of enzymes, receptors, transporters and ion channels. | ||
| M21158 | Vepdegestrant (ARV-471) | PROTAC |
| ARV471; PF-07850327 | ||
| Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer.ARV-471 is a heterobifunctional molecule that promotes the interaction between estrogen receptor alpha and intracellular E3 ligase complexes.ARV-471 causes ubiquitination and subsequent degradation of the estrogen receptor via the proteasome.ARV-471 potently degrades ER-positive The ER in breast cancer cell lines is potently degraded by ARV-471 with a DC50 value of approximately 2 nM. | ||
| M21173 | Tanimilast | Others |
| CHF-6001 | ||
| The M3 antagonist/PDE4 inhibitor dual pharmacology molecule 92a compound is an inhaled compound for lung disease.Tanimilast (CHF-6001) is a novel, potent, selective phosphodiesterase 4 inhibitor (IC50=0.026±0.006 nM) with potent anti-inflammatory activity suitable for topical lung administration. | ||
| M21314 | LEO 39652 | PDE |
| LEO 39652 is a dual-soft PDE4 inhibitor with IC50 values of 1.2 nM for PDE4A, 1.2 nM for PDE4B, 3.0 nM for PDE4C, and 3.8 nM for PDE4D. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used in topical studies of atopic dermatitis. | ||
| M27856 | Lanopepden | Antibiotic |
| GSK 1322322 | ||
| Lanopepden (GSK 1322322) is a peptide deformylase inhibitor active against Staphylococcus aureus strains with MICs of 1 and 1 mg/L for ATCC 29213 and ATCC 25923 strain, respectively. | ||
| M27861 | Siguazodan | PDE |
| SKF 94836 | ||
| Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM. | ||
| M28193 | JNJ-42314415 | PDE |
| JNJ-42314415 is a centrally active phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 35 nM and 64 nM for human recombinant PDE10A and rPDE10A, respectively. | ||
| M28396 | Sp-cAMPS sodium salt | PKA |
| Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM. | ||
| M29161 | Mardepodect hydrochloride | PDE |
| PF-2545920 hydrochloride | ||
| Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier. | ||
| M29620 | PF-07038124 | PDE |
| PF-07038124 is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1 1.06 nM, respectively). | ||
| M30131 | NPD-001 | PDE |
| NPD-001 is a potent Trypanosoma brucei phosphodiesterases TbrPDEB1 and TbrPDEB2 inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits human PDEs (phosphodiesterases). NPD-001 shows good anti trypanosomal activity, with an IC50 of 80 nM. | ||
| M30532 | Sp-cAMPS | PKA |
| Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM. | ||
| M30839 | Mardepodect | PDE |
| PF-2545920 | ||
| Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier. | ||
| M42563 | PDE5-IN-10 | PDE |
| PDE5-IN-10 is a potent PDE5 inhibitor with an IC50 of 20 nM. | ||
| M42566 | PDE4-IN-13 | PDE |
| PDE4-IN-13 is a PDE4 inhibitor with an IC50 of 1.56 μM. | ||
| M56759 | PDE12-IN-1 | PDE |
| PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. | ||
| M58458 | MR-L2 | PDE |
| MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM. | ||
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