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Ayanin is a bioflavonoid isolated from Psychotria serpens. Ayanin is a non-selective phosphodiesterase1-4 inhibitor and can be used for the study of respiratory disease,such as allergic asthma et al [1].
PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC50 values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research [1].
PDE1-IN-6 (compound 6c) is a selectivity PDE1 inhibitor with the IC50 of 7.5 nM. PDE1-IN-6 significantly inhibits the proliferation and induced cell apoptosis in Acute myelogenous leukemia cells [1].
(+)-Medioresinol Di-O-β-D-glucopyranoside is a lignan glucoside with strong inhibitory activity of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterase .
Sequosempervirin B, a norlignan isolated from the branches and leaves of Sequoia sempervirens, has antifungal properties. Sequosempervirin B has an inhibitory effect on cyclic AMP phosphodiesterase .
MDL12330A (RMI12330A) is an adenyl cyclase inhibitor. MDL12330A inhibits the vasopressin action on the short-circuit current (SCC). MDL12330A is also an inhibitor of cAMP phosphodiesterase .
Enpp-1-IN-12 (compound 43) is a potent and orally active ecto-nucleotide pyrophosphatase/phosphodiesterases 1(ENPP1) inhibitor, with a Ki of 41 nM. Enpp-1-IN-12 exhibits anti-tumor activity [1].
5,7-Diacetoxy-8-methoxyflavone is a natural product that could come from scutellaria genus plants. 5,7-Diacetoxy-8-methoxyflavone has inhibitory activity for cAMP phosphodiesterase .
Enpp-1-IN-10 (compound 1) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1(ENPP1) inhibitor with an Ki value of 3.866 μM. Enpp-1-IN-10 can be used for researching anticancer [1].
NPP1-IN-2 (compound 3h) is a potent and selective Ectonucleotide pyrophosphatase/phosphodiesterase-1(NPP1) inhibitor with IC50 values of 0.55, 3.73 µM for NPP1, NPP3, respectively [1].
Enpp-1-IN-4 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1(enpp-1).Enpp-1-IN-4 has the potential for the research of cancer diseases (extracted from patent WO2019177971A1, compound 1) [1].
Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases .
Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases .
Enpp-1-IN-14 (Compound 015) is a potent Ectonucleotide Pyrophosphatase/Phosphodiesterase-1(ENPP1) inhibitor with an IC50 value of 32.38 nM for recombinant human ENPP-1. Enpp-1-IN-14 has anti-tumor activity [1].
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases .
PDE1-IN-3, compound 4 (WO2019156861), is a selective human phosphodiesterase 1(PDE1) inhibitor. PDE1-IN-3 inhibits PDE4D and PDE6AB with IC50 values of 23.99 μM and 10 μM, respectively [1].
TDP1 Inhibitor-2 (compound 5) is a potent inhibitor for TDP1 (tyrosyl-DNA phosphodiesterase 1), with an IC50 of 99 nM. TDP1 Inhibitor-2 also can inhibit SCAN1 (spinocerebellar ataxia syndrome with axonal neuropathy), with an IC50 of 3.5 μM [1].
Enpp-1-IN-2 (Compound C) is a potent ENPP1 (ectonucleotide pyrophosphatase/phosphodiesterase 1) inhibitor with IC50 values of 0.26, 0.48 and 2.0 μM evaluated by means of TG-mAMP, pNP-TMP, and ATP assays, respectively. TG (Tokyo Green)-mAMP: a newly synthesized sensitive ENPP1 fluorescence probe [1].
Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1(ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer [1].
DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1(PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia [1] .
Enpp-1-IN-6 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1(enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-6 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51) [1].
Enpp-1-IN-7 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1(enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-7 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51) [1].
Enpp-1-IN-8 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1(enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-8 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51) [1].
Enpp-1-IN-9 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1(enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-9 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51) [1].
Enpp-1-IN-20 (Compound 31) is an ectonucleotide pyrophosphatase/phosphodiesterase 1(ENPP1) inhibitor, with an IC50 of 0.09 nM. Enpp-1-IN-20 has strongest inhibitory activity in the cell-based assay, with an IC50 of 8.8 nM. Enpp-1-IN-20 has significant potency in both ENPP1 inhibition and STING pathway stimulation in vitro. Enpp-1-IN-20 can be used for the research of cancer [1].
Enpp-1-IN-5 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1(enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-5 has the potential for the research of cancer and infectious diseases (extracted from patent WO2019046778A1/WO2021203772A1, compound 1) [1] .
Furamidine (DB75) is a selective protein arginine methyltransferase 1(PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1(TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent [1] .
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1(PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1(TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent [1] .
Ayanin is a bioflavonoid isolated from Psychotria serpens. Ayanin is a non-selective phosphodiesterase1-4 inhibitor and can be used for the study of respiratory disease,such as allergic asthma et al [1].
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
(+)-Medioresinol Di-O-β-D-glucopyranoside is a lignan glucoside with strong inhibitory activity of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterase .
Sequosempervirin B, a norlignan isolated from the branches and leaves of Sequoia sempervirens, has antifungal properties. Sequosempervirin B has an inhibitory effect on cyclic AMP phosphodiesterase .
5,7-Diacetoxy-8-methoxyflavone is a natural product that could come from scutellaria genus plants. 5,7-Diacetoxy-8-methoxyflavone has inhibitory activity for cAMP phosphodiesterase .
PDE1B protein, a cyclic nucleotide phosphodiesterase, displays dual specificity for cAMP and cGMP, essential second messengers in physiological processes. Preferring cGMP as a substrate, PDE1B fine-tunes cellular responses to cyclic nucleotide signaling. Its dual specificity underscores its regulatory role in diverse physiological pathways. PDE1B Protein, Human (sf9, His-GST) is the recombinant human-derived PDE1B protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of PDE1B Protein, Human (sf9, His-GST) is 536 a.a., with molecular weight of ~75 kDa.
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