ASB16165
ASB16165 is a selective and potent PDE7A inhibitor with an IC50 of 15 nM against human PDE7A. ASB16165 inhibits IL-12-induced IFN-γ production via a cAMP/PKA-dependent mechanism, reduces cutaneous TNF-α production, and suppresses keratinocyte proliferation. ASB16165 can be used in research on skin diseases such as psoriasis.
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- No. CAS: 873541-45-8
- Fòrmula: C23H29N5O2S
- Peso molecular:439.58
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Actividad biológica
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PDE7A 15 nM (IC50) |
PKA |
TNF-α |
ASB16165 potently inhibits recombinant human PDE7A with an IC50 of 15 nM, and exhibits much weaker inhibitory activity on PDE4 with an IC50 of 2.1 μM, PDE1A3, PDE2A3, PDE3, PDE5, PDE8A1, PDE9A2 and PDE10A1 with an IC50 of > 10 μM[1].
ASB16165 (0.1-3 μM; 24 h IL-12 stimulation; 48h) inhibits the IL-12-induced IFN-γ secretion by the activated T cells in a concentration-dependent manner, with significant effects at 1 μM and higher [1].
ASB16165 (0.1-3 μM; 1 μg/mL CD28; 72 h) suppresses CD3/CD28 co-stimulation-triggered proliferation, IL-2 and IFN-γ secretion in primary mouse resting T cells in a concentration-dependent manner[1].
ASB16165 (3 μM; 100 ng/mL IL-12 24 h; 30 min) suppresses IL-12-induced IFN-γ production in mouse T lymphoblasts, and PKA inhibitor Rp-8-Br-cAMP reverses this inhibitory effect in a concentration-dependent manner[1].
ASB16165 (1-10 μM; 30 min) inhibits the Phorbol 12-myristate 13-acetate (TPA, HY-18739)/Calcimycin (A23187, HY-N6687)-induced TNF-α production, with a significant effect at 3 μM and higher [2].
ASB16165 (0.3-3 μM; 48 h) concentration-dependently inhibits the proliferation of human keratinocytes with an IC50 of approximately 1.8 μM [3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse splenic T lymphoblasts
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Concentration:0.1, 0.3, 1, 3 μM; Rp-8-Br-cAMP (HY-137640B) 0, 0.01, 0.1, 1 mM
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Incubation Time:Compound pretreatment 30 min, IL-12 (100 ng/mL) stimulation 24 h
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Result:Significantly reduced IL-12-triggered IFN-γ secretion.
PKA inhibitor Rp-8-Br-cAMP reversed the suppressive effect dose-dependently, with significant reversal at 0.1 mM and highly significant reversal at 1 mM. Rp-8-Br-cAMP alone barely affects basal IFN-γ level.
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Cell Line:Primary mouse resting splenic T cells
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Concentration:0.1, 0.3, 1, 3 μM
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Incubation Time:Compound added before co-stimulation, CD3/CD28 (1 μg/mL CD28) incubation 72 h
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Result:Concentration-dependently suppressed CD3/CD28-induced T cell proliferation, IL-2 secretion and IFN-γ production at 1 μM and above.
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Cell Line:Human epidermal keratinocytes
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Concentration:1, 3, 10 μM
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Incubation Time:Compound pretreatment 30 min, TPA (HY-18739) (100 ng/mL) + A23187 (1 μg/mL) stimulation 8 h
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Result:Markedly inhibits TPA/calcium ionophore induced TNF-α release at 3 μM.
PDE4 inhibitor Rolipram (HY-16900) had no obvious inhibitory activity under identical treatment conditions.
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Cell Line:Human epidermal keratinocytes
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Concentration:0.3, 1, 3 μM
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Incubation Time:Compound incubation 48 h
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Result:Robustly suppressed keratinocyte proliferation, with the antiproliferative IC50 measured at approximately 1.8 μM.
db-cAMP replicated the antiproliferative phenotype, while Rolipram and Betamethasone dipropionate (HY-13571) exert no anti-proliferative effect in vitro.
ASB16165 (0.03%-1%; topical application; once daily; 10 days) alleviates chronic ear thickening and epidermal hyperplasia induced by multiple TPA painting, sharply decreases epidermal Ki67-positive proliferative keratinocytes to 29% of vehicle group, and causes no body weight loss unlike Betamethasone dipropionate (HY-13571)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:TPA-induced acute skin edema model in female BALB/c mice[2]
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Dosage:0.03%, 0.1%, 0.3%, 1%; 0.1% betamethasone dipropionate
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Administration:Topical application; 20 μL TPA (50 μg/mL) mixed with compounds
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Result:Dose-dependently alleviated ear swelling, significant anti-edema was observed activity at ≥0.1% concentration.
Time-course detection (0-6 h): 1% continuously lowered skin TNF-α level up to 6 h post administration, and showed equivalent efficacy to 0.1% betamethasone dipropionate.
Tissue TNF-α content was markedly decreased at concentrations above 0.1%.
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Animal Model:Repeated TPA-induced chronic epidermal hyperplasia model in female BALB/c mice[3]
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Dosage:0.03%, 0.1%, 0.3%, 1%; 0.1% betamethasone dipropionate
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Administration:Topical application; once daily; TPA applied on day 0, 2, 4, 7, 9
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Result:Significantly relieved total ear thickness and epidermal thickening at 0.3% and 1% concentration.
Epidermal Ki67-positive proliferative keratinocytes were reduced to only 29% of vehicle control group.
No obvious body weight loss was observed in mice, while betamethasone dipropionate induced notable weight reduction.
Chemical Information
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No. CAS 873541-45-8
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Peso molecular 439.58
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Fòrmula C23H29N5O2S
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SMILES
O=C(NC1=CN=C(C=C1)N2CCC(O)CC2)C=3SC4=C(C3)C(=NN4C5CCCCC5)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Kadoshima-Yamaoka K et al. ASB16165, a novel inhibitor for phosphodiesterase 7A (PDE7A), suppresses IL-12-induced IFN-gamma production by mouse activated T lymphocytes. Immunol Lett. 2009 Feb 21;122(2):193-7. [Content Brief]
[2]. Kadoshima-Yamaoka K et al. ASB16165, a phosphodiesterase 7A inhibitor, reduces cutaneous TNF-alpha level and ameliorates skin edema in phorbol ester 12-O-tetradecanoylphorbol-13-acetate-induced skin inflammation model in mice. Eur J Pharmacol. 2009 Jun 24;613(1-3):163-6. [Content Brief]
[3]. Goto M et al. Phosphodiesterase 7A inhibitor ASB16165 impairs proliferation of keratinocytes in vitro and in vivo. Eur J Pharmacol. 2010 May 10;633(1-3):93-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ASB16165 Related Classifications
HY-165553 Related Classifications
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- ASB16165
- 873541-45-8
- ASB 16165
- ASB-16165
- Phosphodiesterase (PDE)
- PKA
- TNF Receptor
- PDE7A inhibitor
- phosphodiesterase 7A inhibitor
- cAMP/PKA signaling pathway
- IL-12
- IFN-γ
- activated T lymphocytes
- T lymphoblasts
- anti-CD3 antibody
- Rp-8-Br-cAMPS
- forskolin
- dibutyryl cAMP
- TNF-α
- human keratinocytes
- TPA
- calcium ionophore
- skin inflammation
- TPA-induced skin inflammation model
- skin edema
- cutaneous TNF-α
- keratinocyte proliferation
- Ki67-positive keratinocytes
- epidermal thickening
- psoriasis
- immunological disorders
- Inhibitor
- inhibitor
- inhibit