2. Metabolic Enzyme/Protease TGF-beta/Smad Stem Cell/Wnt Apoptosis
  3. Phosphodiesterase (PDE) PKA TNF Receptor
  4. 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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ASB16165

ASB16165 Chemical Structure

CAS No. : 873541-45-8

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ASB16165 Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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PKA PKAR PKACα

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Description

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[1][2][3].

IC50 & Target[1]

PDE7A

15 nM (IC50)

PKA

 

TNF-α

 

In Vitro

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 TPA (HY-18739)/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.

ASB16165 Related Antibodies

ELISA Assay[1]

Cell Line: Mouse splenic T lymphoblasts
Concentration: 0.1, 0.3, 1, 3 μM; Rp-8-Br-cAMP (HY-137640B) 0, 0.01, 0.1, 1 mM
Incubation Time: Compound pretreatment 30 min, IL-12 (100 ng/mL) stimulation 24 h
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.

Cell Proliferation Assay[1]

Cell Line: Primary mouse resting splenic T cells
Concentration: 0.1, 0.3, 1, 3 μM
Incubation Time: Compound added before co-stimulation, CD3/CD28 (1 μg/mL CD28) incubation 72 h
Result: Concentration-dependently suppressed CD3/CD28-induced T cell proliferation, IL-2 secretion and IFN-γ production at 1 μM and above.

ELISA Assay[2]

Cell Line: Human epidermal keratinocytes
Concentration: 1, 3, 10 μM
Incubation Time: Compound pretreatment 30 min, TPA (HY-18739) (100 ng/mL) + A23187 (1 μg/mL) stimulation 8 h
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.

Cell Proliferation Assay[3]

Cell Line: Human epidermal keratinocytes
Concentration: 0.3, 1, 3 μM
Incubation Time: Compound incubation 48 h
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.
In Vivo

ASB16165 (0.03%-1%; topical application; single dose) reducs skin edema in BALB/c mice, significantly reduces cutaneous TNF-α level at concentrations higher than 0.1%. Until 6 h after administration, 1% the inhibitory efficacy is similar to that of 0.1% Betamethasone dipropionate (HY-13571)[2].
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.

Animal Model: TPA-induced acute skin edema model in female BALB/c mice[2]
Dosage: 0.03%, 0.1%, 0.3%, 1%; 0.1% betamethasone dipropionate
Administration: Topical application; 20 μL TPA (50 μg/mL) mixed with compounds
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%.
Animal Model: Repeated TPA-induced chronic epidermal hyperplasia model in female BALB/c mice[3]
Dosage: 0.03%, 0.1%, 0.3%, 1%; 0.1% betamethasone dipropionate
Administration: Topical application; once daily; TPA applied on day 0, 2, 4, 7, 9
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.
Molecular Weight

439.58

Formula

C23H29N5O2S
CAS No.
SMILES

O=C(NC1=CN=C(C=C1)N2CCC(O)CC2)C=3SC4=C(C3)C(=NN4C5CCCCC5)C
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ASB16165 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ASB16165873541-45-8ASB 16165ASB-16165Phosphodiesterase (PDE)PKATNF ReceptorProtein kinase ATumor Necrosis Factor ReceptorTNFRPDE7A inhibitorphosphodiesterase 7A inhibitorcAMP/PKA signaling pathwayIL-12IFN-γactivated T lymphocytesT lymphoblastsanti-CD3 antibodyRp-8-Br-cAMPSforskolindibutyryl cAMPTNF-αhuman keratinocytesTPAcalcium ionophoreskin inflammationTPA-induced skin inflammation modelskin edemacutaneous TNF-αkeratinocyte proliferationKi67-positive keratinocytesepidermal thickeningpsoriasisimmunological disordersInhibitorinhibitorinhibit

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