2. Metabolic Enzyme/Protease Immunology/Inflammation GPCR/G Protein Apoptosis
  3. Phosphodiesterase (PDE) Interleukin Related CXCR TNF Receptor
  4. PDE4D inhibitor 1

PDE4-IN-1 is a PDE4 inhibitor with high potency (IC50 : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis.

For research use only. We do not sell to patients.

PDE4D inhibitor 1 Chemical Structure

PDE4D inhibitor 1 Chemical Structure

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PDE4D inhibitor 1 Related Antibodies

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Description

PDE4-IN-1 is a PDE4 inhibitor with high potency (IC50 : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis[1].

IC50 & Target[1]

PDE4B1

5.3 nM (IC50)

PDE4D2

8.6 nM (IC50)

PDE4A10

100 nM (IC50)

PDE4C1

747 nM (IC50)

PDE5A1

1730 nM (IC50)

PDE10A2

1953 nM (IC50)

PDE7A1

5913 nM (IC50)

PDE1B2

>10000 nM (IC50)

PDE2A

>10000 nM (IC50)

PDE3A

>10000 nM (IC50)

PDE8A1

>10000 nM (IC50)

PDE9A2

>10000 nM (IC50)

In Vitro

PDE4-IN-1 (Compound L30) (5-20 μM, 2 h) reduces the mRNA levels of the inflammatory cytokines (IL-1β , IL-6, and TNF-α) in LPS-induced Raw264.7 cells[1].
PDE4-IN-1 (5-20 μM, 24 h) reduces the mRNA levels of the inflammatory cytokines (CXCL-2, IL-17, and TNF-α) in M5-stimulated HaCaT cells[1].
PDE4-IN-1 (0-20 μM, 24 h) inhibits the proliferation of M5-stimulated HaCaT cells[1].
PDE4-IN-1 (20 μM, 24 h) decreases the protein expressions of K6 and K17 whilst upregulating the expression of differentiation protein (K1 and K10) in M5-stimulated HaCaT cells[1].
PDE4-IN-1 (20 μM, 2 h) with Roflumilast (HY-15455) restores cAMP levels and enhances phosphorylation of downstream CREB in M5-stimulated HaCaT cells[1].
PDE4-IN-1 (0-80 μM, 24 h) shows low cytotoxicities for RAW264.7 and HaCaT cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PDE4D inhibitor 1 Related Antibodies
In Vivo

PDE4-IN-1 (Compound L30) (0.3% ointment-100 mg, topical administration, 7 d) alleviates the psoriatic symptoms to reduce the severity of skin erythema in Imiquimod (IMQ) (HY-B0180)-induced psoriatic mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice models (6-8 weeks old, weighing 20-22 g each, a total of 40 mice) with 5% IMQ-containing cream for 7 days [1]
Dosage: 0.3% ointment-100 mg
Administration: Topical administrations
Result: Alleviated psoriatic symptoms and was more potent to decrease the thickness, scales, and erythema scores than Roflumilast (20 mg/kg) in the last 4 days.
Downregulated inflammatory cytokines and chemotaxis such as TNF-α, IL-1β, IL-6, IL-17, CXCL-2, and CCL-20.
Reduced protein expression of K6 and K17.
Reversed expression level of K1 and K10.
Exerted antipsoriasis effects by inhibiting the excessive proliferation and promoting poor differentiation.
Partly reversed the body weight loss and reduced skin thickness induced by IMQ suggesting low risk of toxicity in vivo.
Molecular Weight

489.47

Formula

C25H25F2NO7
SMILES

COC([C@H]1C[C@@H](OC2=C3OC(C4=CC=C(OC(F)F)C(OCC5CC5)=C4)=CC3=CC=C2O)CN1)=O
Shipping

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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PDE4D inhibitor 1 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:

PDE4D inhibitor 1Phosphodiesterase (PDE)Interleukin RelatedCXCRTNF ReceptorILCXC chemokine receptorsC-X-C motif chemokine receptorsTumor Necrosis Factor ReceptorTNFRPDE4anti-inflammatoryanti-psoriasiscAMPCREBRaw264.7 cellsHaCaT cellIMQpsoriatic modelBALB/c miceInhibitorinhibitorinhibit

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