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In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AN-2728 is an inhibitor of PDE4 with IC50 value of 0.49 μM [1]. PDE4 is a phosphodiesterase and plays an important role in the chronic inflammation associated with psoriasis and atopic dermatitis [2].AN-2728 is a boron-containing, anti-inflammatory, topically administered compound that inhibits PDE4 activity and suppresses the release of TNF-α, IL-23, IL-12 and other cytokines [2]. In cell based assays, AN-2728 inhibited cytokine release of TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.54, 0.61, 0.83, 2.4 and 5.3 μM, respectively [1].AN-2728 was well tolerated and had good therapeutic potential. AN-2728 is now in clinical development for the treatment of psoriasis and atopic dermatitis [2]. References:[1]. Akama T, Baker SJ, Zhang YK, et al. Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis. Bioorg Med Chem Lett, 2009, 19(8): 2129-2132. [2]. Nazarian R, Weinberg JM. AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin Investig Drugs, 2009, 10(11): 1236-1242.
Cell lines
Peripheral blood mononuclear cells (PBMCs)
Preparation method
The solubility of this compound in DMSO is >12.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition
10 μM
Applications
AN-2728 showed a broad range of potent cytokine release inhibition, such as TNF-α, IL-23, IL-12 and other cytokines.
Animal models
Phorbol ester-induced mouse ear edema model
Dosage form
1 mg/ear×2
Application
AN-2728 demonstrated in vivo efficacy in phorbol ester-induced mouse ear edema model by topical application. AN-2728 showed significant inhibition against the ear edema.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References:
[1]. Akama T, Baker S J, Zhang Y K, et al. Discovery and structure–activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis[J]. Bioorganic & medicinal chemistry letters, 2009, 19(8): 2129-2132.