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TAPI-1

Inhibitor of TNF-α processing
 
BML-PI134-0001 1 mg 289.00 USD
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Inhibitor of TNF-α processing (IC50 is approximately 100 nM using in vitro TNF peptide cleavage assay), similar to TAPI-0, but more stable in tissue culture and in vivo. Inhibits TACE and other metalloproteases. Blocks release of TNF-α (IC50=50-100 µM)1, APP (1-8 µM), ACE (10 µM), IL6R (5-10 µM), TNFRI (5-10 µM), TNFRII (25-50 µM), and ObRa (leptin receptor), but not CSF-1, from cells in culture.

Product Specification

Alternative Name:IC2, N-(R)-(2-(Hydroxyaminocarbonyl)methyl)-4-methylpentanoyl-L-naphthylalanyl-L-alanine 2-aminoethyl amide
 
Sequence:N-(R)-(2-(Hydroxyaminocarbonyl)methyl)-4-methylpentanoyl-L-naphthylalanyl-L-alanine 2-aminoethyl amide
 
Formula:C26H37N5O5
 
MW:499.3
 
Purity:≥98% (HPLC)
 
Appearance:Lyophilized solid.
 
Solubility:Soluble in DMSO or methanol
 
Shipping:Shipped on Dry Ice
 
Long Term Storage:-20°C
 
Use/Stability:Aliquot stock solutions and freeze at -20°C for up to one month. Do not store diluted solutions.
 
Handling:Hygroscopic. Protect from light.
 
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Product Literature References

ADAM12 and ADAM17 are essential molecules for hypoxia-induced impairment of neural vascular barrier function: D. Cui, et al.; Sci. Rep. 5, 12796 (2015), Application(s): Cell Culture, Abstract;
A disintegrin and metalloproteinase 12 (ADAM12) localizes to invasive trophoblast, promotes cell invasion and directs column outgrowth in early placental development: M. Aghababaei, et al.; Mol. Hum. Reprod. 20, 235 (2014), Abstract;
Insulin treatment attenuates renal ADAM17 and ACE2 shedding in diabetic Akita mice: E.S. Salem, et al.; Am. J. Physiol. Renal Physiol. 306, F629 (2014), Abstract;
A Lactobacillus rhamnosus GG-derived soluble protein, p40, stimulates ligand release from intestinal epithelial cells to transactivate epidermal growth factor receptor: F. Yan, et al.; J. Biol. Chem. 288, 30742 (2013), Abstract;
Hydroquinone-induced miR-122 down-regulation elicits ADAM17 up-regulation, leading to increased soluble TNF-α production in human leukemia cells with expressed Bcr/Abl: Y.J. Chen, et al.; Biochem. Pharmacol. 86, 620 (2013), Abstract;
Superantigens are critical for Staphylococcus aureus Infective endocarditis, sepsis, and acute kidney injury: W. Salgado-Pabon, et al.; MBio 4, e00494 (2013), Abstract; Full Text
A disintegrin and metalloproteinase 17 (ADAM17) and epidermal growth factor receptor (EGFR) signaling drive the epithelial response to Staphylococcus aureus toxic shock syndrome toxin-1 (TSST-1): M. Breshears, et al.; J. Biol. Chem. 287, 32578 (2012), Abstract; Full Text
Constitutive shedding of the amyloid precursor protein ectodomain is up-regulated by tumour necrosis factor-alpha converting enzyme: B.E. Slack et al.; Biochem. J. 357, 787 (2001), Abstract;
Generation of human soluble leptin receptor by proteolytic cleavage of membrane-anchored receptors: M. Maamra. et al.; Endocrinology 142, 4389 (2001), Abstract;
Phorbol ester-induced juxtamembrane cleavage of angiotensin-converting enzyme is not inhibited by a stalk containing intrachain disulfides: S.L.U. Schwager; Biochemistry 37, 15449 (1998), Abstract;
A metalloprotease-inhibitor reduces pain associated behavior in mice with experimental neuropathy: C. Sommer; Neurosci. Lett. 237, 45 (1997), Abstract;
Membrane protein secretases: N.M. Hooper, et al.; Biochem. J. 321 , 265 (1997), Abstract;
A metalloprotease inhibitor blocks shedding of the 80-kD TNF receptor and TNF processing in T lymphocytes: P.D. Crowe, et al.; J. Exp. Med. 181, 1205 (1995), Abstract;
A metalloprotease inhibitor blocks shedding of the IL-6 receptor and the p60 TNF receptor: J. Müllberg, et al.; J. Immunol. 155, 5198 (1995), Abstract;
Protection against a lethal dose of endotoxin by an inhibitor of tumour necrosis factor processing: K.M. Mohler, et al.; Nature 370, 218 (1994), Abstract;

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