KP-457 |
Catalog No.GC32452 |
KP‐457 es un inhibidor selectivo de ADAM17, que tiene una estructura de hidroxamato inverso.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1365803-52-6
Sample solution is provided at 25 µL, 10mM.
KP‐457 is a selective ADAM17 inhibitor, which has a reverse-hydroxamate structure. ADAM17, also known as TNF-α-converting enzyme, cleaves various molecules such as GPIbα, GPV, and TNF-α. KP‐457 inhibited cleavages of the TNF‐α sequence with 10 times the potency of GM‐6001 and was >50 times more selective for ADAM17 than for other MMPs and ADAM10 in cell‐free enzyme assays.[1]
The inhibition of C-terminal cleavage of the GPIbα sequence by ADAM17 was concentration dependent, with an IC50 of 10.6 nmol/l for KP-457. KP-457 at the lower concentration blocks Zn2+ chelation of the catalytic domain of ADAM17. Other studies confirmed that KP-457 exhibited neither genotoxicity nor systemic toxicity at doses up to 3 mg/kg administered to dogs intravenously once a day for 1 month. In vitro study also demonstrated that KP-457 could sustain intact GPIbα at levels seen in platelets freshly isolated from human blood. In addition, KP-457 inhibited GPIbα shedding with a potency 10 times that of GM-6001 in the cellular assay.[1]
References:
[1]. Hirata S, et al. Selective Inhibition of ADAM17 Efficiently Mediates Glycoprotein Ibα Retention During Ex Vivo Generation of Human Induced Pluripotent Stem Cell-Derived Platelets. Stem Cells Transl Med. 2017 Mar;6(3):720-730.
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