SynKinase

MBP146-78

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Product Details
Synonyms 4-[2-(4-Fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl] pyridine
Product Type Chemical
Properties
Formula C21H22FN3
MW 335.4
CAS 188343-77-3
Purity Chemicals ≥95% (HPLC)
Appearance Solid.
Solubility Soluble in DMSO.
Declaration Manufactured by SynKinase.
Other Product Data Target: PKG | Kinase Group: AGC | Substrate: Serine-Threonine
InChi Key RBWNFHXBUDPAIO-UHFFFAOYSA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Description

MBP146-78 inhibits the growth of Eimeria spp. both in vitro and in vivo. The molecular target of MBP146-78 was identified as cGMP-dependent protein kinase (PKG) using a tritiated analogue to purify a approximately 120-kDa protein from lysates of Eimeria tenella. This represents the first example of a protozoal PKG. MBP146-78 is a potent inhibitor of both soluble and membrane-associated isoforms of native PKG, as well as recombinant enzyme, with an IC50 of <1nm.

Product References
  1. Purification and molecular characterization of cGMP-dependent protein kinase from Apicomplexan parasites. A novel chemotherapeutic target: A.M. Gurnett, et al.; J. Biol. Chem. 277, 15913 (2002)
  2. Toxoplasma gondii cyclic GMP-dependent kinase: chemotherapeutic targeting of an essential parasite protein kinase: R.G. Donald, et al.; Eukaryot. Cell 1, 317 (2002)
  3. A role for coccidian cGMP-dependent protein kinase in motility and invasion: H.I. Wiersma, et al.; Int. J. Parasitol. 34, 369 (2004)
  4. Characterization of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG): antiparasitic activity of a PKG inhibitor: C.A. Diaz, et al.; Mol. Biochem. Parasitol. 146, 78 (2006)
  5. Anticoccidial kinase inhibitors: identification of protein kinase targets secondary to cGMP-dependent protein kinase: R.G. Donald, et al.; Mol. Biochem. Parasitol. 149, 86 (2006)
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