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Background: KT5823, a semi-synthetic derivate of K-252a, is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG). The in vitro inhibition constant (Ki) for PKG is 234 nM compared to Ki values of 10 µM and 4 µM for PKA and PKC, respectively. KT5823 induces G1 arrest and apoptotic fragmentation of DNA.
Chemical formula: C29H23IN3O5
Molecular weight: 495.5 g/mol
Appearance: white powder
Purity: >99% (HPLC)
Solubility: soluble in DMSO or DMF
CAS number: 126643-37-6
Hidaka H, Kobayashi R. (1992) "Pharmacology of protein kinase inhibitors.", Annu Rev Pharmacol Toxicol.;32:377-97.
Gadbois DM, Crissman HA, Tobey RA, Bradbury EM. (1992) "Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells." Proc Natl Acad Sci U S A.;89(18):8626-30.
Chan SL, Fiscus RR.(2003)"Guanylyl cyclase inhibitors NS2028 and ODQ and protein kinase G (PKG) inhibitor KT5823 trigger apoptotic DNA fragmentation in immortalized uterine epithelial cells: anti-apoptotic effects of basal cGMP/PKG"Mol Hum Reprod.; 12:775-83.
PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.
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