370655
PKG Iα Inhibitor, Cell-Permeable
The PKG Iα Inhibitor, Cell-Permeable controls the biological activity of PKG Iα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
PKG Iα Inhibitor, Cell-Permeable, DT-3, RQIKIWFQNRRMKWKKLRKKKKKH, PKG Inhibitor VIII
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About This Item
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Quality Level
assay
≥95% (HPLC)
form
lyophilized
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A highly potent, reversible, and substrate competitive membrane-permeable Drosophila Antennapedia homeodomain fused-peptide that selectively inhibits protein kinase G Iα (Ki = 25 nM). Shown to efficiently translocate into arterial smooth muscle cells and inhibit NO-induced vasodilation (ED50 = 47 µM). Inhibits protein kinase A at much higher concentrations (Ki = 493 µM). The carrier peptide is also available under Cat. no. 287895.
A highly potent, reversible, and substrate competitive membrane-permeable peptide that selectively inhibits protein kinase G Iα (PKG Iα) (Ki = 25 nM). Inhibitor peptide is fused to the Drosophila Antennapedia homeo domain peptide to allow membrane permeability. Shown to efficiently cross the membrane of arterial smooth muscle cells and inhibit nitric oxide-induced (NO-induced) vasodilation (EC50 = 47 µM). Inhibits protein kinase A (PKA) activity only at much higher concentrations (Ki = 493 µM). The carrier peptide is also available under Cat. no. 287895.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PKG1α
PKG1α
Product competes with ATP.
Reversible: yes
Target Ki: 25 nM against protein kinase G Iα
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Sequence
H-Arg-Gln-Ile-Lys-Ile-Trp-Phe-Gln-Asn-Arg-Arg-Met-Lys-Trp-Lys-Lys-Leu-Arg-Lys-Lys-Lys-Lys-Lys-His-OH
Physical form
Supplied as a trifluoroacetate salt.
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.
Other Notes
Dostmann, W. R.G., et al. 2000. Proc. Natl. Acad. Sci. USA 97, 14772.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Nature communications, 13(1), 149-149 (2022-01-12)
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