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370655

Sigma-Aldrich

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

Empirical Formula (Hill Notation):
C152H258N52O28S
Molecular Weight:
3294.07
UNSPSC Code:
12352200
NACRES:
NA.77

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
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

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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Malgorzata Szaroszyk et al.
Nature communications, 13(1), 149-149 (2022-01-12)
Cachexia is associated with poor prognosis in chronic heart failure patients, but the underlying mechanisms of cachexia triggered disease progression remain poorly understood. Here, we investigate whether the dysregulation of myokine expression from wasting skeletal muscle exaggerates heart failure. RNA

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