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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
Pricing and availability is not currently available.

Quality Level

100

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

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4-Hydroxy-L-isoleucine phyproof® Reference Substance

PHL80474

4-Hydroxy-L-isoleucine

4-Hydroxy-L-isoleucine ≥98.0% (TLC)

49549

4-Hydroxy-L-isoleucine

4-Hydroxyisoleucine United States Pharmacopeia (USP) Reference Standard

1327319

4-Hydroxyisoleucine

4-Hydroxyisophthalic acid phyproof® Reference Substance

PHL80863

4-Hydroxyisophthalic acid

grade

primary reference standard

grade

-

grade

pharmaceutical primary standard

grade

primary reference standard

product line

phyproof® Reference Substance

product line

-

product line

-

product line

phyproof® Reference Substance

assay

≥98.0% (HPLC)

assay

≥98.0% (TLC)

assay

-

assay

≥90.0% (HPLC)

form

solid

form

-

form

-

form

solid

manufacturer/tradename

PhytoLab

manufacturer/tradename

-

manufacturer/tradename

USP

manufacturer/tradename

PhytoLab

General description

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

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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