KT5823

貨號 Cat. No.: K-250
規格 Size: 50 Î¼g 5x50 Î¼g 0.5mg

Description

KT5823

A Selective PKG Inhibitor

Product#:

K-250

Sizes:

50 mg

5 x 50 mg

0.5 mg

M.W.:

495 Daltons

CAS No.:

[126643-37-6]

Structure:

Purity:

Greater than 98% as evaluated by HPLC.

Bioassay:

The biological activity was tested to confirm the ability of KT5823 to inhibit PKG.

C6 glioma cells were grown to 70% confluence, and then serum starved for 18 h.

The cells were preincubated for 30 min in different concentrations of KT5823 and stimulated with 8Br-cGMP (100mM, 4h 37^oC) for PKG activation. Cell extracts were blotted and PKG activity analyzed by measuring the PKG substrate PLCb3, with anti phospho-PLCb3 (p-PLCb3).

References:

1.	Kase, H. et al. (1987) B.B.R.C. 142, 436.
2.	Hidaka, H. and Kobayashi, R. (1992) Annu. Rev. Pharmacol. Toxicol. 32, 377.
3.	Chijiwa, T. et al. (1990) J. Biol. Chem. 265, 5267.
4.	Ruth, P. (1999) Pharmacol. Ther. 82, 355.
5.	Pfeifer, A. et al. (1998) EMBO J. 17, 3045.
6.	Chan, S.L, and Fiscus, R.R. (2003) Mol. Hum. Reprod. 12, 775.

KT5823 is a semi-synthetic derivative of K525a.¹ It is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC₅₀=234nM). KT5823 interferes at the level of the ATP binding site of the catalytic domain of PKG.^2,3The PKG are Ser/Thr protein kinase with broad substrate specificity, and expressed in; brain, smooth muscle cells, platelets, juxtaglomerular kidney cells, and endothelial cells.^4,5KT5823 triggered apoptotic DNA fragmentation in immortalized uterine epithelial cells, suggesting a regulatory role for PKG in the apoptotic process in these cells.⁶

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