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PKG inhibitor peptide

发表于由

PKG inhibitor peptide; 纯度: 98.15%

PKG inhibitor peptide 是一种 ATP 竞争性的 PKG 抑制剂，Ki 值为 86 μM。

PKG inhibitor peptideamp;;

PKG inhibitor peptide Chemical Structure

CAS No. : 82801-73-8

规格 价格 是否有货 数量
1 mg ￥900 In-stock
5 mg ￥2800 In-stock
10 mg ￥4500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

PKG inhibitor peptide 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Peptide Library

生物活性

PKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM[1].

IC50 Target

Ki: 86 μM (PKG)[1]
体外研究
(In Vitro)

Summary of experiments showing that intracellular dialysis of postsynaptic cells with PKG inhibitor PKG inhibitor peptide (1 mM) failed to alter the induction of long-term depression (CCh-LTD)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

943.11

Formula

C38H74N18O10
CAS 号

82801-73-8
Sequence Shortening

RKRARKE
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : 100 mg/mL (106.03 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0603 mL 5.3016 mL 10.6032 mL
5 mM 0.2121 mL 1.0603 mL 2.1206 mL
10 mM 0.1060 mL 0.5302 mL 1.0603 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Bhatnagar D, et al. Synthetic peptide analogues differentially alter the binding affinities of cyclic nucleotide dependent protein kinases for nucleotide substrates. Biochemistry. 1988 Mar 22;27(6):1988-94.

    [2]. Chiung-Chun Huang, et al. Activation of muscarinic acetylcholine receptors induces a nitric oxide-dependent long-term depression in rat medial prefrontal cortex. Cereb Cortex. 2010 Apr;20(4):982-96.

PKG inhibitor peptide TFA

发表于由

PKG inhibitor peptide TFA;

PKG inhibitor peptide TFA 是一种 ATP 竞争性的 PKG 抑制剂，Ki 值为 86 μM。

PKG inhibitor peptide TFAamp;;

PKG inhibitor peptide TFA Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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PKG inhibitor peptide TFA 的其他形式现货产品:

PKG inhibitor peptide

生物活性

PKG inhibitor peptide TFA is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM[1].

IC50 Target

Ki: 86 μM (PKG)[1]
体外研究
(In Vitro)

Summary of experiments showing that intracellular dialysis of postsynaptic cells with PKG inhibitor PKG inhibitor peptide TFA (1 mM) failed to alter the induction of long-term depression (CCh-LTD)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

1057.13

Formula

C40H75F3N18O12
Sequence

Arg-Lys-Arg-Ala-Arg-Lys-Glu
Sequence Shortening

RKRARKE
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Bhatnagar D, et al. Synthetic peptide analogues differentially alter the binding affinities of cyclic nucleotide dependent protein kinases for nucleotide substrates. Biochemistry. 1988 Mar 22;27(6):1988-94.

PKG Substrate

发表于由

PKG Substrate;

PKG Substrate 是一种 cGMP 依赖性的蛋白激酶 (PKG) 的选择性底物。

PKG Substrateamp;;

PKG Substrate Chemical Structure

规格 价格 是否有货 数量
1 mg ￥1100 In-stock
5 mg ￥3900 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

PKG Substrate is a selective substrate for cGMP-dependent protein kinase (PKG).

IC50 Target

PKG[1]
体外研究
(In Vitro)

Incorporation of [33P]ATP into the synthetic peptide PKG substrate RKRSRAE is measured. N6-benzyl-ATP inhibits kinase activity of PKG Iα gatekeeper mutants but not WT. The serotonin transporter (SERT) is responsible for reuptake of serotonin (5-hydroxytryptamine) after its exocytotic release from neurons. SERT is regulated by several processes, including a cyclic GMP signaling pathway involving nitric oxide synthase, guanylyl cyclase, and PKG[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

902.01

Formula

C35H67N17O11
Sequence

Arg-Lys-Arg-Ser-Arg-Ala-Glu
Sequence Shortening

RKRSRAE
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light, stored under nitrogen

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)
Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Wong A, et al. Cyclic GMP-dependent stimulation of serotonin transport does not involve direct transporter phosphorylation by cGMP-dependent protein kinase. J Biol Chem. 2012 Oct 19;287(43):36051-8.
Kinase Assay
[1]

Kinase activity is measured by determining the amount of 33P radioactivity incorporated from [33P]ATP or [33P]N6-benzyl-ATP into a PKG specific peptide substrate (RKRSRAE). The standard 75 μL assay mixture contains 0.15 μCi of [33P]ATP, 10 μM ATP, 15 μM PKG peptide substrate, 2 μM PKI (a synthetic peptide inhibitor of cAMP-dependent protein kinase), 1 μg of purified kinase, and 100 μM 8-Br-cGMP in 50 mM HEPES buffer, pH 7.4, containing 10 mM MgCl2, 0.1% Tween 20, and 1 mM DTT. After incubation at 30°C for 2 min, the reaction is immediately put on ice, and 20 μL of the assay mixture is spotted onto P81 phosphocellulose paper and then quenched in 0.42% H3PO4. The paper is further washed three times in 0.42% H3PO4 for 10 min with gentle agitation and rinsed once with acetone. After air drying, radioactivity on the paper is measured with a Beckman LS6500 liquid scintillation counter. For measuring the effect of N6-benzyl-ATP on the activity of PKG I utilizing ATP as a co-substrate, unlabeled N6-benzyl-ATP is added to each reaction at the indicated concentrations. Saturation kinetic analyses for Km and Vmax with ATP or N6-benzyl-ATP are performed over a concentration range (0.0015-100 μM) by adding unlabeled ATP or N6-benzyl-ATP to a given amount of [33P]ATP or [33P]N6-benzyl-ATP, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Wong A, et al. Cyclic GMP-dependent stimulation of serotonin transport does not involve direct transporter phosphorylation by cGMP-dependent protein kinase. J Biol Chem. 2012 Oct 19;287(43):36051-8.