PKA Inhibitor Fragment (6-22) amide(Synonyms: PKI-(6-22)-amide)

PKA Inhibitor Fragment (6-22) amide;(Synonyms: PKI-(6-22)-amide)

PKA Inhibitor Fragment (6-22) amide 是 cAMP 依赖性蛋白激酶 A (PKA) 的抑制剂,Ki 值为 2.8 nM。PKA Inhibitor Fragment (6-22) amide 可显着逆转小鼠低水平的吗啡缓解疼痛的感受。

PKA Inhibitor Fragment (6-22) amideamp;;(Synonyms: PKI-(6-22)-amide)

PKA Inhibitor Fragment (6-22) amide Chemical Structure

CAS No. : 121932-06-7

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

* Please select Quantity before adding items.

PKA Inhibitor Fragment (6-22) amide 的其他形式现货产品:

PKA Inhibitor Fragment (6-22) amide TFA

生物活性

PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice[1][2].

IC50 Target

PKA

2.8 nM (Ki)

分子量

1868.06

Formula

C80H130N28O24

CAS 号

121932-06-7

Sequence Shortening

TYADFIASGRTGRRNAI-NH2

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.

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]. Katz BM, et, al. Synthesis, characterization and inhibitory activities of (4-N3[3,5-3H]Phe10)PKI(6-22)amide and its precursors: photoaffinity labeling peptides for the active site of cyclic AMP-dependent protein kinase. Int J Pept Protein Res. 1989 Jun;33(6):439

    [2]. Dalton GD, et, al. Alterations in brain Protein Kinase A activity and reversal of morphine tolerance by two fragments of native Protein Kinase A inhibitor peptide (PKI). Neuropharmacology. 2005 Apr; 48(5): 648-57.

STAD 2

STAD 2;

STAD 2 是一种有效和选择性的 PKA-RII 破坏剂,Kd 值为 6.2 nM。STAD 2 以异构体选择性方式破坏 PKA 和 AKAP 之间的相互作用。STAD 2 通过独立于 PKA 的机制显示出抗疟活性。

STAD 2amp;;

STAD 2 Chemical Structure

CAS No. : 1542100-77-5

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

* Please select Quantity before adding items.

生物活性

STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism[1][2].

IC50 Target

PKA-RII[1]

分子量

2096.68

Formula

C102H182N24O22

CAS 号

1542100-77-5

Sequence Shortening

KKLAKFLVS{Aaa}ALK{Aaa}ALK (Covalent bridge:Aaa10-Aaa14)

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.

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]. Wang Y, et, al. Isoform-selective disruption of AKAP-localized PKA using hydrocarbon stapled peptides. ACS Chem Biol. 2014 Mar 21;9(3):635-42.

    [2]. Flaherty BR, et, al. The Stapled AKAP Disruptor Peptide STAD-2 Displays Antimalarial Activity through a PKA-Independent Mechanism. PLoS One. 2015 May 26;10(5):e0129239.