PKA Inhibitor Fragment (6-22) amide TFA
(Synonyms: PKI-(6-22)-amide TFA) 目录号 : GC61512
PKA inhibitor fragment (6-22) amide TFA是一种cAMP依赖性蛋白激酶A（PKA）的合成肽抑制剂，Ki=1.7 nM。
Sample solution is provided at 25 µL, 10mM.
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PKA inhibitor fragment (6-22) amide TFA is a synthetic peptide inhibitor of cAMP-dependent protein kinase A (PKA) with Ki=1.7 nM. PKA inhibitor fragment (6-22) amide TFA is derived from the thermostable PKA inhibitor protein PKI and is the shortest synthetic PKI peptide that retains potent PKA inhibitory activity[1]. Both the arginine pseudosubstrate site at the COOH-terminus of the PKI peptide and the NH2-terminal residue Phe10 are required for this efficient inhibition[2].
PKA inhibitor fragment (6-22) amide TFA (20 μM) can reverse the increase in cAMP level and PN-1 mRNA expression in AtT-20 cells induced by serine protease inhibitors[3]. Moreover, 10 μM PKA inhibitor fragment (6-22) amide TFA can also promote lactate dehydrogenase (LDH) release in human fibroblasts (WS1) and human keratinocytes (HaCaT) cells[4].
References:
[1] Glass, D.B., Cheng, H.C., Mende-Mueller, L., et al.Primary structural determinants essential for potent inhibition of cAMP-dependent protein kinase by inhibitory peptides corresponding to the active portion of the heat-stable inhibitor proteinJ. Biol. Chem.264(15)8802-8810(1989)
[2] Glass, D.B., Lundquist, L.J., Katz, B.M., et al.Protein kinase inhibitor-(6-22)-amide peptide analogs with standard and nonstandard amino acid substitutions for phenylalanine 10. Inhibition of cAMP-dependent protein kinaseJ. Biol. Chem.264(24)14579-14584(1989)
[3] Hisatsugu Koshimizu, Niamh X. Cawley, Taeyoon Kim, Alfred L. Yergey, Y. Peng Loh, Serpinin: A Novel Chromogranin A-Derived, Secreted Peptide Up-Regulates Protease Nexin-1 Expression and Granule Biogenesis in Endocrine Cells, Molecular Endocrinology, Volume 25, Issue 5, 1 May 2011, Pages 732–744.
[4] Yang T, Geng F, Tang X, et al. UV radiation‐induced peptides in frog skin confer protection against cutaneous photodamage through suppressing MAPK signaling[J]. MedComm, 2024, 5(7): e625.
| Cell experiment [1]: | |
Cell lines | AtT-20 cells |
Preparation Method | AtT-20 cells were incubated in the presence or absence of 10 nM serpinin with or without 20 μM PKA inhibitor fragment (6-22) amide TFA for 20 h. Detection of PN-1 mRNA level by RT-PCR. |
Reaction Conditions | 20 μM , 20 h |
Applications | In the presence of PKA inhibitor fragment (6-22) amide TFA, serpinin-inducing elevation of PN-1 mRNA was prevented. |
References: | |
| Cas No. | SDF | ||
| 别名 | PKI-(6-22)-amide TFA | ||
| 分子式 | C82H131F3N28O26 | 分子量 | 1982.08 |
| 溶解度 | Water: 50 mg/mL (25.23 mM) | 储存条件 | -20°C, away from moisture |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.5045 mL | 2.5226 mL | 5.0452 mL |
| 5 mM | 0.1009 mL | 0.5045 mL | 1.009 mL |
| 10 mM | 0.0505 mL | 0.2523 mL | 0.5045 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet