IKKγ NBD 抑制肽是一种高度特异性的NF-κB抑制剂。IKKγ NBD 抑制肽通过阻断 IKKγ/NEMO 结合域 (NBD) 与 IKKα 和 IKKβ 之间的相互作用，而阻断 TNF-α 诱导的NF-κB激活。IKKγ NBD 抑制肽可显著降低炎症、改善脑缺血所致的神经功能缺损。
| 生物活性 | IKKγ NBD Inhibitory Peptide is a highly specific inhibitorNF-κBinhibitor. IKKγ NBD Inhibitory Peptide acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits[1][2][3]. |
体外研究
(In Vitro) | 在一个典型途径中，NF-κB 的激活依赖于 IKK 复合体的活性，该复合体由三个亚基 (IKKκ、IKKβ 和 IKKγ/NEMO) 组成，因此，KKγ NBD 抑制肽抑制 TNF-α 诱导的 NF- kb激活[2]。
IKKγ NBD 抑制肽 (10 μM; 90 min) 能够阻碍Doxorubicin(HY-15142A) 诱导 (15 μM;4 h) 的 BT-474 细胞中 p65 磷酸化[2]。
IKKγ NBD 抑制肽 (10 μM; 48 h) 对BT-474细胞活力有轻微抑制作用，而对 Doxorubicin 的效力有增强作用[2]。
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体内研究
(In Vivo) | IKKγ NBD 抑制肽 (40 μg/4 μL;ICV; 单剂量; 于 MCAO 诱导前 2 h) 在大鼠模型脑中动脉闭塞 (MCAO) 模型中显示出神经保护作用，减少 DNA 碎片化，其机制可能与减少缺血损伤后的炎症有关[3]。
| Animal Model: | Adult male Sprague-Dawley rats (255 g) with middle cerebral artery occlusion (MCAO)[3] | | Dosage: | 40 μg/4 μL | | Administration: | Intracerebroventricular injection; 2 h before MCAO induction | | Result: | Significantly reduced striatal IL-1b level in IKK-NBD peptide treated rats.
Also resulted in reduced staining of microglial OX-42 and protection of BBB from ischemic insult. |
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| 分子量 | |
| Formula | |
| CAS 号 | |
| Sequence Shortening | DRQIKIWFQNRRMKWKKTALDWSWLQTE |
| 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 (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>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. |
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