TAT-cyclo-CLLFVY TFA

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TAT-cyclo-CLLFVY TFA 

TAT-cyclo-CLLFVY TFA 是一种 HIF-1 异二聚化的环肽抑制剂，可抑制癌细胞中的缺氧信号传导。TAT-cyclo-CLLFVY TFA 破坏 HIF-1α/HIF-1β 蛋白相互作用，IC50 为 1.3 μM。

TAT-cyclo-CLLFVY TFA

TAT-cyclo-CLLFVY TFA Chemical Structure

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TAT-cyclo-CLLFVY TFA 的其他形式现货产品:

TAT-cyclo-CLLFVY

生物活性

TAT-cyclo-CLLFVY TFA is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY TFA disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM[1].

体外研究
(In Vitro)

TAT-cyclo-CLLFVY inhibits HIF-1 activity in a mammalian cell luciferase reporter assay[1].
Hypoxia (1% O2) results in a ~12-fold increase in the luciferase signal, which is inhibited in a dose-dependent manner by TAT-cyclo-CLLFVY (IC50 of 19±2 μM)[1].
To assess the cell-specificity of TAT-cyclo-CLLFVY, the experiment is repeated in MCF-7 breast cancer cells with similar results (TAT-cyclo-CLLFVY IC50 of 16±1 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

2673.10

Formula

C113H189F3N42O26S2
Sequence Shortening

CGRKKRRQRRRPPQ.cyclo(CLLFVY) (Disulfide bridge:Cys1-Cys1′)
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.
参考文献

  • [1]. Elena Miranda, et al. A cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. J Am Chem Soc. 2013 Jul 17;135(28):10418-25.

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