标签归档：cllfvy

TAT-cyclo-CLLFVY TFA

发表于由

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 TFAamp;;

TAT-cyclo-CLLFVY TFA Chemical Structure

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

* Please select Quantity before adding items.

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].

MCE 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 (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]. 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.

TAT-cyclo-CLLFVY

发表于由

TAT-cyclo-CLLFVY; 纯度: 99.09%

TAT-cyclo-CLLFVY 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 破坏 HIF-1α/HIF-1β 蛋白相互作用，IC50 为 1.3 μM。

TAT-cyclo-CLLFVYamp;;

TAT-cyclo-CLLFVY Chemical Structure

CAS No. : 1446322-66-2

规格 价格 是否有货 数量
1 mg ￥2100 In-stock
5 mg ￥7400 In-stock
10 mg ￥11800 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

TAT-cyclo-CLLFVY 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY 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].

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

2559.08

Formula

C111H188N42O24S2
CAS 号

1446322-66-2
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
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:;

DMSO : 50 mg/mL (19.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.3908 mL 1.9538 mL 3.9077 mL
5 mM 0.0782 mL 0.3908 mL 0.7815 mL
10 mM 0.0391 mL 0.1954 mL 0.3908 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (0.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.98 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (0.98 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (0.98 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (0.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
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.