1. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  2. DNA-PK Apoptosis
  3. STL127705

STL127705 (Compound L) 是一种有效的 Ku 70/80 异二聚体蛋白 Ku 70/80 heterodimer protein 抑制剂,IC50 为 3.5 μM。STL127705 通过抑制 DNA-PKCS 激酶的激活干扰 Ku70/80 与 DNA 的结合。STL127705 显示出抗增殖和抗肿瘤活性。 STL127705 诱导细胞凋亡 (apoptosis) 。

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STL127705 Chemical Structure

STL127705 Chemical Structure

CAS No. : 1326852-06-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC50 of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis[1][2].

IC50 & Target

IC50: 3.5 μM (Ku 70/80), 2.5 μM (DNA-PKCS)[1]

体外研究
(In Vitro)

STL127705 (Compound L) (0-100 μM) inhibits binding of Ku70/80 to a DNA substrate and inhibits Ku-dependent activation of the DNA-PKCS kinase[1].
? STL127705 (0-100 μM; 6h) decreases the expression of DNA-PKCS auto-phosphorylation in SF-767 cells[1].
? STL127705 (0-40 μM; 6h) shows antiproliferative activity in a dose dependent manner[1].
? TL127705 (1 μM; 48 h) significantly promotes apoptotic when combination with gemcitabine[2].

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

Cell Viability Assay[1]

Cell Line: SF-767, PrEC cells
Concentration: 0-40 µM
Incubation Time: 6 h
Result: Showed cytotoxicity in a dose dependent manner.

Western Blot Analysis[1]

Cell Line: SF-767 cells
Concentration: 0-100 µM
Incubation Time: pre-treated for 2 h and then co-incubation 4 h
Result: Decreased the DNA-PKCS autophosphorylation but total DNA-PKCS was not suppressed by STL127705.

Apoptosis Analysis[1]

Cell Line: H1299 cells
Concentration: 1 µM
Incubation Time: 48 h
Result: Induced apoptosis with apoptosis rate significantly increased to 76% when treated with STL127705 in combination with gemcitabine.
分子量

437.42

Formula

C22H20FN5O4

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

*STL127705 is usually formulated as a suspension.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

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工作液所需浓度 : mg/mL
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纯度 & 产品资料
参考文献
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
STL127705
目录号:
HY-122727
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