2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  3. DNA-PK PI3K Apoptosis
  4. PIK-75

PIK-75 是一种可逆的 DNA-PK 和 p110α-选择性的抑制剂，抑制 DNA-PK，p110α 和 p110γ，IC50 分别为 2，5.8 和 76 nM。PIK-75 抑制 p110α 效果比抑制 p110β (IC50=1.3 μM) 高 200 多倍。PIK-75 诱导凋亡 (apoptosis)。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 PIK-75 hydrochloride 通常具有更好的水溶性和稳定性。

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PIK-75 Chemical Structure

PIK-75 Chemical Structure

CAS No. : 372196-67-3

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PIK-75 的其他形式现货产品:

Customer Review

Other Forms of PIK-75:

PIK-75 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM)[1][2]. PIK-75 induces apoptosis[3].

IC50 & Target

DNA-PK

2 nM (IC50)

p110α

5.8 nM (IC50)

p110γ

76 nM (IC50)

p110δ

510 nM (IC50)

p110β

1.3 μM (IC50)

hsVPS34

2.6 μM (IC50)

PI3KC2β

1 μM (IC50)

PI3KC2α

10 μM (IC50)

mTORC1

1 μM (IC50)

mTORC2

10 μM (IC50)

ATM

2.3 μM (IC50)

ATR

21 μM (IC50)

PI4KIIIβ

50 μM (IC50)

体外研究
(In Vitro)

PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC50s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively[1].
PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC50 values of 1.2 and 1.3 μM, respectively[1].
PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC50 of 78 nM[2].
PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death[3].
PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells[3].

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

PIK-75 相关抗体:

Cell Viability Assay[3]

Cell Line: Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1)
Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM
Incubation Time: 48 hours
Result: Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment.

Western Blot Analysis[2]

Cell Line: Overnight-starved CHO-IR cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 5 minutes
Result: Blocked the phosphorylation of PKB induced by insulin (1 nM, 10 min) on both Ser473and Thr308 in a dose-dependent manner. PIK-75 potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice[3].
体内研究
(In Vivo)

PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice[3].

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

Animal Model: Mice bearing tumors of MIA PaCa-2[3]
Dosage: 2 mg/kg; or combination with Gemcitabine (20 mg/kg)
Administration: Administered injection; 5 times per week. 25 days
Result: Reduced the tumor growth and enhanced the antitumor effect.
分子量

452.28

Formula

C16H14BrN5O4S
CAS 号
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.
纯度 & 产品资料
参考文献

PIK-75 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

PIK-75372196-67-3PIK75PIK 75DNA-PKPI3KApoptosisDNA-dependent protein kinasePhosphoinositide 3-kinasep110αPKBCHO-IRcellspancreaticcancerapoptoticInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-107834
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