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。
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)。
PIK-75 Chemical Structure
CAS No. : 372196-67-3
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
PIK-75 的其他形式现货产品:
PIK-75 hydrochloride
| 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].
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| IC50 & Target |
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p110α
5.8 nM (IC50)
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p110γ
76 nM (IC50)
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p110δ
510 nM (IC50)
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p110β
1.3 μM (IC50)
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hsVPS34
2.6 μM (IC50)
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PI3KC2β
1 μM (IC50)
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PI3KC2α
10 μM (IC50)
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PI4KIIIβ
50 μM (IC50)
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ATM
2.3 μM (IC50)
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ATR
21 μM (IC50)
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mTORC1
1 μM (IC50)
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mTORC2
10 μM (IC50)
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DNA-PK
2 nM (IC50)
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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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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]. |
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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].
上海金畔生物科技有限公司 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. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.
[2]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58.
[3]. Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69.
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