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PIK-75 hydrochloride

CAS No. : 372196-77-5

MCE 站：PIK-75 hydrochloride

产品活性：PIK-75 hydrochloride 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 hydrochloride 抑制 p110α 效果比抑制 p110β (IC₅₀=1.3 μM) 高 200 多倍。PIK-75 hydrochloride 诱导凋亡 (apoptosis)。

研究领域：Cell Cycle/DNA Damage  |  PI3K/Akt/mTOR  |  Apoptosis

作用靶点：DNA-PK  |  PI3K  |  Apoptosis

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.
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.
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.
PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death.
PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells.

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.

相关产品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  MG-132  |  3-Methyladenine  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  Acetylcysteine  |  Angiotensin II human  |  SP600125  |  5-Fluorouracil  |  Staurosporine  |  Bortezomib  |  Tamoxifen  |  2-Deoxy-D-glucose  |  Gemcitabine  |  Verteporfin  |  Decitabine  |  Actinomycin D  |  Temozolomide  |  BAY 11-7082  |  Etoposide  |  Mitomycin C  |  CCCP  |  DAPT  |  Rote  |  Etomoxir  |  Wortmannin  |  Stattic

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