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CAS No. : 24418-86-8
MCE 国际站:SKI V
产品活性:SKI V 是一种非竞争性的,有效的非脂质鞘氨醇激酶 (SPHK; SK) 抑制剂,对 GST-hSK 的 IC50 为 2 μM。 SKI V 有效抑制 PI3K,对 hPI3k 的 IC50 为 6 μM。SKI V 减少有丝分裂的第二信使鞘氨醇-1-磷酸 (S1P) 的形成。SKI V 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。
研究领域:Immunology/Inflammation | PI3K/Akt/mTOR | Apoptosis
作用靶点:SphK | PI3K | Apoptosis
In Vitro: SKI V has weak activity toward ERK2 (IC50 of 80 μM for hERK2) and does not inhibit PKC-α.
SKI V (10 μM; for 24 hours) inhibits cancer cell proliferation and induces apoptosis.
SKI V (0.2, 1, 5 μM; pretreated for 1 hour) decreases phospho-Akt and phospho-MEK levels. Near-confluent cultures of JC cells are serum-starved for 16 hours, followed by pretreatment SKI V for 1 hour.
SKI V has IC50s for inhibition of sphingosine kinase (SK) and tumor cell proliferation of ∼2 μM.
SKI V (20 μg/ml) inhibits not only purified but endogenous SK in in MDA-MB-231 cells.
SKI V (0.2, 1, 5 μM) inhibits intracellular S1P formation in JC cells in a dose-dependent fashion.
In Vivo: SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals.
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货号: HY-12895
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