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抑制剂/激活剂

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凋亡与自噬

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Triciribine API-2; NSC 154020; TCN

Triciribine 是一种 DNA 合成 (DNA synthesis) 抑制剂，也抑制 Akt 和 HIV-1/2，IC50 分别为 130 nM 和 0.02-0.46 μM。

货号：
TK0416
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	35943-35-2
生物活性	Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively.
分子式	C13H16N6O4
分子量	320.30
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 100 mg/mL (312.21 mM; Need ultrasonic)
体内研究	Triciribine (TCBN) treatment, administered for 7 days after 14 days of hypoxia until 21 days of hypoxia is reached, reversed the vascular thickening as shown by immunohistochemistry and Western analyses. On the other hand, Rapamycin treatment did not prevent hypoxia-induced pulmonary alveolar haemorrhage and congestion. Triciribine partially inhibits progressive pruning of the vasculature.
体外研究	The nucleoside analog Triciribine (TCN) is a purine analog which is initially shown to inhibit DNA synthesis. Triciribine selectively inhibits the phosphorylation and activation of all three Akt isoforms. At a concentration of 10 μM Triciribine Akt phosphorylation is inhibited at both Thr308 and Ser473. Triciribine effectively inhibits the phosphorylation and consequently the catalytic activity of Akt in PC-3 cells. The Akt inhibitor Triciribine (TCN) does not effectively inhibit the human cell line U87MG but inhibits other astrocytoma cell lines in a grade-dependent manner. The WHO II K1861-10 line is incompletely inhibited (69% maximum inhibition) with a GI50 value of 1.7 µM for Triciribine. Triciribine exhibits maximum growth inhibition around 1-10 µM and inhibits phosphorylation of Akt, as well as downstream p70S6K, to basal levels at 100 µM (IC50=130 nM) in KR158 cells. Triciribine (TCN) is a novel tricyclic compound with known antitumor activity. Using a syncytial plaque assay, Triciribine is active against HIV-1 at 0.01-0.02 μM. Using a microtiter XTT assay, Triciribine is active against a panel of HIV-1 and HIV-2 strains at IC50 values ranging from 0.02 to 0.46 μM.
文献	•Science. 2017 Dec 1;358(6367):eaan4368. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Oncoimmunology. 2018 Aug 6;7(10):e1488565. •Stem Cell Res Ther. 2018 Mar 1;9(1):52. •Oxid Med Cell Longev. 2021 Mar 30. •Front Pharmacol. 2019 May 31;10:603. •J Cell Mol Med. 2021 May 5. •J Cell Mol Med. 2021 Jan 6. •Int J Antimicrob Agents. 2019 Dec;54(6):814-819. •J Mol Med (Berl). 2019 Aug;97(8):1183-1193. •Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290. •Med Sci Monit. 2019 Dec 30;25:10154-10163. •J Cardiovasc Pharmacol. 2019 Aug;74(2):152-161. •Department of Laboratory Medicine, Laboratory of Hematology of the Radboudumc and Radboud Institute for Molecular Life Sciences in Nijmegen, The Netherlands.2019 Oct.
纯度及产品资料	98%

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