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Triciribine

🥰Excellent
Catalog No. T6065Cas No. 35943-35-2
Alias VD-0002, Tricyclic nucleoside, TCN, NSC 154020, API-2

Triciribine (NSC-154020) is a DNA synthesis inhibitor, and it also inhibits Akt and HIV-1/2.

Triciribine

Triciribine

🥰Excellent
Purity: 100%
Catalog No. T6065Alias VD-0002, Tricyclic nucleoside, TCN, NSC 154020, API-2Cas No. 35943-35-2
Triciribine (NSC-154020) is a DNA synthesis inhibitor, and it also inhibits Akt and HIV-1/2.
Pack SizePriceAvailabilityQuantity
1 mg$36In Stock
2 mg$52In Stock
5 mg$85In Stock
10 mg$137In Stock
25 mg$249In Stock
50 mg$415In Stock
100 mg$619In Stock
1 mL x 10 mM (in DMSO)$94In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
Triciribine (NSC-154020) is a DNA synthesis inhibitor, and it also inhibits Akt and HIV-1/2.
Targets&IC50
HIV-1:20 nM, Akt:130 nM
In vitro
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). Triciribine shows particular promise for inhibiting growth in Nf1 and Trp53 mutant astrocytoma cells in a grade-dependent manner. The WHO II K1861-10 line is inhibited, incompletely (69% maximum inhibition), with a GI50 value of 1.7 μM for Triciribine, whereas higher-grade tumor lines (KR158, KR130, and SF295) are inhibited to a greater extent (>80% maximum inhibition) at lower GI50 values (0.4–1.1 mM). Importantly, Triciribine is much less effective at inhibiting primary astrocytes (GI5013.6 mM), suggesting that this inhibitor may show specificity for tumor cells. [1] Triciribine inihibits HIV-1with an IC50 of 20 nM. Greater than 90% inhibition is achieved at 0.1 μM and complete inhibition of syncytia formation is achieved at 5 μM. Associated cell toxicity in the same cell line for Triciribine is 46 μM, resulting in selectivity indices of 2250. Triciribine markedly inhibits HIV-1-induced p24 core antigen production, reverse transcriptase, and infectious virus production in a dose-dependent manner using HIV-1 acutedly infected CEM-SS, H9, and persistently infected H9III B and U1 cells. [2] Triciribine inhibits Akt phosphorylation at Thr308 and Ser473 and Akt activity in the human prostate cancer cell line PC-3. Triciribine sensitizes PC-3 cells to TRAIL- and anti-CD95-induced apoptosis, whereas the cells remain resistant to DNA damaging chemotherapeutics. [3] Triciribine is highly selective for Akt and does not inhibit the activation of phosphatidylinositol 3-kinase, phosphoinositide-dependent kinase-1, protein kinase C, serum and glucocorticoid-inducible kinase, protein kinase A, signal transducer and activators of transcription 3, extracellular signal-regulated kinase-1/2, or c-Jun NH2-terminal kinase. [4]
In vivo
1 mg/kg/day i.p. treated Triciribine inhibits OVCAR3, OVCAR8 and PANC1 tumor growth, which overexpressing Akt, by 90%, 88% and 80% in nude mice, respectively. However, Triciribine has little effect on the growth of OVCAR5 and COLO357 cells. [4]
Kinase Assay
Akt Phosphorylation Changes Assay: Cells are grown to 80%–90% confluency and stimulated for 5–10 minutes with 1–10 ng/mL of epidermal growth factor or platelet derived growth factor (PDGF)–AA with or without 10–20 mM of U0126 or LY-294002. Protein lysates (5–20 μg) are separated by 12%–15% SDS PAGE and analyzed by Western blot for Akt, phosphorylated Akt (phospho-Ser 473), MAPK, and phosphorylated MAPK (p44/42 phospho-Thr202/Tyr204) antibodies (1:1000).
Cell Research
Triciribine is evaluated for cytotoxicity by seeding CEM-SS cells at a density of 1 × 104 cells/well in growth medium, using a 96-well flat-bottom plate. Serial fivefold dilutions of Triciribine are prepared in growth medium and added to the wells as a second overlay. After a 48-hours incubation at 37 °C, the cells are pulse labeled with [3H]dThd (1 μCi per well, specific activity 20 Ci/mmol) for 6 hours and the cells are harvested to measure total DNA synthesis.(Only for Reference)
AliasVD-0002, Tricyclic nucleoside, TCN, NSC 154020, API-2
Chemical Properties
Molecular Weight320.3
FormulaC13H16N6O4
Cas No.35943-35-2
SmilesCn1nc(N)c2cn([C@@H]3C[C@H](CO)[C@@H](O)[C@H]3O)c3ncnc1c23
Relative Density.1.2633 g/cm3 (Estimated)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
1eq. HCl: 32 mg/mL (100 mM)
DMSO: 32 mg/mL (100 mM)
Solution Preparation Table
1eq. HCl/DMSO
1mg5mg10mg50mg
1 mM3.1221 mL15.6104 mL31.2207 mL156.1037 mL
5 mM0.6244 mL3.1221 mL6.2441 mL31.2207 mL
10 mM0.3122 mL1.5610 mL3.1221 mL15.6104 mL
20 mM0.1561 mL0.7805 mL1.5610 mL7.8052 mL
50 mM0.0624 mL0.3122 mL0.6244 mL3.1221 mL
100 mM0.0312 mL0.1561 mL0.3122 mL1.5610 mL

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