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Triciribine

Catalog No. T6065 CAS 35943-35-2

Synonyms: VD-0002, Tricyclic nucleoside, NSC 154020, API-2, TCN

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Triciribine, CAS 35943-35-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 52.00
5 mg	In stock	$ 85.00
10 mg	In stock	$ 137.00
25 mg	In stock	$ 249.00
50 mg	In stock	$ 415.00
100 mg	In stock	$ 619.00
1 mL * 10 mM (in DMSO)	In stock	$ 94.00

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Purity: 100%

Purity: 99.87%

Biological Description

Chemical Properties

Storage & Solubility Information

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)

Synonyms	VD-0002, Tricyclic nucleoside, NSC 154020, API-2, TCN
Molecular Weight	320.3
Formula	C13H16N6O4
CAS No.	35943-35-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

1eq. HCl: 32 mg/mL (100 mM)

DMSO: 32 mg/mL (100 mM)

References and Literature

1. Gursel DB, et al, Nero Oncol, 2011, 13(6), 610-621. 2. Kucera LS, et al, AIDS Res Hum Retroviruses, 1993, 9(4), 307-314. 3. Dieterle A, et al, Int J Cancer , 2009, 125(4), 932-941. 4. Yang L, et al, Cancer Res, 2004, 64(13), 4394-4399.

Citations

1. Wang G, Xu J, Ma H, et al. Phenolipid JE improves metabolic profile and inhibits gluconeogenesis via modulating AKT-mediated insulin signaling in STZ-induced diabetic mice. Pharmacological Research. 2022: 106569.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Angiogenesis related Compound Library Anti-Colorectal Cancer Compound Library Neural Regeneration Compound Library Antidepressant Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

Triciribine 35943-35-2 Cell Cycle/Checkpoint Cytoskeletal Signaling DNA Damage/DNA Repair Microbiology/Virology PI3K/Akt/mTOR signaling Proteases/Proteasome HIV Protease Akt DNA/RNA Synthesis Inhibitor HIV VD0002 inhibit VD-0002 PKB Protein kinase B Tricyclic nucleoside NSC 154020 NSC-154020 API-2 NSC154020 Human immunodeficiency virus VD 0002 API2 API 2 TCN inhibitor

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