API-2 Chemical Properties

Melting point:

207 °C (decomp)

Boiling point:

459.21°C (rough estimate)

Density 

1.2633 (rough estimate)

refractive index 

1.7000 (estimate)

storage temp. 

Store at RT

solubility 

DMSO: >10mg/mL

form 

powder

pka

12.35±0.70(Predicted)

color 

tan

InChIKey

HOGVTUZUJGHKPL-HTVVRFAVSA-N

Safety Information

WGK Germany 

3

RTECS 

RY8455000

API-2 Usage And Synthesis

Chemical Properties

Off-White Solid

Uses

Triciribine is an antitumor tricyclic nucleoside. Triciribine acts as a potent, small-molecule inhibitor of AKT phosphorylation in subjects with solid tumors contining activated AKT. Triciribine is al so a selective inhibitor of HIV-1 and HIV-2, including strains known to be resistant to AZT or TIBO.

Uses

Triciribine is an antitumor tricyclic nucleoside. Triciribine acts as a potent, small-molecule inhibitor of AKT phosphorylation in subjects with solid tumors contining activated AKT. Triciribine is also a selective inhibitor of HIV-1 and HIV-2, including strains known to be resistant to AZT or TIBO.

Uses

Triciribine hydrate has been used to study the effect of diethyldithiocarbamate (DDC) on matrix metalloproteinase-1 (MMP-1) in hepatic stellate cells¹. It has also been used to analyze ADAM 10 activation by (-)-epigallocatechin-3-gallate (EGCG) in N2a cells overexpressing Swedish mutant APP (SweAPP N2a cells)².

Definition

ChEBI: Triciribine is a nucleoside analogue in which the nucleobase portion is a 1,4,5,6,8-pentaazaacenaphthylene ring system substituted with an amino group at position 3, and a methyl group at position 5 and is bound to the beta-D-ribofuranosyl moiety by an N(1)-glycosidic linkage. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor.

Biological Activity

Selective inhibitor of Akt (protein kinase B) signaling; displays minimal inhibition of PKC, PKA, SGK and p38 pathways. Inhibits phosphorylation and activation of downstream targets of Akt including Bad, GSK-3 β and AFX. In vitro, induces apoptosis and growth arrest preferentially in human cancer cells with elevated levels of Akt. In mice, potently and selectively inhibits growth of Akt-overexpressing tumors. Inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2.

Biochem/physiol Actions

Triciribine is a highly selective Akt/PKB inhibitor, that selectively inhibits the cellular phosphorylation/activation of Akt1/2/3.

storage

Store at RT

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