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HomeProduct name listAPI-2

API-2

Synonym(s):TCN;API-2;MIHC;MYHL;MYO1A

API-2 Structural

What is API-2?

Chemical properties

Off-White Solid

The Uses of API-2

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.

The Uses of API-2

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.

What are the applications of Application

Triciribine is a tricyclic nucleoside that induces apoptosis and has antineoplastic and antiviral activity

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

Properties of API-2

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
pka 12.35±0.70(Predicted)
form  powder
color  tan

Safety information for API-2

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H317:Sensitisation, Skin
H319:Serious eye damage/eye irritation
Precautionary Statement Codes P280:Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for API-2

InChIKey HOGVTUZUJGHKPL-HTVVRFAVSA-N

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