An Akt inhibitor that reduces the level of phosphorylated Akt (IC50 = ~0.8 µM); binds Akt and blocks its translocation to the cell membrane; reduces cell proliferation in cancer cell lines

API-1 – 1 mg

Brand:
Cayman
CAS:
36707-00-3
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

API-1 is an inhibitor of Akt that reduces the level of phosphorylated Akt (IC50 = ~0.8 µM in OVCAR3 cells) by binding to Akt and blocking its translocation to the cell membrane.{37133} It reduces cell proliferation in various cancer cell lines, induces apoptosis, and, at a dose of 10 mg/kg per day, decreases tumor growth in a mouse xenograft model. API-1 inhibition of Akt leads to proteasomal degradation of the downstream mediator Mcl-1.{37132} Likely independent of Akt binding, API-1 inhibits cell growth (IC50s = 2-5 µM) and induces apoptosis in non-small cell lung and head and neck squamous cancer (NSCLC and HNSCC) cell lines with concomitant increases in caspase-3, -8, and -9 cleavage.{37131} It reduces the levels of cellular FLICE-inhibitory protein (c-FLIP), an important regulator of apoptosis, through ubiquitin- and proteasome-mediated degradation. It also has a synergistic effect on apoptosis in combination with TRAIL/APO-2L. The information regarding the reduction in phosphorylated Akt levels, IC50 value, translocation, cell proliferation, and xenograft tumor growth was drawn from a paper that has been retracted; however, the information specified in the retraction statement has not been included.{37133}  

 

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Description

An Akt inhibitor that reduces the level of phosphorylated Akt (IC50 = ~0.8 µM); binds Akt and blocks its translocation to the cell membrane; reduces cell proliferation in cancer cell lines, induces apoptosis, and, at a dose of 10 mg/kg/day, decreases tumor growth in a mouse xenograft model; inhibits cell growth (IC50s = 2-5 µM) and induces apoptosis in NSCLC and HNSCC cell lines; increases cleavage of caspases 8, 9, and 3; reduces c-FLIP levels through ubiquitin/proteasome-mediated degradation; synergistically induces apoptosis in combination with TRAIL/APO-2L

Formal name: 4-amino-5,8-dihydro-5-oxo-8-β-D-ribofuranosyl-pyrido[2,3-d]pyrimidine-6-carboxamide

Synonyms:  NSC 177223

Molecular weight: 337.3

CAS: 36707-00-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PKB/Akt||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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