API-1

SKU: orb1298484

Description

API-1 (NSC-177223) is a selective Akt inhibitor that promotes apoptosis by triggering GSK3β-dependent, β-TrCP/FBXW7-mediated degradation of the anti-apoptotic protein Mcl-1. This mechanism supports its application in cancer research, particularly for studying apoptosis resistance in vitro and evaluating therapeutic potential in vivo.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 36707-00-3
• MW: 337.29
• Purity: 99.07% (May vary between batches)
• Formula: C₁₃H₁₅N₅O₆
• SMILES: NC(=O)c1cn([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c2ncnc(N)c2c1=O
• Target: Akt
• Solubility: DMSO:22.5 mg/mL (66.71 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.93 mM)

Bioactivity

• In Vitro:
  API-1 rapidly and potently reduced the levels of Mcl-1 primarily in API-1-senstive lung cancer cell lines. Ectopic expression of Mcl-1 protected cells from induction of apoptosis by API-1. API-1 treatment decreased the half-life of Mcl-1, whereas inhibition of the proteasome with MG132 rescued Mcl-1 reduction induced by API-1. API-1 decreased Mcl-1 levels accompanied with a rapid increase in Mcl-1 phosphorylation (S159/T163). Moreover, inhibition of GSK3 inhibited Mcl-1 phosphorylation and reduction induced by API-1 and antagonized the effect of API-1 on induction of apoptosis.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, NSC 177223, NSC177223, NSC-177223, Inhibitor, Akt, Akt/PKB inhibitor, Apoptosis, API 1, API1, API-1, Protein kinase B, PKB, TRAIL

Compound Identifiers

PubChem CID

24773090