API-1
API-1 is a potent Akt inhibitor, which induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis . 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.
1: Ren H, Koo J, Guan B, Yue P, Deng X, Chen M, Khuri FR, Sun SY. The E3 ubiquitin ligases β-TrCP and FBXW7 cooperatively mediates GSK3-dependent Mcl-1 degradation induced by the Akt inhibitor API-1, resulting in apoptosis. Mol Cancer. 2013 Nov 22;12:146. doi: 10.1186/1476-4598-12-146. PubMed PMID: 24261825.
2: Li B, Ren H, Yue P, Chen M, Khuri FR, Sun SY. The novel Akt inhibitor API-1 induces c-FLIP degradation and synergizes with TRAIL to augment apoptosis independent of Akt inhibition. Cancer Prev Res (Phila). 2012 Apr;5(4):612-20. doi: 10.1158/1940-6207.CAPR-11-0548. Epub 2012 Feb 16. PubMed PMID: 22345097; PubMed Central PMCID: PMC3324640.
2: Li B, Ren H, Yue P, Chen M, Khuri FR, Sun SY. The novel Akt inhibitor API-1 induces c-FLIP degradation and synergizes with TRAIL to augment apoptosis independent of Akt inhibition. Cancer Prev Res (Phila). 2012 Apr;5(4):612-20. doi: 10.1158/1940-6207.CAPR-11-0548. Epub 2012 Feb 16. PubMed PMID: 22345097; PubMed Central PMCID: PMC3324640.
| Chemical | |
|---|---|
| CAS Num | 36707-00-3 |
| Chemical Formula | C13H15N5O6 |
| Molecular Weight | 337.29 |
| IUPAC Chemical Name | 4-amino-8-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide |
| Exact Mass | 337.10223 |
| Elemental Analysis | C, 46.29; H, 4.48; N, 20.76; O, 28.46 |
| Synonym | API1; API-1; API 1; NSC177233. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(C1=CN([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)C3=NC=NC(N)=C3C1=O)N |
| Biological | |
| Targets and Effects | AKT inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | white solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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