WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406398
Description: 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.
MedKoo Cat#: 406398
Chemical Formula: C13H15N5O6
Exact Mass: 337.10223
Molecular Weight: 337.29
Elemental Analysis: C, 46.29; H, 4.48; N, 20.76; O, 28.46
API-1, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Synonym: API1; API-1; API 1; NSC177233.
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
InChi Key: SPBWHPXCWJLQRU-FITJORAGSA-N
InChi Code: InChI=1S/C13H15N5O6/c14-10-6-7(20)4(11(15)23)1-18(12(6)17-3-16-10)13-9(22)8(21)5(2-19)24-13/h1,3,5,8-9,13,19,21-22H,2H2,(H2,15,23)(H2,14,16,17)/t5-,8-,9-,13-/m1/s1
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
The following data is based on the product molecular weight 337.29 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.