MedKoo Cat#: 406398 | Name: API-1
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

API-1
API-1
CAS#36707-00-3

Theoretical Analysis

MedKoo Cat#: 406398

Name: API-1

CAS#: 36707-00-3

Chemical Formula: C13H15N5O6

Exact Mass: 337.1022

Molecular Weight: 337.29

Elemental Analysis: C, 46.29; H, 4.48; N, 20.76; O, 28.46

Price and Availability

Size Price Availability Quantity
25mg USD 550.00 2 Weeks
100mg USD 1,650.00 2 Weeks
1g USD 4,950.00 2 Weeks
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Related CAS #
No Data
Synonym
API1; API-1; API 1; NSC177223; NSC 177223; NSC-177223
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
Appearance
white solid powder
Purity
>95% (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).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
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Preparing Stock Solutions

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.

Recalculate based on batch purity %
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.