Cat. No.: HY-110077

API-1

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API-1 is a potent selective Akt/PKB inhibitor that reduces the level of phosphorylated Akt (IC₅₀ = 0.8 μM). API-1 binds to the PH domain and inhibits Akt membrane translocation. API-1 induces c-FLIP degradation. API-1 reduces cell proliferation and induces apoptosis. API-1 decreases tumor growth in mouse xenograft model.

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Pureté: 99.62%
CAS No.: 36707-00-3
Formule: C₁₃H₁₅N₅O₆
Masse moléculaire:337.29

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

API-1 Chemical Structure

CAS No.: 36707-00-3

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Caspase-8

Caspase 3

Caspase-9

PARP

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In Vitro

API-1 (0.625-10 μM, 3 d) effectively inhibits the growth of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) cell lines^[1].
API-1 (5-10 μM, 24 h) effectively induces apoptosis in API-1-sensitive NSCLC and HNSCC cell lines^[1].
API-1 (1.25-5 μM, 24 h) synergizes with factor-related apoptosis-inducing ligand (TRAIL) to induce apoptosis in H1229 and 22A^[1].
API-1 (0.625-10 μM, 2-24 h) reduces the levels of c-FLIP (through facilitating ubiquitin/proteasome-mediated degradation) without increasing the expression of DR4 or DR5 in NSCLC and HNSCC cells^[1].
API-1 (0.625-10 μM, 2-24 h) inhibits the phosphorylation of Akt in NSCLC and HNSCC cells^[1].
API-1 (0.5-20 μM, 12-72 h) induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis in NSCLC cell lines^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

Human non-small cell lung cancer (NSCLC) cell lines (H157, Calu-1 and H1299) and head and neck squamous cell carcinoma (HNSCC) cell lines (22A, Tr146 and SqCC/Y1)
Concentration:

0.625, 1.25, 2.5, 5, 10 μM
Incubation Time:

3 d
Result:

Effectively inhibited the growth of 5 (H1299, H157, SqCC/Y1, 22A and Tr146) of 6 tested cancer cell lines.
The effective concentrations that decreased cell numbers by 50% (IC₅₀s) ranged between 2 and 5 μM for these sensitive cell lines.

Apoptosis Analysis^[1]

Cell Line:

H1299, Calu-1, SqCC/Y1
Concentration:

5, 10 μM
Incubation Time:

24 h
Result:

Dose-dependently increased annexin V-positive (or apoptotic) cells in H1299 and SqCC/Y1 cells (> 40% at 10 μM), but did so only minimally in Calu-1 cells (< 15% at 10 μM).
Dose-dependent increased cleavage of caspase-8, caspase-9, caspase-3 and PARP in H1299 and SqCC/Y1 cells, but this was not apparent in Calu-1 cells.

Apoptosis Analysis^[1]

Cell Line:

H1299, H157, Calu-1, SqCC/Y1, 22A, Tr146
Concentration:

1,25, 2.5, 5 μM; 5 μM (H1299, 22A)
Incubation Time:

24 h
Result:

Combination (5 or 2.5 μM) with TRAIL (25 to 100 ng/ml) was much more effective than either agent alone in decreasing the survival of the tested NSCLC and HNSCC cell lines, except for Calu-1 cells.
The CIs for these combinations were < 1.
Combination with TRAIL was much more potent than used alone in increasing cleavage of caspase-8, caspase-9, caspase-3 and PARP in H1229 and 22A.
Increased the proportion of annexin Vpositive cells in H1229 and 22A.

Western Blot Analysis^[1]

Cell Line:

H1299, H157, Calu-1, SqCC/Y1, 22A, Tr146
Concentration:

5 μM; 0.625, 1.25, 2.5, 5, 10 μM (H157)
Incubation Time:

24 h; 12 h (H157 with different concentrations); 2, 4, 8, 12, 16 h (H157 with concentration of 5 μM)
Result:

Reduced the levels of c-FLIP in H157, H1299, SqCC/Y1 and Tr146 cells, but not in Calu-1 cells at 5 μM.
Did not increase the expression of either DR5 or DR4 in any of the cell lines.
Reduced the levels of DR4 in some cell lines (H1299, SqCC/Y1 and Tr146).
Showed dose-course and time-course studies of the effects on the levels of c-FLIP, DR4 and DR5 in H157 cells.
The apparent reduction of c-FLIP in cells occurred after 4 h exposure.

In Vivo

API-1 (10 mg/kg; i.p.; daily for 6-8 weeks) selectively inhibits the growth of tumors with hyperactivated Akt in OVCAR3 and PANC-1 xenograft mice model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

8-week-old female nude mice (implanted tumors with hyperactivated Akt (OVCAR3 and PANC-1) into the left flank and those tumors that express low levels of activated Akt (OVCAR5 and COLO357) into the right flank)^[3]
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection (i.p.); daily for 6-8 weeks
Result:

Inhibited OVCAR3 and PANC1 tumor growth by 70 and 50%, respectively.
Had little effect on the growth of OVCAR5 and COLO357 cells in nude mice.
Had no effects on blood glucose level, body weight, activity, and food intake of mice.
Phosphorylation levels of Akt were reduced about 70% without a change of total Akt content.

Chemical Information

CAS No. 36707-00-3
Appearance Solid
Masse moléculaire 337.29
Formule C₁₃H₁₅N₅O₆
Color White to off-white
SMILES

O[C@H]1[C@@H](O[C@H](CO)[C@H]1O)N2C3=NC=NC(N)=C3C(C(C(N)=O)=C2)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Adv Sci (Weinh)

CpG-Based Nanovaccines Enhance Ovarian Cancer Immune Response by Gbp2-Mediated Remodeling of Tumor-Associated Macrophages. [Abstract]

2025 Apr;12(15):e2412881. PMID: 39985265

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (148.24 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9648 mL

14.8240 mL

29.6481 mL

5 mM

0.5930 mL

2.9648 mL

5.9296 mL

10 mM

0.2965 mL

1.4824 mL

2.9648 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (291 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Li B, et al. 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.

[2]. Ren H, et al. 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.

[3]. Kim D, et al. A small molecule inhibits Akt through direct binding to Akt and preventing Akt membrane translocation. J Biol Chem. 2010 Mar 12;285(11):8383-94. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9648 mL	14.8240 mL	29.6481 mL	74.1202 mL
	5 mM	0.5930 mL	2.9648 mL	5.9296 mL	14.8240 mL
	10 mM	0.2965 mL	1.4824 mL	2.9648 mL	7.4120 mL
	15 mM	0.1977 mL	0.9883 mL	1.9765 mL	4.9413 mL
	20 mM	0.1482 mL	0.7412 mL	1.4824 mL	3.7060 mL
	25 mM	0.1186 mL	0.5930 mL	1.1859 mL	2.9648 mL
	30 mM	0.0988 mL	0.4941 mL	0.9883 mL	2.4707 mL
	40 mM	0.0741 mL	0.3706 mL	0.7412 mL	1.8530 mL
	50 mM	0.0593 mL	0.2965 mL	0.5930 mL	1.4824 mL
	60 mM	0.0494 mL	0.2471 mL	0.4941 mL	1.2353 mL
	80 mM	0.0371 mL	0.1853 mL	0.3706 mL	0.9265 mL
	100 mM	0.0296 mL	0.1482 mL	0.2965 mL	0.7412 mL

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API-1

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Cell Cycle/DNA Damage Compound Library

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Publications Citing Use of MedChemExpress (MCE) API-1

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform Caspase

Voir tous les produits spécifiques à Isoform PARP

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

API-1 Related Classifications

HY-110077 Related Classifications