2. PI3K/Akt/mTOR Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Akt Apoptosis Caspase PARP
  4. API-1

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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API-1

API-1 構造式

CAS 番号 : 36707-00-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 170 在庫あり
Solution
10 mM * 1 mL in DMSO USD 170 在庫あり
Solid
5 mg $155 在庫あり
10 mg $265 在庫あり
25 mg $490 在庫あり
50 mg $780 在庫あり
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Based on 1 publication(s) in Google Scholar

API-1 関連抗体

Top Publications Citing Use of Products

Akt アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Akt Akt1 Akt2 Akt3

Caspase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

PARP アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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製品説明

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[1][2][3].

IC50 & Target

Caspase-8

 

Caspase 3

 

Caspase-9

 

PARP

 

体外実験

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.

API-1 関連抗体

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.
体内実験

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.
分子量

337.29

分子式

C13H15N5O6
CAS 番号
Appearance

Solid

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
View the Complete Stock Solution Preparation Table

* 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.

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  • Dilution Calculator

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

一般には略語で表示されます：C1V1 = C2V2

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体内:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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参考文献

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

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

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

API-136707-00-3API1API 1AktApoptosisCaspasePARPPKBProtein kinase Bpoly ADP ribose polymeraseAkt/PKB inhibitorTRAILcancerNSCLCHNSCCH1299Inhibitorinhibitorinhibit

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