Cat. No.: HY-50862

Akt1/Akt2-IN-1

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC₅₀=3.5 nM) and Akt2 (IC₅₀=42 nM), with potent and balanced activity.

For research use only. We do not sell to patients.

Purity: 99.30%
CAS No.: 893422-47-4
Formula: C₃₃H₂₉N₇O
Molecular Weight:539.63

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Akt1/Akt2-IN-1 Chemical Structure

CAS No.: 893422-47-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC₅₀=3.5 nM) and Akt2 (IC₅₀=42 nM), with potent and balanced activity^[1].

IC₅₀ & Target^[1]

Akt1

3.5 nM (IC₅₀)

Akt2

42 nM (IC₅₀)

All Akt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	5610 nM Compound: 1	Inhibition of human ERG expressed in HEK cells by competitive radioligand binding assay Inhibition of human ERG expressed in HEK cells by competitive radioligand binding assay	[PMID: 19097777]

In Vitro

Consistent with the allosteric mode of inhibition, Akt1/Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC₅₀=1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1/Akt2-IN-1 has moderate activity in an hERG binding assay (IC₅₀=5610 nM) and is a substrate for human P-glycoprotein^[1].

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

In Vivo

Akt1/Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1/Akt2-IN-1 has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1/Akt2-IN-1 has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1/Akt2-IN-1 shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1/Akt2-IN-1, tolerability and Akt inhibition are assessed in mice. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1/Akt2-IN-1 is well tolerated in mice and shows high levels of Akt inhibition in mouse lung^[1].

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

Chemical Information

CAS No. 893422-47-4
Appearance Solid
Molecular Weight 539.63
Formula C₃₃H₂₉N₇O
Color White to off-white
SMILES

O=C(NC=C1)C2=C1N=C(C(C3=CC=CC=C3)=C2)C(C=C4)=CC=C4CN5CCC(CC5)C6=NNC(C7=NC=CC=C7)=N6
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Research (Wash D C)

Single-Cell RNA Sequencing Analysis Reveals the Role of Macrophage-Mediated CD44-AKT-CCL2 Pathways in Renal Tubule Injury during Calcium Oxalate Crystal Formation. [Abstract]

2025 May 6:8:0690. PMID: 40330661
Cell Mol Biol Lett

Feedback loop centered on MAF1 reduces blood-brain barrier damage in sepsis-associated encephalopathy. [Abstract]

2025 Jan 20;30(1):8. PMID: 39833662

Solvent & Solubility

In Vitro:

DMSO : ≥ 35 mg/mL (64.86 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8531 mL

9.2656 mL

18.5312 mL

5 mM

0.3706 mL

1.8531 mL

3.7062 mL

10 mM

0.1853 mL

0.9266 mL

1.8531 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Bilodeau MT, Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3178-82. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8531 mL	9.2656 mL	18.5312 mL	46.3280 mL
	5 mM	0.3706 mL	1.8531 mL	3.7062 mL	9.2656 mL
	10 mM	0.1853 mL	0.9266 mL	1.8531 mL	4.6328 mL
	15 mM	0.1235 mL	0.6177 mL	1.2354 mL	3.0885 mL
	20 mM	0.0927 mL	0.4633 mL	0.9266 mL	2.3164 mL
	25 mM	0.0741 mL	0.3706 mL	0.7412 mL	1.8531 mL
	30 mM	0.0618 mL	0.3089 mL	0.6177 mL	1.5443 mL
	40 mM	0.0463 mL	0.2316 mL	0.4633 mL	1.1582 mL
	50 mM	0.0371 mL	0.1853 mL	0.3706 mL	0.9266 mL
	60 mM	0.0309 mL	0.1544 mL	0.3089 mL	0.7721 mL

Keywords

Akt1/Akt2-IN-1

2 Cited Publications

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Akt1/Akt2-IN-1

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Publications Citing Use of MedChemExpress (MCE) Akt1/Akt2-IN-1

All Akt Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Akt1/Akt2-IN-1 Related Classifications

HY-50862 Related Classifications