1. PI3K/Akt/mTOR
  2. Akt

Akt1 and Akt2-IN-1 

Cat. No.: HY-50862
Handling Instructions

Akt1 and Akt2-IN-1 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.
Akt1 and Akt2-IN-1 Chemical Structure

Akt1 and Akt2-IN-1 Chemical Structure

CAS No. : 893422-47-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO $416 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
50 mg $1500 In-stock
100 mg $2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

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Description

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity. IC50 value: 3.5 nM (Akt1), 42 nM (Akt2) Target: Akt in vitro: Akt1 and Akt2-IN-1 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 lM vs PKA, PKC, SGK). Akt1 and Akt2-IN-1 has moderate activity in an hERG binding assay (IC50 = 5610 nM) and is a substrate for human P-glycoprotein (MDR1 Directional Transport Ratio (B to A/A to B) = 17.6). Akt1 and Akt2-IN-1 also shows good physical properties with a human plasma protein binding of 97.3% and a logP = 3.51. in vivo: Akt1 and Akt2-IN-1 has potent inhibitory activity against Akt1 and Akt 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1 and 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.

References
Molecular Weight

539.63

Formula

C₃₃H₂₉N₇O

CAS No.

893422-47-4

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 35 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Akt1 and Akt2-IN-1
Cat. No.:
HY-50862
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