Enzymes for Research, Diagnostic and Industrial Use


Cat No.
A-443654 is a potent and selective inhibitor of Akt1 with Ki value of 160 pM.
Product Overview
A-443654 is a potent and selective inhibitor of Akt with Ki value of 160 pM. The Akt kinases play important roles in cellular signal transduction and take participate in the regulation of cell transformation and tumor progression. The activities of them are usually elevated in human malignancies. A-443654 is a pan inhibitor of Akt1, 2 and 3. It binds to the ATP-binding site of Akt and inhibits the kinase activity reversibly. A-443654 shows selectivity against Akt. The inhibition ability of it for Akt is much higher than that for other kinases. It is found that A-443654 can suppress the phosphorylation of the downstream proteins of Akt while increased the Ser473 and Thr308 phosphorylation of Akt. In murine FL5.12 cells stably transfected with human Akt1, 2 or 3, A-443654 inhibited the phosphorylation of GSK3 dose-dependently. A-443654 at a concentration of 0.6 μM inhibited Akt and induced G2/M accumulation in H1299 cells. In MiaPaCa-2 cells, treatment of A-443654 for 48 h resulted in a suppression of tumor proliferation with EC50 value of 100 nM. In chronic lymphocytic leukemia cells, A-443654 also inhibited the activity of Akt and induced apoptosis with EC50 value of 0.63 μM. Besides that, A-443654 was found to cause decreased phosphorylation of GSK3, FOXO3, TSC2 and mTOR in MiaPaCa-2 cells. It is also reported that A-443654 was effective in blocking the phosphorylation of 4EBP-1 and S6 protein in both T47D and LNCaP cells. A-443654 is not oral available. In mice model with human MiaPaCa-2 pancreatic cell xenograft, the administration of A-443654 at a dose of 7.5mg/kg/d significantly inhibited tumor growth. A-443654 also inhibited tumor growth in 3T3 murine fibroblast model expressing active Akt. When using the combination of A-443654 and rapamycin in mice model with MiaPaCa-2 pancreatic cancer xenograft, the administration showed more efficacy than each monotherapy
Molecular Weight
Store at -20°C
A 443654; A443654
160 pM (Ki)
Molecular Formula
Chemical Name
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
Download Datasheet:

Online Inquiry
*E-mail Address:
Country or Region:
*Products or Services of Interest:
Project Description:
Our Products Are Not Intended For Clinical Use.
*Verification Code:
Verification code

Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.

Sitemap | Privacy Policy | Terms and Conditions
Copyright ©2011 - 2021 Creative Enzymes.
Contact Us address-USA
Fax: fax
Distributors To view the contact information for a specific location, select the desired country or region:
Click unfold / close
Inquiry Basket
Delete selected Check Out
Decide to move out of the shopping cart??

Sure No, Back

Please choose product!

< Go Back
You have already added to buy this product