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Catalog No. T14072   CAS 552325-16-3

A-443654 is a pan-Akt inhibitor. A-443654 has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).

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A-443654 Chemical Structure
A-443654, CAS 552325-16-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 84.00
5 mg In stock $ 198.00
10 mg In stock $ 322.00
25 mg In stock $ 597.00
50 mg In stock $ 913.00
100 mg In stock $ 1,370.00
200 mg In stock $ 1,850.00
500 mg In stock $ 2,730.00
1 mL * 10 mM (in DMSO) In stock $ 226.00
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Purity: 98.04%
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Biological Description
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Description A-443654 is a pan-Akt inhibitor. A-443654 has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
Targets&IC50 CK2:2.4 μM (ki), Chk1:2.3 μM (ki), cKIT:1.2 μM (ki), ERK2:340 nM (ki), Akt3:160 pM (ki), PKCδ:33 nM (ki), PKCγ:24 nM (ki), MAPK-AP2:3.3 μM (ki), KDR:3.1 μM (ki), PKA:6.3 nM (ki), CDK2:24 nM (ki), RSK2:11 nM (ki), Akt2:160 pM (ki), Src:2.6 μM (ki), Akt1:160 pM (ki), GSK3β:41 nM (ki)
In vitro A-443654 exhibits a Ki of 160 pM which is a 30,000-fold improvement in potency versus the initial lead molecule. A-443654 reduces the P-GSK3 in a dose-responsive manner in all three cell lines. A-443654 is 40-fold selective for Akt over PKA, and it inhibits Akt1, Akt2, or Akt3 equally within cells. A-443654-induced morphological changes occur very rapidly (within 2 to 4 h) in both 10A and 10CA1a cells, with 10CA1a cells more sensitive to A-443654 than the 10A cells. A-443654 inhibits the proliferation of tumor cells with EC50 of 0.1 μM[1]. A-443654 demonstrates the greatest selective effect on the mutant cells compared to the WT cells with greater than 3.5 fold relative growth inhibition of the mutant cells[3]. FACScan Analysis of rapamycin and A-443654 effects on DNA content in 10A and 10CA1a cells. In contrast, A-443654 at 2 and 5 μM decreases Bcl-2 levels by 30 to 40% in the 10CA1a cells at 8h. The combination of rapamycin with 2 or 5 μM A-443654, however, markedly decreases Bcl-2 protein levels by appr 40 to 50% in the 10A cells and by appr 70% in the 10CA1a cells, respectively. A-443654 alone at 2 μM causes the 10CA1a cells, but not the 10A cells, to detach from the plate after 12 h, whereas 1 μM of A-443654 causes 10CA1a cells to detach from the plate after 12 h [2].
In vivo A-443654 (7.5 mg/kg/d, s.c.) inhibits tumor growth in the 3T3-Akt1 flank tumor model. A-443654 (30 mg/kg, s.c.) caused increased levels of phosphorylated Akt1 in MiaPaCa-2 tumors. A-443654 (50 mg/kg, s.c.) induces apoptosis in 3T3-Akt1 flank tumors [1].
Molecular Weight 397.47
Formula C24H23N5O
CAS No. 552325-16-3


Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (251.59 mM)

TargetMolReferences and Literature

1. Luo Y, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther. 2005 Jun;4(6):977-86. 2. Zheng J, et al. Rapamycin sensitizes Akt inhibition in malignant human breast epithelial cells. Cancer Lett. 2010 Oct 1;296(1):74-87. 3. Gallia GL, et al. Inhibition of Akt inhibits growth of glioblastoma and glioblastoma stem-like cells. Mol Cancer Ther. 2009 Feb;8(2):386-93. 4. Zhao Y, et al. Estrogen receptor alpha and beta regulate actin polymerization and spatial memory through an SRC-1/mTORC2-dependent pathway in the hippocampus of female mice. J Steroid Biochem Mol Biol. 2017 Nov;174:96-113.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Metabolism Compound Library TGF-beta/Smad Compound Library Glutamine Metabolism Compound Library Epigenetics Compound Library PI3K-AKT-mTOR Compound Library HIF-1 Signaling Pathway Compound Library Neural Regeneration Compound Library Anti-Lung Cancer Compound Library Cell Cycle Compound Library Anti-Alzheimer's Disease Compound Library

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A-443654 552325-16-3 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling MAPK Metabolism PI3K/Akt/mTOR signaling Stem Cells Tyrosine Kinase/Adaptors Akt CDK Chk PKA Src PKC S6 Kinase Casein Kinase FLT GSK-3 VEGFR ERK A443654 inhibit A 443654 Inhibitor PKB Protein kinase B inhibitor