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A-443654

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, CAS 552325-16-3

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Purity: 98%

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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	ERK2:340 nM (ki), cKIT:1.2 μM (ki), Chk1:2.3 μM (ki), CK2:2.4 μM (ki), MAPK-AP2:3.3 μM (ki), KDR:3.1 μM (ki), PKA:6.3 nM (ki), PKCδ:33 nM (ki), Akt3:160 pM (ki), PKCγ:24 nM (ki), Src:2.6 μM (ki), RSK2:11 nM (ki), Akt2:160 pM (ki), CDK2:24 nM (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

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 100 mg/mL (251.59 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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.

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Keywords

A-443654 T4444 MAPK信号通路 PI3K/Akt/mTOR信号通路表观遗传代谢蛋白酪氨酸激酶干细胞细胞骨架细胞周期血管生成 Akt Casein Kinase CDK Chk ERK FLT GSK-3 MAPK PKA PKC S6 Kinase Src VEGFR inhibit A443654 Inhibitor PKB A 443654 Protein kinase B inhibitor

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