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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

CAY10567

Cayman Chemical Item Number 10010233

BML-257 (CAS 32387-96-5)

CAY10567 (CAS 32387-96-5)

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Description

Akt1, 2, and 3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival.1,2 Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. CAY10567 is an Akt1 translocation inhibitor. At a concentration of 12.5 µM, it prevents the translocation of Akt1 by apparently compromising the function of the PH domain. A structurally similar compound inhibits kinase activity in vitro with an EC50 value of 12 µM by binding to the kinase domain.3 CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 µM. 4

1 Vivanco, I., and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nat Rev Cancer 2 489-501 (2002).

2 Hennessy, B.T., Smith, D.L., Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nat Rev Drug Discov 4 988-1004 (2005).

3 Lundholt, B.K., Linde, V., Loechel, F., et al. Identification of Akt pathway inhibitors using redistribution screening on the FLIPR and the IN cell 3000 analyzer. J Biomol Screen 10(1) 20-29 (2005).

4 Rong, F., Chow, S., Yan, S., et al. Structure-activity relationship (SAR) studies of quinoxalines as novel HCV NS5B RNA-dependent RNA polymerase inhibitors. Bioorg Med Chem Lett 17 1663-1666 (2007).

Synonyms
  • BML-257
Formal Name 2,​3-​diphenyl-​6-​quinoxalinecarboxylic acid
CAS Number 32387-96-5
Molecular Formula C21H14N2O2
Formula Weight 326.4
Formulation A crystalline solid
Purity >98%
λmax 249, 351 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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OC(=O)​c1ccc2nc(c3ccccc3)​c(nc2c1)​c1ccccc1

Background Reading

Vivanco, I., and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nat Rev Cancer 2 489-501 (2002).

Hennessy, B.T., Smith, D.L., Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nat Rev Drug Discov 4 988-1004 (2005).

Rong, F., Chow, S., Yan, S., et al. Structure-activity relationship (SAR) studies of quinoxalines as novel HCV NS5B RNA-dependent RNA polymerase inhibitors. Bioorg Med Chem Lett 17 1663-1666 (2007).

Lundholt, B.K., Linde, V., Loechel, F., et al. Identification of Akt pathway inhibitors using redistribution screening on the FLIPR and the IN cell 3000 analyzer. J Biomol Screen 10(1) 20-29 (2005).

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Size Price Quantity Subtotal
100 mg $21.00 $0.00
250 mg $50.00 $0.00
500 mg $95.00 $0.00
1 g $160.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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