Apoptosis
Telomerase
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Product name : BX 912
Item : cc391
Price : 200mg, $950;500mg, $1650; 1g $2450; 2g, $3650
contact : Send inquiry to: info@acesobio.com,or by fax to: 1-845-673-1239.
CAS : 702674-56-4
Molecular Weight : 471.35
Formula : C₂₀H₂₃BrN₈O
Storage : at -20°C
Additional information : We offer significant discount for larger quantity order
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BX912 prevents ChcK1, PKA, c-kit, and KDR with IC50 of 0.83, 0.11, 0.85, and 0.41 μM, resepectively. BX912 blocks PDK1/Akt signaling in tumor cells and suppresses the anchorage-dependent growth of a variety of tumor cell lines (such as PC-3 cells ) in culture or induces apoptosis. A number of cancer cell lines (such as MDA-468 breast cancer) with elevated Akt activity are >30-fold more sensitive to growth inhibition by PDK1 inhibitor BX912 in soft agar than on tissue culture plastic, consistent with the cell survival function of the PDK1/Akt signaling pathway, which is particularly important for unattached cells. BX912 potently blocks PDK1 enzyme activity in a direct kinase assay format, although BX912 fails to block preactivated AKT2 activity (IC50 > 10 μM). Therefore, BX-912 is a direct inhibitor of PDK1. BX912 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP, suggesting that BX912 binds to the ATP binding pocket of PDK1. [1][2]
Reference:
[1] J Biol. Chem. 2006, 280, 19867-19874.
[2] Proc. Natl. Acad. Sci. USA. 2011, 108, 272-277.
Chemical Information
PLEASE KEEP THE PRODUCT UNDER -20℃ FOR LONG-TERM STORAGE.
NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
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