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PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1 without affecting other protein kinases such as S6K, PKB/Akt, or GSK3. Its prodrug, PS423, serves as a substrate-selective inhibitor of PDK1 in cells, inhibiting the phosphorylation and activation of S6K.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
2 mg | $44 | In Stock | |
5 mg | $68 | In Stock | |
10 mg | $109 | In Stock | |
25 mg | $207 | In Stock | |
50 mg | $369 | In Stock | |
100 mg | $549 | In Stock | |
1 mL x 10 mM (in DMSO) | $77 | In Stock |
Description | PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1 without affecting other protein kinases such as S6K, PKB/Akt, or GSK3. Its prodrug, PS423, serves as a substrate-selective inhibitor of PDK1 in cells, inhibiting the phosphorylation and activation of S6K. |
Targets&IC50 | PDK1:(kd)3 μM |
In vitro | PS210 stabilized the residue Arg131 when PS210 causes stabilization of PDK1 to the temperature gradient, located opposite to the helix a-B at the other extreme of the helix a-C. So, the residues forming part of the phosphate-binding site appear to be a fixed point that allows for the relative movement of the helices in the process of PDK1 activation[1]. |
Molecular Weight | 380.31 |
Formula | C19H15F3O5 |
Cas No. | 1221962-86-2 |
Smiles | OC(=O)C(C(CC(=O)c1ccc(cc1)C(F)(F)F)c1ccccc1)C(O)=O |
Relative Density. | 1.400 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/ml (157.77 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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