Description
PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
Product information
CAS Number: 1221962-86-2
Molecular Weight: 380.31
Formula: C19H15F3O5
Chemical Name: 2-{3-oxo-1-phenyl-3-[4-(trifluoromethyl)phenyl]propyl}propanedioic acid
Smiles: OC(=O)C(C(CC(=O)C1C=CC(=CC=1)C(F)(F)F)C1C=CC=CC=1)C(O)=O
InChiKey: MLJPLHGJBUWCBA-UHFFFAOYSA-N
InChi: InChI=1S/C19H15F3O5/c20-19(21,22)13-8-6-12(7-9-13)15(23)10-14(11-4-2-1-3-5-11)16(17(24)25)18(26)27/h1-9,14,16H,10H2,(H,24,25)(H,26,27)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (262.94 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
When PS210 induces a stabilization of PDK1 to the temperature gradien, PS210 stabilized the residue Arg131, located opposite to the helix a-B at the other extreme of the helix a-C. Thus, 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.
Products are for research use only. Not for human use.
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