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PS210

Catalog No. T16670 CAS 1221962-86-2

PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1, without acting against 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.

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PS210, CAS 1221962-86-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 109.00
25 mg	In stock	$ 207.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 549.00
1 mL * 10 mM (in DMSO)	In stock	$ 77.00

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Purity: 99.65%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1, without acting against 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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/ml (157.77 mM)

References and Literature

1. Busschots K, et al. Substrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking site. Chem Biol. 2012 Sep 21;19(9):1152-63. 2. Rettenmaier TJ, et al. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1. Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):18590-5.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Ovarian Cancer Compound Library Oxidation-Reduction Compound Library Antidepressant Compound Library Anti-Breast Cancer Compound Library Glycolysis Compound Library Kinase Inhibitor Library Antioxidant Compound Library Metabolism Compound Library NO PAINS Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PS210 1221962-86-2 PI3K/Akt/mTOR signaling PDK pocket Arg131 Thr148 S6K PS423 PIF-binding PDK-1 PIFtide Inhibitor a-B Lys76 PS 210 helix PS-210 inhibit inhibitor

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