PROTAC SGK3 degrader-1

For research use only.

Catalog No.S9672 Synonyms: SGK3-PROTAC1

PROTAC SGK3 degrader-1 Chemical Structure

CAS No. 2381320-35-8

PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3 (Serum/Glucocorticoid Regulated Kinase Family Member 3) for degradation.

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Biological Activity

Description PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3 (Serum/Glucocorticoid Regulated Kinase Family Member 3) for degradation.
Targets
SGK3 [1]
()
In vitro

SGK3-PROTAC1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 h, with maximal 80% degradation observed within 8 h, accompanied by a loss of phosphorylation of NDRG1, an SGK3 substrate. Low doses of SGK3-PROTAC1 (0.1−0.3 μM) restores sensitivity of SGK3 dependent ZR-75-1 and CAMA-1 breast cancer cells to Akt and PI3K inhibitors, whereas the cis epimer analogue incapable of binding to the VHL E3 ligase has no impact. SGK3-PROTAC1 suppresses proliferation of ZR-75-1 and CAMA-1 cancer cell lines treated with a PI3K inhibitor more effectively than could be achieved by a conventional SGK isoform inhibitor.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: CAMA-1, HEK293 cells
  • Concentrations: 0.3 μM
  • Incubation Time: 8 h
  • Method:

    Cells are treated with DMSO (control), SGK3-PROTAC1 (0.3 μM), or cisSGK3-PROTAC1 (0.3 μM) for 8 h and lysed. Lysates are subjected to immunoblot analysis with the indicated antibodies.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (86.4 mM)
Water Insoluble
Ethanol '''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1157.38
Formula

C57H73FN10O11S2

CAS No. 2381320-35-8
Storage powder
in solvent
Synonyms SGK3-PROTAC1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID