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PROTAC SGK3 degrader-1 SGK inhibitor

Cat.No.S9672

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.
PROTAC SGK3 degrader-1 SGK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 1157.38

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Quality Control

Batch: Purity: 99.78%
99.78

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (86.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 1157.38 Formula

C57H73FN10O11S2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2381320-35-8 -- Storage of Stock Solutions

Synonyms SGK3-PROTAC1 Smiles CC1=CC=C(F)C(=C1)[S](=O)(=O)NC2=CC=C(C=C2)C3=NC4=C(C=N[NH]4)C(=N3)OCC5CN(CCCCCCOCCOCCOCC(=O)NC(C(=O)N6CC(O)CC6C(=O)NCC7=CC=C(C=C7)C8=C(C)N=CS8)C(C)(C)C)CCO5

Mechanism of Action

Targets/IC50/Ki
SGK3
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.
References

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