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PROTAC SGK3 degrader-2

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Catalog No. T212560Cas No. 2381196-78-5

PROTACSGK3degrader-2 is the cis-diastereomer of PROTACSGK3degrader-1 (SGK3-PROTAC1), featuring a cis-hydroxy group in its VH032 section, which prevents binding to the VHL E3 ligase. This compound inhibits SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but does not degrade SGK3. It serves as a control compound for studying the specific degradation effects mediated by SGK3-PROTAC1.

PROTAC SGK3 degrader-2

PROTAC SGK3 degrader-2

😃Good
Catalog No. T212560Cas No. 2381196-78-5
PROTACSGK3degrader-2 is the cis-diastereomer of PROTACSGK3degrader-1 (SGK3-PROTAC1), featuring a cis-hydroxy group in its VH032 section, which prevents binding to the VHL E3 ligase. This compound inhibits SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but does not degrade SGK3. It serves as a control compound for studying the specific degradation effects mediated by SGK3-PROTAC1.
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
PROTACSGK3degrader-2 is the cis-diastereomer of PROTACSGK3degrader-1 (SGK3-PROTAC1), featuring a cis-hydroxy group in its VH032 section, which prevents binding to the VHL E3 ligase. This compound inhibits SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but does not degrade SGK3. It serves as a control compound for studying the specific degradation effects mediated by SGK3-PROTAC1.
Targets&IC50
SGK1:1.4 μM
In vitro
PROTAC SGK3 degrader-2 (cisSGK3-PROTAC1) at concentrations of 0.03-3 μM over 8 hours does not induce degradation of SGK3 in HEK293, CAMA-1, ZR-75-1, and JIMT-1 cells; it only reduces phosphorylation of NDRG1 in HEK293 cells at concentrations greater than 1 μM. Moreover, PROTAC SGK3 degrader-2 at 0.3 μM for 5 days has no effect on SGK3 levels or the phosphorylation of TSC2, S6K1, and S6 in CAMA-1 and ZR-75-1 cells treated with GDC0941 or AZD5363.
Chemical Properties
Molecular Weight1157.38
FormulaC57H73FN10O11S2
Cas No.2381196-78-5
SmilesO(C[C@H]1CN(CCCCCCOCCOCCOCC(N[C@H](C(=O)N2[C@H](C(NCC3=CC=C(C=C3)C4=C(C)N=CS4)=O)C[C@H](O)C2)C(C)(C)C)=O)CCO1)C=5N=C(N=C6C5C=NN6)C7=CC=C(NS(=O)(=O)C8=C(F)C=CC(C)=C8)C=C7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

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
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