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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
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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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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