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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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| 10 mg | Inquiry | Inquiry | Inquiry | |
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| 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. |
| Molecular Weight | 1157.38 |
| Formula | C57H73FN10O11S2 |
| Cas No. | 2381196-78-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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