A PROTAC that drives SGK3 degradation
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SGK3-PROTAC1

Item No. 41170

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,4R)-1-((S)-2-(tert-butyl)-18-((R)-2-(((6-(4-((2-fluoro-5-methylphenyl)sulfonamido)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)oxy)methyl)morpholino)-4-oxo-6,9,12-trioxa-3-azaoctadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
CAS Number
2381320-35-8
Synonyms
  • Serum/Glucocorticoid-regulated Kinase 3-PROTAC1
  • Serum/Glucocorticoid-regulated Kinase 3-Proteolysis-targeting Chimera 1
  • SGK3-Proteolysis-targeting Chimera 1
Molecular Formula
C57H73FN10O11S2
Formula Weight
1157.4
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
FC(C=CC(C)=C1)=C1S(=O)(NC2=CC=C(C3=NC(OC[C@@H]4OCCN(C4)CCCCCCOCCOCCOCC(N[C@H](C(N5C[C@H](O)C[C@H]5C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)C(C)(C)C)=O)=C8C=NNC8=N3)C=C2)=O
InChi Code
InChI=1S/C57H73FN10O11S2/c1-37-10-19-46(58)48(28-37)81(73,74)66-42-17-15-41(16-18-42)52-63-53-45(31-61-65-53)55(64-52)79-34-44-33-67(21-23-78-44)20-8-6-7-9-22-75-24-25-76-26-27-77-35-49(70)62-51(57(3,4)5)56(72)68-32-43(69)29-47(68)54(71)59-30-39-11-13-40(14-12-39)50-38(2)60-36-80-50/h10-19,28,31,36,43-44,47,51,66,69H,6-9,20-27,29-30,32-35H2,1-5H3,(H,59,71)(H,62,70)(H,61,63,64,65)/t43-,44-,47+,51-/m1/s1
InChi Key
RTFQFPZKDYMMMJ-RIAKQDHQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $244

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    5 mg

    $973

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    10 mg

    $1,824

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    Product Description

    SGK3-PROTAC1 is a proteolysis-targeting chimera (PROTAC) containing the serum/glucocorticoid-regulated kinase 3 (SGK3) inhibitor 308-R conjugated to VHL ligand 1 (Item No. 21591) via an alkyl linker with two PEG units.1 It inhibits SGK3, SGK1, and p70 ribosomal S6 kinase 1 (S6K1; IC50s = 0.3, 0.22, and 1.8 µM, respectively) but selectively induces degradation of SGK3 over SGK1 and S6K1 in HEK293 cells when used at concentrations ranging from 0.3 to 3 µM. SGK3-PROTAC1 (0.3 µM) potentiates cell growth inhibition induced by GDC-0941 (Item No. 11600) in CAMA-1 and ZR-75-1 breast cancer cells. It also reduces SGK3 levels, sodium-dependent phosphate transporter 1 (PiT-1) levels, and calcium deposition induced by high levels of inorganic phosphate (Pi) in primary mouse vascular smooth muscle cells (VSMCs) when used at a concentration of 2.5 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tovell, H., Testa, A., Zhou, H., et al. Design and characterization of SGK3-PROTAC1, an isoform specific SGK3 kinase PROTAC degrader. ACS Chem. Biol. 14(9), 2024-2034 (2019).

    2. Dong, Q.-Q., Tu, Y.-C., Gao, P., et al. SGK3 promotes vascular calcification via Pit-1 in chronic kidney disease. Theranostics 14(2), 861-878 (2024).