2381196-78-5
Chemical Structure
PROTAC SGK3 degrader-2
- CAS. Nr.: 2381196-78-5
- Formula:C57H73FN10O11S2
- Molecular Weight:1157.38
IUPAC Name: (2S,4S)-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
InChIKey: RTFQFPZKDYMMMJ-RLHUTWFYSA-N
SMILES: O=C(N1[C@@H](C[C@@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCOCCOCCCCCCN(CCO4)C[C@@H]4COC5=C(C=NN6)C6=NC(C7=CC=C(C=C7)NS(=O)(C8=C(C=CC(C)=C8)F)=O)=N5)=O
Biological Activity: PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878), with a cis hydroxyl group in its VH032 moiety, which is incapable of binding to the VHL E3 ligase. PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but shows no SGK3 degradation efficiency. PROTAC SGK3 degrader-2 can be used as a control compound to study the specific effects of SGK3-PROTAC1-mediated SGK3 degradation[1].
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PROTAC SGK3 degrader-2 | PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878), with a cis hydroxyl group in its VH032 moiety, which is incapable of binding to the VHL E3 ligase. PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but shows no SGK3 degradation efficiency. PROTAC SGK3 degrader-2 can be used as a control compound to study the specific effects of SGK3-PROTAC1-mediated SGK3 degradation. | |||||||||||||||||||||
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Keywords
