PROTAC STK4 Degrader-1
PROTAC STK4 Degrader-1 is a cereblon-recruiting STK4 PROTAC degrader. PROTAC STK4 Degrader-1 mediates ubiquitination and proteasomal degradation of STK4, induces dose- and time-dependent downregulation of STK4 in cancer cells, and exhibits reduced cytotoxicity in cereblon-knockout cells. PROTAC STK4 Degrader-1 can be used in research related to multiple myeloma.
(Pink: STK4 Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker (HY-115384)).
For research use only. We do not sell to patients.
- CAS No.: 2353563-15-0
- Formula: C52H61FN8O13S
- Molecular Weight:1057.15
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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- References
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Biological Activity
Description
IC50 & Target
[1]|
STK4 |
In Vitro
PROTAC STK4 Degrader-1 (compound I-19) (2.5-5 μM; 4-24 h) induces time- and dose-dependent degradation of STK4 protein in MM.1S multiple myeloma cells[1].
PROTAC STK4 Degrader-1 (0.5-2.5 μM; 24 h) degrades STK4 in MM.1S multiple myeloma cells in a CRBN-dependent manner[1].
PROTAC STK4 Degrader-1 (0.1-10 μM; 24 h) exhibits CRBN-dependent cytotoxicity against MM.1S multiple myeloma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S multiple myeloma cells
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Concentration:2.5 μM (time-course); 0.16, 0.31, 0.62, 1.25, 2.5, 5 μM (24 h dose-response)
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Incubation Time:4, 8, 16, 24 h
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Result:Induced time-dependent downregulation of STK4 protein levels, with reduced STK4 observed as early as 4 hours and further decreases through 24 hours.
Caused dose-dependent downregulation of STK4, with visible reduction at concentrations of 2.5 μM and 5 μM after 24 hours, and dose-dependent decreases across the range of 0.15 to 5 μM.
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Cell Line:parental and cereblon (CRBN)-knockout MM.1S multiple myeloma cells
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Concentration:0.5, 2.5 μM
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Incubation Time:24 h
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Result:Induced dose-dependent downregulation of STK4 in parental MM.1S cells.
Failed to degrade STK4 in CRBN-knockout MM.1S cells at the same concentrations.
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Cell Line:parental and cereblon (CRBN)-knockout MM.1S multiple myeloma cells
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Concentration:0.1, 0.2, 1, 3, 10 μM
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Incubation Time:24 h
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Result:Reduced cell growth in parental MM.1S cells.
Showed significantly decreased cytotoxic effect in CRBN-knockout MM.1S cells.
Chemical Information
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CAS No. 2353563-15-0
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Molecular Weight 1057.15
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Formula C52H61FN8O13S
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SMILES
O=C1NCCC2=C1C=CC(C3=CC(C4=C(F)C=C(S(=O)(N(C5CC5)CCCNC(CCOCCOCCOCCOCCOCCNC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O)=O)=O)C=C4)=CN=C3N)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC STK4 Degrader-1 Related Classifications
HY-131731 Related Classifications
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