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: ligand (HY-188093); Blue: Cereblon ligand (HY-10984); Black: linker (HY-115384)).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 2353563-15-0
- 화학식: C52H61FN8O13S
- 분자량:1057.15
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
More
Biological Activity
제품 설명
IC50 & Target
[1]|
STK4 |
In Vitro
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.
-
Cell Line:MM.1S multiple myeloma cells
-
Concentration:2.5 μM (time-course); 0.16, 0.31, 0.62, 1.25, 2.5, 5 μM (24 h dose-response)
-
Incubation Time:4, 8, 16, 24 h
-
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.
-
Cell Line:parental and cereblon (CRBN)-knockout MM.1S multiple myeloma cells
-
Concentration:0.5, 2.5 μM
-
Incubation Time:24 h
-
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.
-
Cell Line:parental and cereblon (CRBN)-knockout MM.1S multiple myeloma cells
-
Concentration:0.1, 0.2, 1, 3, 10 μM
-
Incubation Time:24 h
-
Result:Reduced cell growth in parental MM.1S cells.
Showed significantly decreased cytotoxic effect in CRBN-knockout MM.1S cells.
Chemical Information
-
CAS No. 2353563-15-0
-
분자량 1057.15
-
화학식 C52H61FN8O13S
-
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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)