OICR41114
OICR41114 is a WDR5 PROTAC degrader with an EC50 of 40 nM. OICR41114 binds both DCAF1 and WDR5, and its binding affinity for DCAF1 is significantly enhanced in the presence of WDR5 (KD increases from 59 nM to 5 nM). OICR41114 exerts antiproliferative effects on MV4-11 cells. OICR41114 can be used for the research of acute myeloid leukemia.
(Pink: WDR5 ligand (HY-141799); Blue: VHL ligand (HY-169390); Black: linker (HY-140210)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C70H83Cl2F6N9O15
- Molecular Weight:1475.36
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
VHL |
In Vitro
OICR41114 (5.5 μM; 20 min) binds and stabilizes recombinant DCAF1 and WDR5 proteins individually, and forms a ternary complex with the combined protein mixture as measured by DSF[1].
OICR41114 (0.002-10 μM; 5 days) reduces viability of MV4-11 cells with an EC50 of 158 nM after 5 days of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Molecular Weight 1475.36
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Formel C70H83Cl2F6N9O15
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SMILES
O=C(/C=C/C1=C(C(C(N[C@H](C2=CC=C(C(Cl)=C2)F)CC(N)=O)=O)=CN1)C3=C(C=C(C=C3)Cl)F)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(C4=CC=C(C(C5=CC=C(C(NC(C6=CNC(C=C6C(F)(F)F)=O)=O)=C5)N7C[C@H](N([C@H](C7)C)C)C)=C4)F)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)