PROTAC WDR5 degrader 1
PROTAC WDR5 degrader 1 is a heterobifunctional WDR5 PROTAC degrader with a DC50 value of 53 nM and a Kd value of 18 nM, exhibiting selective WDR5 degradation activity and cell permeability. PROTAC WDR5 degrader 1 induces proliferation defects in leukemia cells, with enhanced efficacy in cells overexpressing VHL. PROTAC WDR5 degrader 1 is applicable to research related to acute myeloid leukemia.
(Pink: WDR5 ligand (HY-168488); Blue: VHL ligand (HY-125845); Black: linker (HY-W015878)).
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- CAS No.: 2737222-94-3
- Formule: C52H60F3N9O7S
- Masse moléculaire:1012.15
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
WDR5[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
13600 nM
Compound: EUB0001122a
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Cellular target engagement assay with: WDR5
Cellular target engagement assay with: WDR5
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10.6019/CHEMBL5058541 |
| HEK-293T | IC50 |
2150 nM
Compound: EUB0001122a
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Cellular target engagement assay with: WDR5
Cellular target engagement assay with: WDR5
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10.6019/CHEMBL5058541 |
PROTAC WDR5 degrader 1 (Compound 8g) exhibits cell permeability and binds to WDR5 in live MV4-11 cells with an IC50 of 13.6 μM; its IC50 for binding to WDR5 in MV4-11 cell lysates is 2.15 μM[1].
PROTAC WDR5 degrader 1 (0.004-10 μM; 24 h) induces dose-dependent degradation of HiBiT-tagged WDR5 in MV4-11WDR5-HiBiT cells, with a DC50 of 0.053 μM and a maximum degradation rate of 58% after 24 h of treatment[1].
PROTAC WDR5 degrader 1 (0.01-10 μM; 24 h) induces dose-dependent depletion of endogenous WDR5 in untreated MV4-11 cells, and a degradative effect lasting 72 h is observed at a concentration of 0.04 μM[1].
PROTAC WDR5 degrader 1 (5-10 μM; 15 days) induces moderate proliferation defects in untreated MV4-11 cells; in MV4-11VHL cells overexpressing VHL, stronger growth inhibition is consistently observed due to enhanced WDR5 degradation efficiency[1].
PROTAC WDR5 degrader 1 mediates the depletion of endogenous WDR5 in HL-60 human leukemia cells and exhibits activity across a variety of cancer cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Naive MV4-11 cells
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Concentration:0.01, 0.1, 1 and 10 μM
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Incubation Time:24 h; 72 h
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Result:Induced dose-dependent depletion of endogenous WDR5, with efficacy matching that observed for HiBiT-tagged WDR5.
Sustained degradation for up to 72 h post-treatment at 0.04 μM.
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Cell Line:Naive MV4-11 cells, VHL-overexpressing MV4-11VHL cells
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Concentration:5 μM, 10 μM
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Incubation Time:15 days
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Result:Induced a moderate proliferation defect over 15 days in naive MV4-11 cells at 10 μM.
Induced more pronounced growth defects in VHL-overexpressing MV4-11VHL cells at both 5 μM and 10 μM, correlating with enhanced WDR5 degradation due to increased VHL expression.
Chemical Information
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CAS No. 2737222-94-3
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Masse moléculaire 1012.15
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Formule C52H60F3N9O7S
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SMILES
O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=C(N3CCN(CC3)C)C=CC(C4=CC=C(C=C4)C(NCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC WDR5 degrader 1 Related Classifications
HY-168487 Related Classifications
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