NHWL071065
NHWL071065 is a CRBN-targeting IKZF1/IKZF3 molecular glues degrader. NHWL071065 selectively degrades IKZF1 and IKZF3 in lymphoma cells via the ubiquitin-proteasome pathway. NHWL071065 inhibits the proliferation of lymphoma cells. NHWL071065 downregulates proteins involved in cytoskeleton assembly, cell adhesion and immune regulation in cells, while upregulating proteins related to the type I IFN signaling pathway. NHWL071065 can be used in the research of lymphoma.
For research use only. We do not sell to patients.
- CAS No.: 3117340-01-6
- Formula: C31H37FN6O4
- Molecular Weight:576.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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IKZF1 |
IKZF3 |
NHWL071065 (Compound 26) (3 days) potently inhibits the proliferation of TMD8 cells (IC50 = 6.6 nM) and WSU-DLCL2 cells (IC50 = 2.6 nM), but shows no inhibitory activity against MKN28, PANC-1, LO2 or HUVEC cells[1].
NHWL071065 (1.25-40 nM, 0.313-5 μM; 16 h) potently and selectively degrades IKZF1 (DC50 = 1.8 nM) and IKZF3 (DC50 = 14.9 nM) in TMD8 cells, induces concentration-dependent degradation of IKZF1/IKZF3 in WSU-DLCL2 cells, and does not degrade PDE6D, SALL4 or GSPT1[1].
NHWL071065 (100 nM; 6 h) significantly downregulates IKZF1/IKZF3 and proteins involved in cytoskeleton assembly, cell adhesion and immune regulation in TMD8 cells, while upregulating proteins related to the type I interferon signaling pathway, but exerts no significant effects on GSPT1, NEK7 or CK1α[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TMD8 lymphoma cells, WSU-DLCL2 lymphoma cells
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Concentration:1.25, 2.5, 5, 10, 20, 40 nM (TMD8 cells, IKZF1/IKZF3); 1, 5, 10, 50 nM (WSU-DLCL2 cells, IKZF1/IKZF3); 0.313, 0.625, 1.25, 2.5, 5 μM (TMD8 cells, PDE6D/SALL4); 1, 5, 10, 50 nM (TMD8 cells, GSPT1)
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Incubation Time:16 h
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Result:Achieved a DC50 of 1.8 nM for IKZF1 degradation and 14.9 nM for IKZF3 degradation in TMD8 cells, with near-complete degradation at 40 nM.
Concentration-dependently degraded both IKZF1 and IKZF3 in WSU-DLCL2 cells, with significant reduction observed at 1 nM.
Did not degrade PDE6D (up to 5 μM), SALL4 (up to 2.5 μM), or GSPT1 (at concentrations that potently degrade IKZF1/3) in TMD8 cells.
Chemical Information
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CAS No. 3117340-01-6
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Molecular Weight 576.66
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Formula C31H37FN6O4
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SMILES
O=C(C(N1C(C)=NC2=C(C(NCC3=CC=C(CN4CCC(N5CCOCC5)CC4)C=C3F)=CC=C2)C1=O)CC6)NC6=O
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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)