2. PROTAC Immunology/Inflammation
  3. Molecular Glues IKZF Family IFNAR
  4. 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.

NHWL071065

NHWL071065 Chemical Structure

CAS No. : 3117340-01-6

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NHWL071065 Related Antibodies

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Description

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[1].

IC50 & Target[1]

IKZF1

 

IKZF3

 

In Vitro

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.

NHWL071065 Related Antibodies

Western Blot Analysis[1]

Cell Line: TMD8 lymphoma cells, WSU-DLCL2 lymphoma cells
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)
Incubation Time: 16 h
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.
Parmacokinetics
Species Dose Route AUC0-∞ MRT0-∞ T1/2β Tmax Vz Cmax
Rat[1] 2 mg/kg i.v. 1078.319 μg/L·h 5.807 h 6.395 h / 17.456 L/kg 2330 μg/L
Rat[1] 10 mg/kg p.o. 1105.037 μg/L·h 8.046 h 5.913 h 0.667 h 77.406 L/kg 157.667 μg/L
Molecular Weight

576.66

Formula

C31H37FN6O4
CAS No.
SMILES

O=C(C(N1C(C)=NC2=C(C(NCC3=CC=C(CN4CCC(N5CCOCC5)CC4)C=C3F)=CC=C2)C1=O)CC6)NC6=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NHWL071065 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NHWL0710653117340-01-6NHWL 071065NHWL-071065Molecular GluesIKZF FamilyIFNARIkaros zinc finger protein familyInterferon-α/β receptorInterferon-alpha/beta receptorIKZF1TMD8 cellsCRBN E3 ligase modulatorlymphomaWSU-DLCL2 cellsIKZF3type I interferon signaling pathwayhuman liver microsomesubiquitin-proteasome pathwaylymphoma cellsInhibitorinhibitorinhibit

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