IKZF2-degrader 5
IKZF2-degrader 5 is a highly efficient, highly selective, rapidly acting, and orally active IKZF2 molecular glue degrader. IKZF2-degrader 5 induces IKZF2 degradation via the Cullin-CRBN-dependent pathway. IKZF2-degrader 5 promotes the production of pro-inflammatory IL-2. IKZF2-degrader 5 attenuates the immunosuppressive function of regulatory T cells (Tregs). IKZF2-degrader 5 triggers rapid, significant, and sustained IKZF2 degradation in the spleen and thymus of mice. IKZF2-degrader 5 inhibits tumor growth. IKZF2-degrader 5 can be used for the research of B16F melanoma.
For research use only. We do not sell to patients.
- Formula: C33H35N7O3
- Molecular Weight:577.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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IKZF2 |
IL-2 |
IKZF2-degrader 5 (compound 25) (48 h) induces potent IKZF2 degradation in IKZF2-HiBit engineered HEK293T cells, with a DC50 of 0.00178 μM and a maximum degradation rate of 93.2%[1].
IKZF2-degrader 5 (0.001-1 μM; 24 h) induces potent, dose-dependent degradation of endogenous IKZF2 in Jurkat T and MV-4-11 cells[1].
IKZF2-degrader 5 (0.001-1 μM; 24 h) induces dose-dependent reductions in MYC and HOXA9 protein levels in MV-4-11 acute myeloid leukemia cells[1].
IKZF2-degrader 5 (0.001-10 μM; 24 h) induces CRBN-dependent IKZF2 degradation in HEK293T cells, whereas its activity is completely ablated in CRBN-/- cells[1].
IKZF2-degrader 5 (0.001-10 μM; 6 h) induces potent, dose-dependent degradation of IKZF2 in primary human CD25+ regulatory T cells, with a DC50 of 6.19 nM and a maximum degradation rate of 89.9%[1].
IKZF2-degrader 5 (0.001-1 μM; 24 h) promotes IL-2 secretion in CD3/CD28-activated Jurkat T cells in a dose-dependent manner[1].
IKZF2-degrader 5 (0.001-1 μM) dose-dependently enhances IFN-γ production in in vitro induced exhausted CD4+ and CD8+ effector T cells[1].
IKZF2-degrader 5 (0.1 μM; 24 h) alters gene expression in Jurkat T cells and significantly activates the T cell receptor, TNF signaling pathway, and NF-κB signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat T cells
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:24 h
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Result:Elicited dose-dependent IKZF2 degradation, with near-complete degradation achieved at 0.1 μM after 24 h.
Achieved a DC50 for IKZF2 degradation of 1.59 nM with a Dₘₐₓ of 92.2%.
Caused minimal degradation of IKZF1, IKZF3, SALL4, GSPT1, CK1α, or ZFP91.
IKZF2-degrader 5 (10-30 mg/kg; p.o.; single administration) induces rapid, potent and sustained degradation of IKZF2 in the spleen and thymus of mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:humanized CRBNI391V C57BL/6 mice[1]
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Dosage:30 mg/kg
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Administration:p.o.; once daily; 24 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 77.30%, with a mean tumor volume of 550.7 mm3 (compared to vehicle control mean tumor volume of 1581.4 mm3).
Caused no significant body weight loss or systemic toxicity.
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Animal Model:humanized CRBNI391V C57BL/6 mice[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Reduced IKZF2 levels to 32.2% of vehicle control in the spleen and 16.6% of vehicle control in the thymus at 3 h post-administration of 30 mg/kg.
Reduced IKZF2 levels to 36.0% of vehicle control in the spleen and 44.2% of vehicle control in the thymus at 6 h post-administration of 10 mg/kg.
Reduced IKZF2 levels to 23.7% of vehicle control in the spleen and 27.7% of vehicle control in the thymus at 6 h post-administration of 30 mg/kg.
Reduced IKZF2 levels to 26.5% of vehicle control in the spleen and 32.6% of vehicle control in the thymus at 12 h post-administration of 10 mg/kg.
Reduced IKZF2 levels to 16.7% of vehicle control in the spleen and 20.6% of vehicle control in the thymus at 12 h post-administration of 30 mg/kg.
Chemical Information
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Molecular Weight 577.68
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Formula C33H35N7O3
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SMILES
O=C1N(C2CCC(NC2=O)=O)N(C)CC3=C1C=CC(NCC4=CC(CN5CCN(C6=CC=CC(C#N)=C6)CC5)=CC=C4)=C3
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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)
IKZF2-degrader 5 Related Classifications
HY-182945 Related Classifications
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