2. PROTAC Immunology/Inflammation
  3. Molecular Glues IKZF Family
  4. IKZF2-degrader 2

IKZF2-degrader 2 is a selective and orally active IKZF2 molecular glue degrader with DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS. The IKZF2-degrader 2 mediates the ubiquitination and degradation of target proteins by recruiting the CRL4-CRBN E3 ubiquitin ligase. IKZF2-degrader 2 displays moderate degradation against SALL4 with a DC50 of 9 nM but does not induce any significant degradation towards IKZF1, IKZF3, CK1α and GSPT1. IKZF2-degrader 2 can be used for the study of cancer immunology.

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IKZF2-degrader 2

IKZF2-degrader 2 Chemical Structure

CAS No. : 2983841-00-3

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IKZF2-degrader 2 Related Antibodies

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Description

IKZF2-degrader 2 is a selective and orally active IKZF2 molecular glue degrader with DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS. The IKZF2-degrader 2 mediates the ubiquitination and degradation of target proteins by recruiting the CRL4-CRBN E3 ubiquitin ligase. IKZF2-degrader 2 displays moderate degradation against SALL4 with a DC50 of 9 nM but does not induce any significant degradation towards IKZF1, IKZF3, CK1α and GSPT1. IKZF2-degrader 2 can be used for the study of cancer immunology[1].

IC50 & Target[1]

IZKF2

0.5 nM (DC50)

In Vitro

IKZF2-degrader 2 (Compound 55) (41 nM-10 μM, 6 h) is a highly selective IKZF2 degrader with minimal off-target neo-substrate degradation in Jurkat cells[1].
IKZF2-degrader 2 (1 μM) exhibits excellent metabolic stability in human, crab-eating monkey, rat and mouse liver microsomes, especially in the human[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

IKZF2-degrader 2 Related Antibodies

Western Blot Analysis[1]

Cell Line: Jurkat cells and CRBN knockout (KO) Jurkat cells
Concentration: 41, 123, 370, 1111, 3333 and 10000 nM
Incubation Time: 6 h
Result: Selectively degraded IKZF2 without impacting IKZF1, CK1α, or GSPT1.
Was completely lost in CRBN KO cells, confirming CRBN-mediated activity.
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. T1/2 1.46 h
Mice 3 mg/kg p.o. T1/2 1.38 h
Rat 1 mg/kg i.v. T1/2 1.36 h
Rat 3 mg/kg p.o. T1/2 1.92 h
Mice 1 mg/kg i.v. CL 32.7 mL/min/kg
Mice 3 mg/kg p.o. Cmax 489 ng/mL
Rat 1 mg/kg i.v. CL 35.7 mL/min/kg
Rat 3 mg/kg p.o. Cmax 138 ng/mL
Mice 1 mg/kg i.v. Vss 2.83 L/kg
Mice 3 mg/kg p.o. AUC 947 ng·h/mL
Rat 1 mg/kg i.v. Vss 2.46 L/kg
Rat 3 mg/kg p.o. AUC 563 ng·h/mL
Mice 3 mg/kg p.o. F 61 %
Rat 3 mg/kg p.o. F 38 %
In Vivo

IKZF2-degrader 2 (Compound 55) (10-30 mg/kg, i.g., single dose) achieves strong and long-lasting degradation of the IKZF2 protein in immune organs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PK/PD evaluation in immune competent established in gene-edited C57BL/6 mice harboring humanized CRBNMI391 V protein[1]
Dosage: 10 and 30 mg/kg
Administration: Oral gavage (i.g.), single dose
Result: Showed profound IKZF2 degradation at 6 h which was attenuated at 24 h in both spleen and thymus tissues.
Was comparable with that in thymus in spleen, while 8-fold higher drug exposures in spleen was observed than that in thymus.
Molecular Weight

509.96

Formula

C26H25ClFN5O3
CAS No.
SMILES

O=C1C2=C(CN1C3C(NC(CC3)=O)=O)C(F)=C(C4=C(Cl)C(CN5CCCC5)=C(C=CN6C)C6=N4)C=C2
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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IKZF2-degrader 2 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:

IKZF2-degrader 22983841-00-3Molecular GluesIKZF FamilyIkaros zinc finger protein familyIKZF2-degraderPharmacokineticsPharmacodynamicsCRBNcancer immunotherapyInhibitorinhibitorinhibit

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