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Cat. No.: HY-W1128213

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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.

For research use only. We do not sell to patients.

CAS No.: 2983841-00-3
Formula: C₂₆H₂₅ClFN₅O₃
Molecular Weight:509.96

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

IKZF2-degrader 2 Chemical Structure

CAS No.: 2983841-00-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

IZKF2

0.5 nM (DC₅₀)

All IKZF Family Isoforms :

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.

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

Species	Dose	Route	T_1/2	CL	V_ss	C_max	AUC	F
Mice^[1]	1 mg/kg	i.v.	1.46 h	32.7 mL/min/kg	2.83 L/kg	/	/	/
Mice^[1]	3 mg/kg	p.o.	1.38 h	/	/	489 ng/mL	947 ng·h/mL	61 %
Rat^[1]	1 mg/kg	i.v.	1.36 h	35.7 mL/min/kg	2.46 L/kg	/	/	/
Rat^[1]	3 mg/kg	p.o.	1.92 h	/	/	138 ng/mL	563 ng·h/mL	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 CRBNM^{I391 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.

Chemical Information

CAS No. 2983841-00-3
Molecular Weight 509.96
Formula C₂₆H₂₅ClFN₅O₃
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhang X, et al. Discovery of a Novel Series of iso-Indolinone-Based Glutarimides as Highly Efficacious and Selective IKZF2 Molecular Glue Degraders. J Med Chem. 2025 Sep 11;68(17):18230-18257. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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IKZF2-degrader 2

All IKZF Family Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

IKZF2-degrader 2 Related Classifications

HY-W1128213 Related Classifications