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

IKZF2-degrader 2 是一种具有选择性和口服活性的 IKZF2 分子胶降解剂，其 DC50 值分别为 0.5 nM (HiBit) 和 1.8 nM (FACS)。IKZF2-degrader 2 通过募集 CRL4-CRBN E3 泛素连接酶来介导靶蛋白的泛素化和降解。IKZF2-degrader 2 对 SALL4 表现出中等程度的降解作用，其 DC50 值为 9 nM，但对 IKZF1、IKZF3、CK1α 和 GSPT1 无显著降解。IKZF2-degrader 2 可用于癌症免疫学研究。

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IKZF2-degrader 2

IKZF2-degrader 2 Chemical Structure

CAS No. : 2983841-00-3

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IKZF2-degrader 2 相关抗体

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查看 IKZF Family 亚型特异性产品:

查看所有亚型
IKZF1 IKZF2 IKZF3 IKZF4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

IKZF2-degrader 2 (Compound 55) (41 nM-10 μM, 6 h) 是一种高选择性 IKZF2 降解剂，在 Jurkat 细胞中，其脱靶新底物降解率极低[1]。
IKZF2-degrader 2 (1 μM) 在人、食蟹猴、大鼠和小鼠肝微粒体中表现出优异的代谢稳定性，尤其是在人体中[1]。

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

IKZF2-degrader 2 相关抗体:

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.
药代动力学
(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 %
体内研究
(In Vivo)

IKZF2-degrader 2 (Compound 55) (10-30 mg/kg, i.g., 单剂量) 可在免疫器官中实现强效且持久的 IKZF2 蛋白的降解[1]。

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.
分子量

509.96

Formula

C26H25ClFN5O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

IKZF2-degrader 2 相关分类

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  • 稀释计算器

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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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