2. PROTAC Immunology/Inflammation Cell Cycle/DNA Damage NF-κB
  3. Molecular Glues IKZF Family HOXA Interleukin Related NF-κB
  4. IKZF2-degrader 5

IKZF2-degrader 5 是一种高效、高选择性、起效迅速且具有口服活性的 IKZF2 分子胶降解剂。IKZF2-degrader 5 通过 Cullin-CRBN 依赖通路诱导 IKZF2 降解。IKZF2-degrader 5 可促炎型 IL-2 的生成。IKZF2-degrader 5 能减弱调节性 T 细胞 (Tregs) 的免疫抑制功能。IKZF2-degrader 5 可在小鼠脾脏和胸腺中触发快速、显著且持久的 IKZF2 降解。IKZF2-degrader 5 可抑制肿瘤的生长。IKZF2-degrader 5 可用于 B16F 黑色素瘤的研究。

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IKZF2-degrader 5

IKZF2-degrader 5 Chemical Structure

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IKZF2-degrader 5 相关抗体

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查看 IKZF Family 亚型特异性产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

IC50 & Target[1]

IKZF2

 

IL-2

 

体外研究
(In Vitro)

IKZF2-degrader 5 (compound 25) (48 h) 可在经 IKZF2-HiBit 改造的 HEK293T 细胞中诱导强效的 IKZF2 降解，其 DC50 为 0.00178 μM，最大降解率达 93.2%[1]。
IKZF2-degrader 5 (0.001-1 μM; 24 h) 可在 Jurkat T 和 MV-4-11 细胞中诱导强效的、剂量依赖性的内源性 IKZF2 降解[1]。
IKZF2-degrader 5 (0.001-1 μM; 24 h) 可诱导 MV-4-11 急性髓系白血病细胞中 MYC 和 HOXA9 蛋白水平呈剂量依赖性降低[1]。
IKZF2-degrader 5 (0.001-10 μM; 24 h) 可在 HEK293T 细胞中诱导 CRBN 依赖性 IKZF2 降解，而在 CRBN-/-细胞中其活性被完全消除[1]。
IKZF2-degrader 5 (0.001-10 μM; 6 h) 可在原代人 CD25+调节性 T 细胞中诱导强效的、剂量依赖性 IKZF2 降解，其 DC50 为 6.19 nM，最大降解率达 89.9%[1]。
IKZF2-degrader 5 (0.001-1 μM; 24 h) 以剂量依赖方式促进经 CD3/CD28 激活的 Jurkat T 细胞分泌 IL-2[1]。
IKZF2-degrader 5 (0.001-1 μM) 可呈剂量依赖性提升体外诱导的耗竭型 CD4+ 和 CD8+ 效应 T 细胞中 IFN-γ 的产生[1]。
IKZF2-degrader 5 (0.1 μM; 24 h) 可改变 Jurkat T 细胞的基因表达，显著激活 T 细胞受体、TNF 信号通路及 NF-kappa B 信号通路[1]。

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

IKZF2-degrader 5 相关抗体:

Western Blot Analysis[1]

Cell Line: Jurkat T cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 24 h
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.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUC0-t AUC0-∞ Vss CL MRT0-∞ Tmax Cmax Bioavailability
Mice[1] 1 mg/kg i.v. 0.49 h 132.81 ng·h/mL 133.29 ng·h/mL 2244.18 mL/kg 7539.98 mL/h/kg 0.29 h / / /
Mice[1] 10 mg/kg p.o. 0.50 h 192.45 ng·h/mL 193.05 ng·h/mL / / 0.56 h 0.08 h 460.60 ng/mL 14.49 %
体内研究
(In Vivo)

Compound 25 (30 mg/kg；口服；每日 1 次；连续 24 天) 在小鼠中对 B16F 黑色素瘤的肿瘤生长具有抑制活性[1]。
Compound 25 (10-30 mg/kg；口服；单次给药) 可在小鼠的脾脏和胸腺中诱导 IKZF2 快速、强效且持续的降解[1]。

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

Animal Model: humanized CRBNI391V C57BL/6 mice[1]
Dosage: 30 mg/kg
Administration: p.o.; once daily; 24 days
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.
Animal Model: humanized CRBNI391V C57BL/6 mice[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
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.
分子量

577.68

Formula

C33H35N7O3
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 5 相关分类

  • 摩尔计算器

  • 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 5Molecular GluesIKZF FamilyHOXAInterleukin RelatedNF-κBIkaros zinc finger protein familyHomeobox AILNuclear factor-κBNuclear factor-kappaBmouse spleenCRBNIKZF2mouse thymusCullin-CRBNregulatory T cellsTregsB16F melanomaHeliosHEK293T cellsInhibitorinhibitorinhibit

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