1. PROTAC Immunology/Inflammation
  2. PROTACs Molecular Glues IKZF Family
  3. IBA-12

IBA-12 是一种 IKZF2 分子胶/PROTAC (molecular glue/PROTAC) 降解剂,其 DC50 为 276.2 nM (Jurkat 细胞) 和 461.8 nM (Mino 细胞),IC50 为 179.9 nM。IBA-12 可结合 CRBN 的经典三色氨酸口袋,与 IKZF2 形成三元复合物。IBA-12 可诱导 CRBN 依赖的泛素-蛋白酶体系统介导的 IKZF2 降解,对其他 CRBN 底物无影响。IBA-12 可通过降解 IKZF2 诱导白细胞介素-2 (IL-2) 的产生。IBA-12 可用于癌症免疫研究。
(粉色: IZKF2 配体 (HY-Y1863);蓝色: Cereblon 配体 (HY-182807);黑色: 连接子)。

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IBA-12

IBA-12 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IBA-12 is a IKZF2 molecular glue/PROTAC degrader with a DC50 of 276.2 nM (Jurkat cells) and 461.8 nM (Mino cells), and an IC50 of 179.9 nM. IBA-12 binds to the canonical tryptophan triad pocket of CRBN to form a ternary complex with IKZF2. IBA-12 induces IKZF2 degradation mediated by the CRBN-dependent ubiquitin-proteasome system, with no effect on other CRBN substrates. IBA-12 induces the production of interleukin-2 (IL-2) through degrading IKZF2. IBA-12 is applicable to cancer immunology research[1]. (Pink: IZKF2 ligand (HY-Y1863); Blue: Cereblon ligand (HY-182807); Black: linker).

IC50 & Target[1]

IKZF2

276.2 nM (DC50)

Cereblon

 

体外研究
(In Vitro)

IBA-12 (0-1000 nM; 24 h) 呈剂量依赖性上调受刺激 Jurkat 细胞中 IL-2 的产生,证实其可对 IKZF2 调控的转录通路进行功能性调节[1]

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

ELISA Assay[1]

Cell Line: stimulated Jurkat cells
Concentration: 0, 10, 100, 1000 and 1000 nM
Incubation Time: 24 h
Result: Induced dose-dependent increases in IL-2 production.
Showed statistically significant increases observed at 100 and 1000 nM.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t MRT0-∞ F Vss CL
Rat[1] 2 mg/kg i.v. 2.68 h 0.194 h 1359 ng/mL 3748 2.39 h / 1.27 L/kg 8.87 mL/min/kg
Rat[1] 10 mg/kg p.o. 2.49 h 0.667 h 2540 ng/mL 8339 2.57 h 44.5 % / /
分子量

452.93

Formula

C24H25ClN4O3

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
IBA-12
目录号:
HY-182799
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