2. PROTAC Stem Cell/Wnt Cell Cycle/DNA Damage
  3. Molecular Glues Casein Kinase
  4. IBA-11

IBA-11 是一种选择性依赖 CRBN 的 CK1α 分子胶 (molecular glue) 降解剂。IBA-11 结合 CRBN 的经典三色氨酸口袋，与 CK1α 形成三元复合物以介导其降解。IBA-11 诱导依赖 CRBN 的泛素-蛋白酶体系统介导的 CK1α 降解。IBA-11 对癌细胞表现出细胞毒性。IBA-11 在大鼠肝微粒体中表现出体外代谢稳定性，且对 hERG 的抑制作用极弱。IBA-11 可用于癌症相关研究，例如急性髓系白血病。

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IBA-11

IBA-11 Chemical Structure

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IBA-11 相关抗体

Top Publications Citing Use of Products

查看 Casein Kinase 亚型特异性产品:

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CK1 CK2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia[1].

IC50 & Target[1]

CK1α

 

Cereblon

 

体外研究
(In Vitro)

IBA-11 在无细胞 TR-FRET 实验中以 IC50 为 2285 nM 的亲和力结合 CRBN[1]。
IBA-11 可强效抑制 MV-4-11 细胞的活力，其 IC50 为 82.11 nM，而在 MM.1S 和 Mino 细胞中仅表现出极弱的活性[1]。
IBA-11 (0.1-2.5 nM; 8 h) 可在 MV-4-11 和 Mino 细胞中诱导 CK1α 呈剂量依赖性降解，但不会诱导 IKZF1/2/3 或 GSPT1 降解[1]。
IBA-11 (500 nM; 2-16 h) 可在 2 h 内诱导 Mino 细胞中 CK1α 快速、近乎完全降解[1]。
IBA-11 (500 nM; 3 h) 诱导 Mino 细胞中 CK1α 降解的过程依赖于 CRBN 介导的泛素-蛋白酶体系统，这一点已通过 MLN4924 (HY-70062)、PS341 (HY-10227) 和 MG132 (HY-13259) 的挽救实验得到证实[1]。
IBA-11 (0.2-2 μM) 诱导的 CK1α 降解严格依赖于 CRBN，因为在 CRBN 敲除的 HEK293T 细胞中该降解作用被完全阻断[1]。
IBA-11 在大鼠肝微粒体中具有良好的体外代谢稳定性，且心脏毒性风险较低，这一点可由其极弱的 hERG 抑制作用 (IC50 >40 μM) 得到证明[1]。

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

IBA-11 相关抗体:

Western Blot Analysis[1]

Cell Line: MV-4-11, Mino
Concentration: 0.1, 0.5, 2.5 nM
Incubation Time: 8 h
Result: Induced dose-dependent degradation of CK1α in both MV-4-11 and Mino cells.
Left IKZF1/2/3 and GSPT1 largely unaffected across all tested concentrations.

Western Blot Analysis[1]

Cell Line: Mino
Concentration: 500 nM
Incubation Time: 2, 4, 8, 16 h
Result: Induced near-complete depletion of CK1α within 2 h of treatment.
Induced time-dependent degradation.
分子量

437.40

Formula

C22H17F2N5O3
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

IBA-11 相关分类

  • 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.

Keywords:

IBA-11IBA11IBA 11Molecular GluesCasein KinaseCK1αCRBNacute myeloid leukemiaubiquitin-proteasome systemhERGMV-4-11 cellsMino cellsCereblonrat liver microsomesMM.1S cellsInhibitorinhibitorinhibit

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目录号：
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