2. Apoptosis
  3. MDM-2/p53
  4. WB214

WB214 是一种 MDM2 和 GSPT1 降解剂，其对人源 MDM2 的 Ki >10 μM。WB214 可诱导 MDM2 与 cereblon E3 连接酶复合物产生新的相互作用，触发 MDM2 泛素化、蛋白酶体降解以及旁系 p53 降解，且不结合 MDM2 的 p53 结合区域。WB214 可诱导 GSPT1 降解，并在白血病细胞中表现出抗增殖活性。WB214 可用于白血病的研究。

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WB214

WB214 Chemical Structure

CAS No. : 2640723-72-2

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WB214 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WB214 is an MDM2 and GSPT1 degrader with human MDM2 Ki >10 μM. WB214 induces a neo-interaction between MDM2 and the cereblon E3 ligase complex, triggering MDM2 ubiquitination, proteasomal degradation, and bystander p53 degradation, and does not bind MDM2’s p53 binding region. WB214 induces GSPT1 degradation, and exhibits anti-proliferative activity in leukemia cells. WB214 can be used for the research of leukemia[1].

体外研究
(In Vitro)

WB214 (compound 11) (97 nM-10 μM；72 小时) 可强效抑制人急性白血病细胞 RS4;11 的增殖，其 IC50 为 1.2 nM[1]。
WB214 (1.2 nM-1 μM；1-12 小时) 可在人急性白血病细胞 RS4;11 中以时间和剂量依赖的方式诱导 MDM2 (DC50 = 4.1 nM) 和 p53 (DC50 = 29 nM) 降解[1]。
WB214 (100 nM；6 小时) 在人急性白血病细胞 RS4;11 中介导的 MDM2 和 p53 降解依赖于 CRBN E3 连接酶和泛素-蛋白酶体系统，其中 p53 因与 MDM2 结合而作为旁观者被降解[1]。
WB214 (97 nM-10 μM；0.5 小时) 不与纯化 MDM2 蛋白的 p53 结合口袋结合[1]。
WB214 (100 nM) 可在人急性白血病细胞 RS4;11 中高效诱导 MDM2 与 CRBN 形成三元复合物[1]。
WB214 (15 min) 可强效诱导纯化的 CRBN/DDB1 与 MDM2 蛋白之间形成剂量依赖性的三元复合物[1]。
WB214 (100 nM；6 小时) 可导致 MDM2 和 p53 降解，而当与 Lenalidomide (HY-A0003) 或 MG132 (HY-13259) 共同处理时，这种降解作用会被消除[1]。
WB214 (1.2-100 nM；6-12 小时) 可在人急性白血病细胞 RS4;11 中诱导 GSPT1 呈剂量依赖性降解，其 DC50 = 0.64 nM[1]。

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

WB214 相关抗体:

Western Blot Analysis[1]

Cell Line: RS4;11 human acute leukemia cells
Concentration: 1.2 nM; 3.7 nM; 11 nM; 33 nM; 100 nM; 1 μM
Incubation Time: 1 h; 2 h; 4 h; 6 h; 8 h; 12 h
Result: Induced time-dependent degradation of MDM2 and p53, with detectable degradation observed as early as 4 h post-treatment with 100 nM, and near-complete MDM2 depletion by 8 h.
Exhibited dose-dependent degradation with a DC50 of 4.1 nM for MDM2 and 29 nM for p53 at 12 h.
Resulted in significant depletion of both MDM2 and p53 protein levels when treated at 1 μM for 6 h.

Western Blot Analysis[1]

Cell Line: RS4;11 human acute leukemia cells
Concentration: 100 nM; 100 nM plus 20 μM Lenalidomide; 100 nM plus 5 μM MG132; 100 nM plus 10 μM ligand 1; 100 nM plus 10 μM WB138
Incubation Time: 6 h
Result: Caused degradation of MDM2 and p53 that was abolished when co-treated with Lenalidomide or MG132.
Induced degradation of MDM2 that was not blocked, and degradation of p53 that was rescued, when co-treated with MDM2 inhibitors ligand 1 or WB138.

Western Blot Analysis[1]

Cell Line: RS4;11 human acute leukemia cells
Concentration: 1.2 nM; 3.7 nM; 11 nM; 33 nM; 100 nM
Incubation Time: 6 h; 12 h
Result: Induced potent degradation of GSPT1, with dose-dependent degradation observed and a DC50 of 0.64 nM at 12 h.
Resulted in significant depletion of GSPT1 protein levels when treated with 10 nM or 100 nM for 6 h.
分子量

846.29

Formula

C44H43ClF3N5O7
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

WB214 相关分类

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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:

WB2142640723-72-2WB 214WB-214MDM-2/p53p53leukemia cellsCRBN E3 ligaseubiquitin-proteasome systemGSPT1RS4;11 human acute leukemia cellsMDM2proteasomal degradationcereblon E3 ligase complexubiquitinationInhibitorinhibitorinhibit

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