2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. Wee1 HSP
  4. HEMTAC WEE1 degrader-1

HEMTAC WEE1 degrader-1 是一种 WEE1 的 HSP90 介导靶向嵌合体 (HEMTAC) 降解剂 (HSP90 酶抑制活性为 IC50: 16.76 nM)。HEMTAC WEE1 degrader-1 能促进 WEE1 的泛素化和降解。HEMTAC WEE1 degrader-1 可阻断 G2/M 细胞周期。HEMTAC WEE1 degrader-1 在急性髓系白血病 (AML) 患者来源的异种移植 (PDX) 模型中具有抗癌活性。HEMTAC WEE1 degrader-1 可用于 AML 的研究。(粉色：HSP90 结合剂；蓝色：WEE1 配体；黑色：连接子)。

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HEMTAC WEE1 degrader-1 Chemical Structure

HEMTAC WEE1 degrader-1 Chemical Structure

CAS No. : 3002417-64-0

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HEMTAC WEE1 degrader-1 相关抗体

Top Publications Citing Use of Products

查看 Wee1 亚型特异性产品:

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PKMYT1

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker)[1].

IC50 & Target

HSP90

16.76 nM (IC50)

体外研究
(In Vitro)

HEMTAC WEE1 degrader-1 (Compound 9c) (72 小时) 可抑制 MV-4-11 细胞 (IC50: 8.08 nM) 和原发性 AML 细胞的增殖活性 (IC50: 4.77 nM)[1]。
HEMTAC WEE1 degrader-1 (0.01-10 μM, 12 小时) 可降解 MV-4-11 细胞中 WEE1 蛋白，且对 AKT 蛋白的影响较小，表明该作用独立于 HSP90 抑制[1]。
HEMTAC WEE1 degrader-1 (0.1-10 μM, 12 小时) 以浓度依赖性方式促进 MV-4-11 细胞中 WEE1 mRNA 的表达[1]。
HEMTAC WEE1 degrader-1 (3-30 nM, 72 小时) 以浓度依赖性方式诱导 MV-4-11 细胞周期停滞于 G2/M 期[1]。

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

HEMTAC WEE1 degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0.01 μM, 0.1 μM, 1 μM and 10 μM
Incubation Time: 12 h
Result: Down-regulated the expression of WEE1 protein.

RT-PCR[1]

Cell Line: MV-4-11 cells
Concentration: 0.1 μM, 1 μM and 10 μM
Incubation Time: 12 h
Result: Up-regulated the expression of WEE1 mRNA.

Cell Cycle Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 3 nM, 10 nM and 30 nM
Incubation Time: 72 h
Result: Induced a large accumulation of cells in the G2/M phase.
体内研究
(In Vivo)

HEMTAC WEE1 degrader-1 (Compound 9c) (3 mg/kg，静脉注射，一天一次，四周) 在小鼠 AML 患者来源的异种移植 (PDX) 模型具有抗癌活性且毒性小[1]。
HEMTAC WEE1 degrader-1 (10 mg/kg，静脉注射，一天一次，三天) 在健康小鼠中的骨髓抑制毒性小[1]。

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

Animal Model: AML patient-derived xenograft (PDX) model, Female NOD/SCID mice (6-9 weeks old)[1]
Dosage: 3 mg/kg
Administration: Intravenous injection (i.v.), once every day for 4 weeks
Result: Reduced the percentage of huCD45-positive cells in the bone marrow (>75%).
Inhibited splenomegaly.
Animal Model: Healthy male BALA/C mice (20-22 g)[1]
Dosage: 10 mg/kg
Administration: Intravenous injection (i.v.), once every day for 3 d
Result: Had minimal effect on platelets, leukocytes and neutrophils
分子量

1062.27

Formula

C57H71N15O6
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

HEMTAC WEE1 degrader-1 相关分类

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  • 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:

HEMTAC WEE1 degrader-13002417-64-0Wee1HSPHeat shock proteinsAnticancerMV-4-11 cellsAMLAML patient-derived xenograft (PDX) modelInhibitorinhibitorinhibit

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