2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. WWZ-11-098

WWZ-11-098 是一种选择性 CDK6 降解剂，其 DC50 为 2.6 nM。WWZ-11-098 以 CRBN 依赖的方式诱导 CDK6 降解，同时不影响 CDK1、CDK2、CDK4 和 CDK9。WWZ-11-098 可诱导细胞凋亡 (apoptosis)、G1-S 细胞周期阻滞，并在癌细胞中表现出抗增殖活性。WWZ-11-098 在异种移植模型中展现出抗肿瘤功效，且无毒性迹象。WWZ-11-098 可用于白血病的研究。

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WWZ-11-098

WWZ-11-098 Chemical Structure

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WWZ-11-098 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WWZ-11-098 is a selective CDK6 degrader with DC50 of 2.6 nM. WWZ-11-098 induces degradation of CDK6 in a CRBN-dependent manner, while sparing CDK1, CDK2, CDK4, and CDK9. WWZ-11-098 induces apoptosis, G1-S cell cycle arrest and shows anti-proliferative activity in cancer cells. WWZ-11-098 exhibits antitumor efficacy in a xenograft model without signs of toxicity. WWZ-11-098 can be used for the research of leukemia[1].

IC50 & Target[1]

CDK6

2.6 nM (DC50)

体外研究
(In Vitro)

WWZ-11-098 (5 days) 可强效抑制 MOLT-4 细胞 (IC50 = 70 nM) 和 MV4-11 细胞 (IC50 = 0.13 μM) 的增殖[1]。
WWZ-11-098 (10 nM-10 μM; 3-24 h) 可在 MOLT-4 细胞中强效且选择性地降解 CDK6，其 DC50 为 2.6 nM，在 100 nM 作用 24 h 时降解率超过 98%；同时该化合物不影响 CDK1、CDK2、CDK4 和 CDK9，其作用机制依赖于 CRBN[1]。
WWZ-11-098 (100-200 nM; 48 h) 可诱导 MOLT-4 细胞发生 G1-S 细胞周期阻滞并诱导凋亡[1]。

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

WWZ-11-098 相关抗体:

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 10, 100 nM, 10 μM
Incubation Time: 3, 6, 9, 12, 24 h
Result: Achieved 98% degradation of CDK6 at 100 nM for 24 h.
Induced dose-dependent CDK6 degradation with a DC50 of 2.6 nM and a Dmax exceeding 99%, with no hook effect up to 10 μM.
Depleted over 80% of CDK6 within 3 h of treatment with 100 nM.
Showed rescued CDK6 degradation by pre-treatment with CDK2/4/6 inhibitor, MG132 (HY-13259), confirming CRBN-dependent activity via the ubiquitin-proteasome pathway.

Cell Cycle Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 100, 200 nM
Incubation Time: 48 h
Result: Induced G1-S cell cycle arrest in MOLT-4 cells, with a stronger effect than control compounds at equivalent concentrations.

Apoptosis Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 100, 200 nM
Incubation Time: 48 h
Result: Significantly promoted apoptosis in MOLT-4 cells, with superior efficacy compared to control compounds.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax Tmax AUC0-∞ AUC0-t F C0 CL
Mice[1] 5 mg/kg i.v. 2.64 ± 0.899 h 11833 ± 1242 ng/mL 0.0833 ± 0.000 h 7821 ± 1464 ng·h/mL 7766 ± 1393 ng·h/mL / 17358 ± 2227 ng/mL 655 ± 123 mL/h/kg
Mice[1] 20 mg/kg p.o. 0.293 ± 0.0441 h 294 ± 155 ng/mL 0.250 ± 0.00 h 203 ± 97.4 ng·h/mL 201 ± 97.5 ng·h/mL 0.647 ± 0.31 % / /
体内研究
(In Vivo)

WWZ-11-098 (10 mg/kg；静脉注射；每天一次；21 天) 可在 MOLT-4 异种移植小鼠模型中实现显著且耐受性良好的肿瘤生长抑制[1]。

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

Animal Model: Nude mice (male, 4-6 weeks old, 18-22 g, MOLT-4 cell line xenograft model)[1]
Dosage: 10 mg/kg
Administration: 21 days
Result: Induced sustained degradation of CDK6 and corresponding reductions of phosphorylated retinoblastoma protein (p-RB) in tumor tissues 6 hours after final dose at day 3.
Significantly suppressed MOLT-4 xenograft tumor growth, with marked reductions in both tumor volume and final tumor weight.
Caused no significant body weight loss throughout the study.
分子量

828.90

Formula

C39H47F3N8O7S
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

WWZ-11-098 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:

WWZ-11-098CDKApoptosisCyclin dependent kinaseCRBNacute lymphoblastic leukemiaCereblonCDK6G1-S cell cycle arrestMOLT-4 cellsleukemiaInhibitorinhibitorinhibit

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产品名称：
WWZ-11-098
目录号：
HY-181490
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