2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis c-Myc
  4. TZ1104

TZ1104 是一种基于 PROTAC 的 CDK7 降解剂。TZ1104 可与 VHL E3 连接酶和 CDK7 形成三元复合物，触发蛋白酶体依赖的 CDK7 降解，使 CDK7-cyclin H-MAT1 复合物不稳定。TZ1104 可抑制 RNA 聚合酶 II CTD Ser5、CDK1 Thr161 和 CDK2 Thr160 的磷酸化。TZ1104 可激活 p53-p21 轴，并可抑制致癌 Myc 信号通路。TZ1104 可诱导急性白血病细胞发生细胞周期阻滞、凋亡 (apoptosis) 和分化。TZ1104 可用于急性白血病的研究。
(粉色: CDK7 配体 (HY-183071)；蓝色: Ligands for E3 Ligase 和 VHL 配体 (HY-112078)；黑色: 连接子 (HY-W108876))。

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TZ1104

TZ1104 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

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Customer Review

TZ1104 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

TZ1104 is a PROTAC-based CDK7 degrader. TZ1104 forms a ternary complex with VHL E3 ligase and CDK7 to trigger proteasome-dependent CDK7 degradation, destabilizing the CDK7-cyclin H-MAT1 complex. TZ1104 suppresses phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. TZ1104 activates the p53-p21 axis and suppresses oncogenic Myc signaling. TZ1104 induces cell cycle arrest, apoptosis, and differentiation of acute leukemia cells. TZ1104 can be used for the research of acute leukemia[1].


(Pink: CDK7 ligand (HY-183071); Blue: Ligands for E3 Ligase and VHL ligand (HY-112078); Black: linker (HY-W108876)).

IC50 & Target[1]

CDK7/Cyclin H/MAT1

 

体外研究
(In Vitro)

TZ1104 (0.1-10 nM；6 小时) 是一种高效的 CDK7 降解剂，在 MV4-11 细胞中实现了 4.92 nM 的半数降解浓度 (DC50) 和 98.87% 的最大降解率 (Dmax)[1]。
TZ1104 (72 小时) 在多种急性白血病细胞系中均表现出强效且广泛的 CDK7 降解作用，包括 AML（Molm13、THP-1、HL60、CESS）和 ALL（RS4;11）模型[1]。
TZ1104 在人外周血单核细胞 (PBMC) 中表现出显著增强的抗增殖作用，同时保持了最小的细胞毒性[1]。

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

TZ1104 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.1 nM; 1 nM; 10 nM
Incubation Time: 6 h
Result: Emerged as a potent CDK7 degrader and achieved a half degradation concentration (DC50) of 4.92 nM and a maximum degradation (Dmax).
体内研究
(In Vivo)

TZ1104 (50 mg/kg；腹腔注射；每日 2 次；持续 26 天) 可实现肿瘤选择性 CDK7 降解，并抑制 Nu/Nu 小鼠体内 MV4-11 异种移植瘤的生长[1]。

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

Animal Model: Nu/Nu (female; 6-8 weeks old; implanted subcutaneously in
the right flank with 5 × 106 MV4-11 cells for a MV4-11 subcutaneous xenograft model)[1]
Dosage: 50 mg/kg
Administration: i.p.; twice daily; 26 days
Result: Reduced tumor weight relative to vehicle control.
Induced robust CDK7 degradation in tumor tissues.
Caused no significant CDK7 reduction in PBMCs.
Caused no observable body weight loss during treatment.
分子量

992.69

Formula

C49H66ClN9O7S2
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

TZ1104 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:

TZ1104TZ 1104TZ-1104CDKApoptosisc-MycCyclin dependent kinaseMycproteasomeRNA polymerase II CTD Ser5cyclin HCDK2 Thr160VHL E3 ligaseCDK1 Thr161CDK7xenograft modelsMAT1acute leukemia cellsInhibitorinhibitorinhibit

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目录号：
HY-183073
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