2. PROTAC Cell Cycle/DNA Damage Apoptosis Epigenetics
  3. PROTACs CDK Caspase PARP Apoptosis
  4. dCDK9-202

dCDK9-202 是一种强效的 CDK9 PROTAC 降解剂，其 DC50 值为 3.5 nM。dCDK9-202 具有广谱抗肿瘤活性，并能广泛破坏致癌转录组。dCDK9-202 可激活 Caspase-3/7，增加裂解型 PARP 的水平，并直接诱导肿瘤细胞凋亡 (apoptosis)。dCDK9-202 能有效抑制 TC-71 肿瘤的生长，且在小鼠体内未观察到任何毒性反应。dCDK9-202 可用于研究 EGFR 驱动的癌症，例如肉瘤 (粉色：CDK9 配体 (HY-178862)；蓝色：CRBN 配体 (HY-W248665)；黑色：连接子 (HY-N8015))。

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dCDK9-202

dCDK9-202 Chemical Structure

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dCDK9-202 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 PARP 亚型特异性产品:

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015))[1].

IC50 & Target[1]

CDK9

3.5 nM (DC50)

Caspase-3

 

Caspase-7

 

Cereblon

 

体外研究
(In Vitro)

dCDK9-202 (10 nM, 0-24 h) 在 TC-71 细胞 2 小时内可显著降低 CDK9 蛋白水平，并在 8 小时内实现完全且几乎持续的降解[1]。
dCDK9-202 (0.1 nM-1 μM, 24 h) 在 12 种源自肺、肝、骨和脑等不同组织的癌细胞系中表现出纳摩尔级的增殖抑制活性。例如，在 TC-71 细胞中，IC₅₀ 为 8.5 nM[1]。
dCDK9-202 (10-50 nM，24 h) 激活 Caspase-3/7，增加 PARP 裂解水平，并直接诱导 TC-71 细胞凋亡[1]。
dCDK9-202 (0.25-25 nM，6 h) 显著降低 RNA 聚合酶 II CTD 结构域 Ser2 的磷酸化水平 (p-Rpb1 Ser2)，并下调多种受 CDK9 调控且与 TC-71 细胞癌变密切相关的短半衰期蛋白[1]。

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

dCDK9-202 相关抗体:

Western Blot Analysis[1]

Cell Line: TC-71 cells
Concentration: 10 and 50 nM
Incubation Time: 24 h
Result: Activated Caspase-3/7, increased the level of cleaved PARP.

Western Blot Analysis[1]

Cell Line: TC-71 cells
Concentration: 0.25, 2.5 and 25 nM
Incubation Time: 6 h
Result: Significantly reduced the phosphorylation of Ser2 in the CTD domain of RNA polymerase II (p-Rpb1 Ser2).
Strongly down-regulated a variety of short half-life proteins that are regulated by CDK9 and are closely related to cancer occurrence, such as MYC, MCL1, BCL-xL, etc.
体内研究
(In Vivo)

dCDK9-202 (10 mg/kg，静脉注射，每隔一天一次，共 7 次) 可显著抑制 TC-71 细胞系建立的小鼠异种移植瘤模型中的肿瘤体积和重量[1]。

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

Animal Model: TC-71 cells xenografts model established in NCG mice (female, 6-8 weeks)[1]
Dosage: 10 mg/kg
Administration: Intravenous injection (i.v.), once every other days for 7 doses
Result: Significantly inhibited the tumor volume and weight.
Effectively reduced the level of CDK9 protein in tumor tissues after a single administration 2 hours later.
Did not show any weight loss or other obvious signs of toxicity in mice.
分子量

803.99

Formula

C40H49N7O7S2
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

dCDK9-202 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

dCDK9-202PROTACsCDKCaspasePARPApoptosisCyclin dependent kinasepoly ADP ribose polymerase PROTACCDK9 degraderTC-71 cell linein vivo antitumor activitykinase selectivitytranscriptional addictionInhibitorinhibitorinhibit

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