2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. CDK HDAC Apoptosis
  4. CDK9/HDAC1/HDAC3-IN-1

CDK9/HDAC1/HDAC3-IN-1 是 CDK9 和 HDAC 的双功能抑制剂。CDK9/HDAC1/HDAC3-IN-1 可抑制 CDK9/HDAC/HDAC3 的蛋白活性，对 CDK9、HDAC1 和 HDAC3 的 IC50 分别为 0.17 μM、1.73 μM 和 1.11 μM。CDK9/HDAC1/HDAC3-IN-1 通过诱导细胞凋亡 (apoptosis) 和细胞周期停滞于 G2/M 期来抑制癌细胞，并在小鼠 TNBC MDA-MB-231 异种移植模型中抑制肿瘤生长。CDK9/HDAC1/HDAC3-IN-1 具有广谱抗癌活性，例如乳腺癌、宫颈癌和肝癌。

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CDK9/HDAC1/HDAC3-IN-1 Chemical Structure

CDK9/HDAC1/HDAC3-IN-1 Chemical Structure

CAS No. : 2197029-81-3

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CDK9/HDAC1/HDAC3-IN-1 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC50 s of 0.17  μM, 1.73  μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer[1].

IC50 & Target

CDK9

0.17 μM (EC50)

HDAC1

1.73 μM (IC50)

HDAC3

1.11 μM (IC50)

体外研究
(In Vitro)

CDK9/HDAC1/HDAC3-IN-1 (Compound 13EA) (24 小时) 在多种癌细胞系中表现出强效的抗增殖活性 (例如：对 HeLa、MDA-MB-231 和 HepG2 的 IC50 分别为 1.51 μM、2.47 μM 和 4.52 μM) [1]。
CDK9/HDAC1/HDAC3-IN-1（MDA-MB-231 细胞：0.625-5 μM，HeLa 细胞：0.625-1.25 μM，24 小时）以时间和剂量依赖性方式抑制 MDA-MB-231 细胞中 p-Ser2 的 mRNA 表达[1]。
CDK9/HDAC1/HDAC3-IN-1（MDA-MB-231 细胞：0.625-5 μM，24 小时）显著降低 MDA-MB-231 细胞和 Hela 细胞中 p-Ser2 (CDK9 底物) 的蛋白表达，同时增加 Ac-H3 (HDAC 底物) 的蛋白表达[1]。
CDK9/HDAC1/HDAC3-IN-1 (0.625-5 μM，24 小时) 浓度依赖性地诱导线粒体相关细胞凋亡，增加裂解 PARP 的表达，并使 MDA-MB-231 细胞和 Hela 细胞中的细胞周期停滞在 G2/M 期[1]。

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

CDK9/HDAC1/HDAC3-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells, HeLa cells
Concentration: MDA-MB-231 cells (0.625, 1.25, 2.5, 5 μM), HeLa cells (0.625, 1.25 μM)
Incubation Time: 24 h
Result: Dose-dependently suppressed p-Ser2 (substrate of CDK9) level and upregulated Ac-H3 (substrate of HDAC) level.

Real Time qPCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.625, 1.25, 2.5, 5 μM
Incubation Time: 3, 6, 12, 24 h
Result: Time- and dose-dependently downregulated CDK9 mRNA with maximal suppression at 24 h.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells, HeLa cells
Concentration: 3  μM
Incubation Time: 24 h
Result: Diminished p-Ser2 level and upregulated Ac-H3 level in both HeLa and MDA-MB-231 cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells, HeLa cells
Concentration: 2.5 μM/3  μM
Incubation Time: 24 h
Result: Dose-dependently decreased protein expression of Bcl-2 and Mcl-1 in MDA-MB-231 cells, and escalated protein expression of cleaved PARP in MDA-MB-231 cells and Hela cells.
Dose-dependently increased the percentage of apoptotic cells induced, ranging from 11.30 % (0.31 μM) up to 77.38 % (2.5  μM) by Annexin V-FITC/PI staining assay (HY-K1073).
Concentration-dependently decreased the mitochondrial membrane potential (MMP, Δψ) in the MDA-MB-231 cells with 17.06 %, 26.83 %, 41.97 %, and 52.73 % loss of Δψ for concentrations of 0.31, 0.63, 1.35, and 2.5  μM, respectively.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.31, 0.63, 1.35, and 2.5 μM
Incubation Time: 24 h
Result: Significant increased the number of cells in the G2/M phase [ (27.43 % (0.31 μM), 79.47 % (0.63 μM), 47.58 % (1.25 μM), and 42.20 % (2.5 μM) ], and gradually promoted cells in the sub-G1 phase [(3.00 % (0.31 μM), 7.64 % (0.63 μM), 23.89 % (1.25 μM), and 27.94 % (2.5 μM)].
体内研究
(In Vivo)

CDK9/HDAC1/HDAC3-IN-1 (30 mg/kg，腹腔注射，每日一次，持续 10 天) 显著抑制 MDA-MB-231 小鼠异种移植模型中的肿瘤生长[1]。

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

Animal Model: female BALB/c nude mice (6 weeks old) were injected subcutaneously with log growth-phase of MDA-MB-231 cells (3 × 107 cells/mouse) [1].
Dosage: 30 mg/kg
Administration: i.p., once a day for 10 days after tumors reaching approximately 100 mm3.
Result: Time-dependently inhibited MDA-MB-231 xenograft tumor growth and remarkably reduced the tumor volume.
Notably increased cleaved caspase-3 level, and decreased PCNA level in the tumor tissue with IHC staining.
分子量

470.55

Formula

C24H22N8OS
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

CDK9/HDAC1/HDAC3-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

CDK9/HDAC1/HDAC3-IN-12197029-81-3CDKHDACApoptosisCyclin dependent kinaseHistone deacetylasesDual-functional inhibitorsAnticancerTNBC MDA-MB-231 xenograft modelHeLaMDA-MB-231HepG2 cellsInhibitorinhibitorinhibit

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