2. PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. PI3K HDAC Bcl-2 Family Caspase Reactive Oxygen Species (ROS)
  4. PI3Kδ/HDAC6-IN-1

PI3Kδ/HDAC6-IN-1 是 PI3Kδ 和 HDAC6 口服有效的双重有效抑制剂， IC50 值分别为 2.4 nM 和 6.2 nM。PI3Kδ/HDAC6-IN-1 对非霍奇金淋巴瘤 (NHL) 细胞表现出强大的抗增殖作用，并具有体内抗肿瘤活性且无明显毒性。PI3Kδ/HDAC6-IN-1 将细胞周期阻滞于 G0/G1 期，并诱导细胞凋亡(apoptosis)。PI3Kδ/HDAC6-IN-1 阻断 PI3K/AKT/mTOR 信号通路，并增加 α-微管蛋白和组蛋白 H3 的乙酰化水平。

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PI3Kδ/HDAC6-IN-1 Chemical Structure

PI3Kδ/HDAC6-IN-1 Chemical Structure

CAS No. : 3075011-99-0

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PI3Kδ/HDAC6-IN-1 相关抗体

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 HDAC 亚型特异性产品:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3Kδ/HDAC6-IN-1 is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3[1].

IC50 & Target

PI3Kδ

2.4 nM (IC50)

HDAC6

6.2 nM (IC50)

体外研究
(In Vitro)

PI3Kδ/HDAC6-IN-1 (Compound 22E) (浓度为 0.1 nM -10 μM，24-120 小时) 对 PI3Kδ 和 HDAC6 均有抑制活性，IC50 分别为 2.4 nM 和 6.4 nM，并对 JEKO-1 细胞表现出抗增殖活性[1]。

PI3Kδ/HDAC6-IN-1 (浓度为 10-30 μM，45-85 °C) 可提高 PI3Kδ 和 HDAC6 的热稳定性[1]。

PI3Kδ/HDAC6-IN-1 (浓度为 0.1-10 μM， 4 天) 抑制 NHL 细胞的增殖，IC50 值分别为 34 nM (SU-DHL-6 细胞) 和 53 nM (JEKO-1细胞)[1]。

PI3Kδ/HDAC6-IN-1 (.3-9 μM，24 小时) 可诱导 SU-DHL-6 和 JEKO-1 细胞发生 G0/G1 期阻滞[1]。

PI3Kδ/HDAC6-IN-1 (3-9 μM，72 小时) 可诱导 SU-DHL-6 和 JEKO-1 细胞发生浓度依赖性的细胞凋亡 (nexin V 阳性)[1]。

PI3Kδ/HDAC6-IN-1 (3-9 μM，12 小时) 在细胞水平上抑制 SU-DHL-6 和 JEKO-1 细胞中的 PI3K 和 HDAC 相关蛋白[1]。

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

PI3Kδ/HDAC6-IN-1 相关抗体:

Cell Cycle Analysis[1]

Cell Line: SU-DHL-6 and JEKO-1 cells
Concentration: 0.3 μM, 1 μM, 3 μM, 9 μM
Incubation Time: 24 h
Result: Increased the ratio of cells in G0/G1 phase, blocked cancer cells in the G0/G1 phase.
Downregulated cyclin D1, cyclin E1, CDK6, CDK4, and CDK2 proteins.

Apoptosis Analysis[1]

Cell Line: SU-DHL-6 and JEKO-1 cells
Concentration: 0.3 μM, 1 μM, 3 μM, 9 μM
Incubation Time: 72 h
Result: Induced Annexin V positivity, downregulated the anti-apoptotic protein BCL-2, increased levels of cleaved PARP and cleaved caspase-3.
Induced a concentration-dependent increase in the ROS-positive cell count in JEKO-1 cells.

Western Blot Analysis[1]

Cell Line: SU-DHL-6 and JEKO-1 cells
Concentration: 0.3 μM, 1 μM, 3 μM, 9 μM
Incubation Time: 12 h
Result: Inhibited hosphorylation of downstream signaling proteins of PI3K, including AKT, P70S6K, and 4EBP1, as well as the oncogene-encoded protein c-MYC, while having no effect on total protein levels.
Increased histone H3 and α-tubulin acetylation levels.
体内研究
(In Vivo)

PI3Kδ/HDAC6-IN-1 (Compound 22E) (25 mg/kg，口服，每日一次，21 天) 具有抗肿瘤潜力，可抑制 NOD-SCID 小鼠 SU-DHL-6 和 JEKO-1 肿瘤异种移植模型中的 PI3K 通路和 HDAC 相关蛋白[1]。

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

Animal Model: SU-DHL-6 and JEKO-1 tumor xenograft models in NOD-SCID mice[1]
Dosage: 25 mg/kg
Administration: p.o., 21 days
Result: Reduced tumor growth, exhibited antitumor activity, with corresponding TGI rates of 69.42 % in the SU-DHL-6 model and 67.56 % in the JEKO-1 model.
Reduced p-AKT levels and increased acetyl-α-tubulin levels, reduced Ki-67 levels and increased cleaved caspase-3 levels.
分子量

650.73

Formula

C34H38N10O4
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

PI3Kδ/HDAC6-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

PI3Kδ/HDAC6-IN-13075011-99-0PI3KHDACBcl-2 FamilyCaspaseReactive Oxygen Species (ROS)Phosphoinositide 3-kinaseHistone deacetylasesInhibitorSU-DHL-6 cellsJEKO-1 cellsapoptosisSU-DHL-6 and JEKO-1 tumor xenograft modelsinhibitorinhibit

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