2. Cell Cycle/DNA Damage Apoptosis PI3K/Akt/mTOR
  3. Zinc Finger Protein Apoptosis PI3K Akt
  4. PLAGL2-IN-1

PLAGL2-IN-1 是一种多形性腺瘤样蛋白 2 (PLAGL2) 抑制剂，其 Kd 值为 2.23 µM。PLAGL2-IN-1 可抑制 PLAGL2 的转录活性，诱导 G0/G1 期细胞周期阻滞和细胞凋亡 (apoptosis)，从而抑制肝细胞癌 (HCC) 细胞增殖。PLAGL2-IN-1 可破坏细胞外基质结构，并通过降低 AKT 磷酸化水平抑制 PI3K-AKT 信号通路。PLAGL2-IN-1 可抑制 HCCLM3 异种移植小鼠模型中的肿瘤生长。PLAGL2-IN-1 可用于肝细胞癌的研究。

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PLAGL2-IN-1

PLAGL2-IN-1 Chemical Structure

CAS No. : 3099026-16-8

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PLAGL2-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PLAGL2-IN-1 is a inhibitor of pleiomorphic adenoma-like protein 2 (PLAGL2) with a Kd of 2.23 µM. PLAGL2-IN-1 suppresses PLAGL2 transcriptional activity, induces G0/G1 cell cycle arrest, and apoptosis, thereby inhibiting hepatocellular carcinoma (HCC) cell proliferation. PLAGL2-IN-1 disrupts extracellular matrix organization and suppresses the PI3K-AKT pathway by reducing AKT phosphorylation. PLAGL2-IN-1 inhibits tumor growth in an HCCLM3 xenograft mouse model. PLAGL2-IN-1 can be used for the research of HCC[1].

IC50 & Target[1]

PLAGL2

2.23 μM (Kd)

体外研究
(In Vitro)

PLAGL2-IN-1 (compound C8) (72 小时) 在一系列癌细胞中表现出广谱抗增殖活性，其 IC50 值分别为：0.96 (A549)、1.35 (NCI-H1650)、1.03 (NCI-H460)、3.31 (MGC803)、3.28 (HGC27)、7.63 (SW620)、0.92 (HT29)、1.64 (MDA-MB-231)、2.21 (HCC1937)、1.43 (U87-MG)、24.96 (LN229)、8.83 (U937)、5.67 (K562)、5.33 (MEG01)、19.54 (Jurkat)、4.14 (PC-3) 和 16.19 μM (SKOV3)[1]。
PLAGL2-IN-1 (0-1 μM，14 天) 以浓度依赖的方式抑制 MHCC-97H 和 HCCLM3 细胞的集落形成[1]。
PLAGL2-IN-1 (10 μM，48 小时) 可诱导 MHCC-97H 和 HCCLM3 细胞凋亡[1]。
PLAGL2-IN-1 (5 μM，24 小时) 可诱导 MHCC-97H 细胞发生 G0/G1 期阻滞[1]。
PLAGL2-IN-1 (0-10 μM，48 小时) 以剂量依赖的方式抑制 HCCLM3 和 MHCC-97H 细胞的迁移和侵袭，对 HCCLM3 肝癌细胞的细胞分裂表现出显著的抑制作用[1]。
PLAGL2-IN-1 (5-10 μM，24-48 小时) 在 HCCLM3 细胞中破坏细胞外基质组织，并通过降低 AKT 磷酸化来抑制 PI3K-AKT 通路[1]。

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

PLAGL2-IN-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MHCC-97H and HCCLM3
Concentration: 0, 0.01, 0.1, 1 μM
Incubation Time: 14 days
Result: Resulted in a marked reduction incolony formation.
Showed concentration-dependent inhibition in both cells.

Apoptosis Analysis[1]

Cell Line: MHCC-97H and HCCLM3
Concentration: 10 μM
Incubation Time: 48 h
Result: Induced late-stage apoptosis in both cells.
Exhibited stronger pro-apoptotic effects than the 5μM 5-FU (HY-90006) positive control.

Cell Cycle Analysis[1]

Cell Line: MHCC-97H and HCCLM3
Concentration: 5 μM
Incubation Time: 24 h
Result: Induced G0/G1 phase arrest in MHCC-97H cells.
Did not induce cell cycle arrest in HCCLM3 cells.

Cell Migration Assay [1]

Cell Line: MHCC-97H and HCCLM3
Concentration: 0, 5, 10 μM
Incubation Time: 48 h
Result: Showed a dose-dependent inhibition of cell wound healing in HCCLM3 and MHCC-97H cells.
Inhibited cell migration in HCCLM3 and MHCC-97H cells.

Cell Invasion Assay[1]

Cell Line: MHCC-97H and HCCLM3
Concentration: 0, 5, 10 μM
Incubation Time: 48 h
Result: Inhibited cell invasion in HCCLM3 and MHCC-97H cells in a dose-dependent manner.

Immunofluorescence[1]

Cell Line: HCCLM3
Concentration: 5 μM
Incubation Time: 48 h
Result: Reduced the protein expression levels Vimentin.
Increased E-cadherin expression.

Western Blot Analysis[1]

Cell Line: HCCLM3
Concentration: 5, 10 μM
Incubation Time: 48 h
Result: Reduced theprotein expression levels of ZEB1, Vimentin, MMP2, and MMP9.
Increased E-cadherin expression.
Significantly inhibited PLAGL2-dependent AKT phosphorylation at both Thr308 and Ser473.
体内研究
(In Vivo)

PLAGL2-IN-1 (compound C8) (15 mg/kg，腹腔注射，每日一次，持续 19 天) 在 HCCLM3 异种移植小鼠模型中显著抑制肿瘤生长，且无明显毒性[1]。

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

Animal Model: Male BALB/C nude mice (6-8 weeks old) subcutaneously injected with HCCLM3 cells[1]
Dosage: 15 mg/kg
Administration: i.p., daily for 19 days
Result: Effectively inhibited tumor growth, with a TGI of 63.27%.
Significantly reduced tumor weight and volume.
Showed no observable toxicity in major organs but induced noticeable tumornecrosis.
Reduced expression of Ki-67 and α-SMA in tumor tissues.
Demonstrated a stable body weight during administration.
分子量

632.60

Formula

C30H35Cl2N5O4S
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

PLAGL2-IN-1 相关分类

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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:

PLAGL2-IN-13099026-16-8Zinc Finger ProteinApoptosisPI3KAktPhosphoinositide 3-kinasePKBProtein kinase B3-(Phenylsulfonamido) benzamide derivativesHepatocellular carcinomaStructural optimizationPLAGL2Inhibitorinhibitorinhibit

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