2. MAPK/ERK Pathway PI3K/Akt/mTOR NF-κB
  3. p38 MAPK PI3K Akt NF-κB
  4. A2073

A2073 是一种黄酮类衍生物，通过诱导细胞周期阻滞和抑制 MAPK、NF-κB 和 PI3K 信号通路抑制红白血病细胞的增殖。A2073与细胞周期相关蛋白 (CDK1、CCNA2、PRIM1) 形成稳定的相互作用。在斑马鱼异种移植肿瘤模型中，A2073 展现出显著的抗肿瘤细胞增殖活性，同时保持较低的毒性。A2073 可用于急性红白血病的研究[1]。

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A2073 Chemical Structure

A2073 Chemical Structure

CAS No. : 2834742-70-8

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A2073 相关抗体

Top Publications Citing Use of Products

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways.A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia[1].

体外研究
(In Vitro)

A2073 (25-100 nM, 24-72 h) 以剂量和时间依赖的方式显著抑制HEL和K562细胞的增殖，IC50值分别为55.02 nM (HEL) 和 77.07 nM (K562)[1]。

A2073 (25-100 nM, 24-72 h) 减少HEL细胞数量但不显著增加凋亡，诱导HEL细胞红系分化 (表现为 CD71 表达增加)，并引起细胞周期阻滞，同时下调关键细胞周期调控蛋白[1]。

A2073 (25-100 nM, 48 h) 下调 MAPK (RAS、RAF、MAPK、MEK、PI3K-AKT (PI3K、AKT) 和 NF-κB (p-NF-κB、p-IκBα) 通路中的关键蛋白[1]。

A2073与细胞周期相关蛋白 (CDK1、CCNA2、PRIM1) 形成稳定的相互作用[1]。

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

A2073 相关抗体:

Cell Viability Assay[1]

Cell Line: HEL cells
Concentration:
Incubation Time: 72 h
Result: Reduced HEL cell numbers more effectively than Cytarabine (Ara-C) (HY-13605), with a lower IC50 (55.02 nM vs. 73.36 nM)

RT-PCR[1]

Cell Line: HEL cells
Concentration: 100 nM
Incubation Time: 48 h
Result: Increased the expression levels of erythroid differentiation markers GATA1, EKLF, SHIP1, and NFE2.

Cell Cycle Analysis[1]

Cell Line: HEL cells
Concentration: 25, 50, 100 nM
Incubation Time: 24, 48, 72 h
Result: Caused cell cycle arrest in the G0 and G2 phases, reduces the proportion of cells in the S phase.

Western Blot Analysis[1]

Cell Line: HEL cells
Concentration: 25, 50, 100 nM
Incubation Time: 48 h
Result: Downregulatesd key cell cycle regulatory proteins including CMYC, CDK1, CDK2, CCNB1, and CCNA2.
体内研究
(In Vivo)

A2073 (25-100 nM，1-5 days) 在斑马鱼异种移植肿瘤模型中有效抑制 HEL 细胞的增殖[1]。

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

Animal Model: CM-Dil dye-labeled HEL cells into zebrafish embryos at 48 h post-fertilizations[1]
Dosage: 25, 50, 100 nM
Administration: 1, 3, 5 days
Result: Showed no significant morphological abnormalities (morphology, survival, body length, and heart rate) at any examined time points (1, 3, 5 days) compared to the control group.
Did not induce significant in vivo toxicity in zebrafish embryos.Reduced HEL cell proliferation and migration.
Inhibited the proliferation of HEL cells in the zebrafish xenograft tumor model.
分子量

559.65

Formula

C33H37NO7
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

A2073 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

A20732834742-70-8A 2073A-2073p38 MAPKPI3KAktNF-κBPhosphoinositide 3-kinasePKBProtein kinase BNuclear factor-κBNuclear factor-kappaBNatural compoundsErythroleukemiaCell cyclePI3K pathwayMAPK pathwayNF-κB pathwayInhibitorinhibitorinhibit

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