2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. Reactive Oxygen Species (ROS) Apoptosis p38 MAPK CDK Caspase Bcl-2 Family
  4. FKA-9i

FKA-9i 是一种口服有效的抗癌剂。FKA-9i 可直接结合并促进 LRPPRC (kd: 7.387 μM)、YBX1 (kd: 16.52 μM) 与 RPN1 (kd: 26.82 μM) 癌蛋白降解。FKA-9i 可抑制 MAPK 信号通路及线粒体氧化磷酸化。FKA-9i 也能够诱导癌细胞周期阻滞、凋亡 (apoptosis)、线粒体功能障碍和 ROS 积累。FKA-9i 可用于胃癌等肿瘤的研究。

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FKA-9i

FKA-9i Chemical Structure

CAS No. : 3060515-85-4

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FKA-9i 相关抗体

Top Publications Citing Use of Products

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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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

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FKA-9i is an orally active anticancer agent. FKA-9i directly binds to and promotes the degradation of oncoproteins LRPPRC (kd: 7.387 μM), YBX1 (kd: 16.52 μM) and RPN1 (kd: 26.82 μM). FKA-9i inhibits the MAPK signaling pathway and mitochondrial oxidative phosphorylation. FKA-9i also induces cancer cell cycle arrest, apoptosis, mitochondrial dysfunction and ROS accumulation. FKA-9i can be used in the research of tumors such as gastric cancer[1].

IC50 & Target[1]

CDK1

 

Caspase 3

 

Bcl-2

 

体外研究
(In Vitro)

FKA-9i (0-72 h) 可抑制 HGC27、KYSE70、KYSE450、HCT116 和 A549 癌细胞的增殖，其 IC50 值分别为 1.49、3.15、2.25、3.53 和 4.48 μM[1]。
FKA-9i (0-8 μM；0-48 h) 可抑制肿瘤细胞增殖，诱导细胞周期阻滞和凋亡[1]。
FKA-9i (0-8 μM；0-48 h) 会降低 HGC27 细胞中 LRPPRC、YBX1 和 RPN1 蛋白的稳定性，促进其降解[1]。
FKA-9i (48 h) 在 HGC27 细胞中抑制 MAPK 信号通路相关基因的表达，抑制 MAPK 级联反应[1]。
FKA-9i (4-8 μM; 48 h) 在 HGC27 和 HCT116 细胞中剂量依赖性地增加细胞内 ROS 水平[1]。

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

FKA-9i 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HGC27, KYSE450, HCT116
Concentration: 0, 2, 4 and 8 μM
Incubation Time: 48 h
Result: Induced G1 phase arrest in HGC27 and HCT116 cells, and S phase arrest in KYSE450 cells.
Downregulated cell cycle regulators CCND1 and CDK1.

Western Blot Analysis[1]

Cell Line: HGC27, KYSE450, HCT116
Concentration: 0, 2, 4 and 8 μM
Incubation Time: 48 h
Result: Reduced protein expression levels of caspase-3 and anti-apoptotic protein Bcl-2.
体内研究
(In Vivo)

FKA-9i (2.5-5 mg/kg；灌胃；31 天) 在 HGC27 CDX 小鼠模型中展现出抗肿瘤活性[1]。
FKA-9i (100-200 mg/kg；灌胃；10 天) 在 C57BL/6 小鼠中未表现出明显的急性器官毒性[1]。

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

Animal Model: BALB/c-nu nude mice (female, 6-week-old) treated HGC27 cells[1]
Dosage: 2.5 mg/kg/day; 5 mg/kg/day
Administration: Oral gavage; 31 days
Result: Reduced mean tumor volume, tumor number, and tumor weight.
Showed no significant differences in body weight compared to the control group.
Animal Model: C57BL/6 mice (male, 8-week-old)[1]
Dosage: 100 mg/kg/day; 200 mg/kg/day
Administration: Oral gavage; 10 days
Result: Showed no significant differences in body weight organ weights compared to the control group.
Observed no histopathological changes (H&E staining of liver and kidney tissues) compared to the control group.
分子量

660.66

Formula

C30H26F2N2O9S2
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

FKA-9i 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:

FKA-9i3060515-85-4Reactive Oxygen Species (ROS)Apoptosisp38 MAPKCDKCaspaseBcl-2 FamilyCyclin dependent kinaselung cancerLRPPRCcolon cancerHGC27MAPKYBX1gastric cancerInhibitorinhibitorinhibit

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