2. Membrane Transporter/Ion Channel PI3K/Akt/mTOR Apoptosis
  3. GLUT PI3K Akt Apoptosis
  4. FKL-137

FKL-137 是一种 GLUT1 和 PI3K/AKT 信号通路抑制剂。FKL-137 可结合 GLUT1，降低葡萄糖摄取与乳酸分泌，下调糖代谢相关蛋白，并抑制红白血病细胞增殖。FKL-137 可下调 PI3K、p-PI3K、AKT、p-AKT 水平，破坏 PI3K/AKT-GLUT1 正反馈环路，进而抑制红白血病细胞增殖。FKL-137 可通过上调 Bax、Cleaved-PARP 并下调 Bcl-2、PARP 诱导细胞凋亡 (apoptosis)。FKL-137 可用于红白血病的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

FKL-137

FKL-137 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

FKL-137 相关抗体

Top Publications Citing Use of Products

查看 GLUT 亚型特异性产品:

查看所有亚型
GLUT1 GLUT2 GLUT3 GLUT4

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FKL-137 is a GLUT1 and PI3K/AKT signaling pathway inhibitor. FKL-137 binds to GLUT1, reduces glucose uptake and lactate secretion, downregulates glucose metabolism-related proteins, and inhibits erythroleukemia cell proliferation. FKL-137 downregulates PI3K, p-PI3K, AKT, p-AKT levels, disrupts the PI3K/AKT-GLUT1 positive feedback loop, and suppresses erythroleukemia cell proliferation. FKL-137 induces apoptosis via upregulated Bax, Cleaved-PARP and downregulated Bcl-2, PARP. FKL-137 can be used for the research of erythroleukemia[1].

IC50 & Target[1]

GLUT1

 

Akt

 

PI3K

 

体外研究
(In Vitro)

FKL-137 (0.001-10 μM；24-72 小时) 可强效抑制 HEL 和 K562 红白血病细胞的增殖；同时与 HepG2 肝癌细胞相比，其在正常 LX-2 肝细胞中表现出相对安全性[1]。
FKL-137 (0.1-0.4 μM；48 小时) 可在 HEL 和 K562 红白血病细胞中诱导凋亡性细胞核变化[1]。
FKL-137 (0.1-0.4 μM；48 小时) 可在 HEL 和 K562 红白血病细胞中诱导剂量依赖性凋亡，其中 K562 细胞在所有测试浓度下均检测到显著的凋亡细胞群，HEL 细胞则在 0.2-0.4 μM 浓度下检测到显著凋亡细胞群[1]。
FKL-137 (0.1-0.4 μM；48 小时) 通过上调 Bax 和 Cleaved-PARP、下调 Bcl-2 和 PARP，调控 HEL 和 K562 红白血病细胞中凋亡相关蛋白的表达[1]。
FKL-137 (0.1-0.4 μM；48 小时) 可下调 HEL 和 K562 红白血病细胞中糖代谢相关蛋白 HK2、PKM2 及 LDH 的表达[1]。
FKL-137 (0.1-0.4 μM；48 小时) 以剂量依赖方式下调 HEL 和 K562 红白血病细胞中 PI3K、p-PI3K、AKT 及 p-AKT 的蛋白水平[1]。
FKL-137 (0.1-0.4 μM；6-24 小时) 以剂量和时间依赖的方式抑制 HEL 和 K562 红白血病细胞的葡萄糖摄取和乳酸分泌，最早在 6 小时时即可观察到显著效应[1]。
FKL-137 (0.001-10 μM；2 小时) 可提高 K562 红白血病细胞中 GLUT1 的热稳定性，且在 0.01-1 μM 浓度下不会改变 GLUT1 的总蛋白水平[1]。
FKL-137 (0-0.6 μM；6 小时) 可抑制 K562 红白血病细胞中 GLUT1 介导的葡萄糖摄取，其 IC50 为 0.15 μM；且在高糖培养基中其抑制作用会减弱，证实其对 GLUT1 具有竞争性靶向作用[1]。
FKL-137 (0.1-0.4 μM) 可在体外以剂量依赖的方式降低 HEL 红白血病细胞中 GLUT1 的表达[1]。
FKL-137 (0.001-10 μM；48-72 小时) 在 72 小时时对 GLUT1 敲低的 K562 红白血病细胞表现出显著强于阴性对照细胞的、呈剂量和时间依赖性的抗增殖作用[1]。
FKL-137 (0.1-0.4 μM；6-24 小时) 可进一步抑制 GLUT1 敲低的 K562 红白血病细胞的葡萄糖摄取与乳酸分泌，且在 12 小时内即可检测到显著效应[1]。
FKL-137 (0.1-0.4 μM；48 小时) 可调控 GLUT1 敲低的 K562 红白血病细胞中代偿性上调的糖代谢相关蛋白 HK2 和 LDH 的表达[1]。

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

FKL-137 相关抗体:

Cell Viability Assay[1]

Cell Line: human erythroleukemia HEL cells, human erythroleukemia K562 cells, human normal hepatic stellate LX-2 cells, human hepatoma HepG2 cells
Concentration: 0.001 μM; 0.01 μM; 0.1 μM; 1 μM; 10 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Exerted significant, time- and dose-dependent inhibitory effects on HEL and K562 cell proliferation.
Achieved IC50 values of 0.6 μmol/L (24 h), 0.25 μmol/L (48 h), and 0.1 μmol/L (72 h) in HEL cells.
Achieved IC50 values of 0.8 μmol/L (24 h), 0.4 μmol/L (48 h), and 0.2 μmol/L (72 h) in K562 cells.
Exhibited hepatotoxicity safety index values of 1.65 (24 h), 1.66 (48 h), and 2.29 (72 h), indicating relative safety.

Apoptosis Analysis[1]

Cell Line: human erythroleukemia HEL cells, human erythroleukemia K562 cells
Concentration: 0.1 μM; 0.2 μM; 0.4 μM
Incubation Time: 48 h
Result: Induced characteristic apoptotic morphological changes including nuclear condensation, fragmentation, and chromatin margination in both HEL and K562 cells.
Showed effects increasing with compound concentration.\nCaused a dose-dependent increase in apoptotic cell populations in both cell lines.
Increased early and late apoptosis rates significantly at 0.2 μM and 0.4 μM in HEL cells.
Increased early and late apoptosis rates significantly at all tested concentrations, with the highest effects at 0.4 μM in K562 cells.

Western Blot Analysis[1]

Cell Line: human erythroleukemia HEL cells, human erythroleukemia K562 cells
Concentration: 0.1 μM; 0.2 μM; 0.4 μM
Incubation Time: 48 h
Result: Dose-dependently upregulated pro-apoptotic Bax and Cleaved-PARP protein expression in both HEL and K562 cells compared to DMSO controls.
Downregulated anti-apoptotic Bcl-2 and full-length PARP protein expression in both HEL and K562 cells compared to DMSO controls.\nDose-dependently downregulated the expression of glucose metabolism-related proteins HK2, PKM2, and LDH in both HEL and K562 cells compared to DMSO controls.\nDose-dependently downregulated the protein levels of PI3K, p-PI3K, AKT, and p-AKT in HEL and K562 cells.

Cell Viability Assay[1]

Cell Line: GLUT1-knockdown (shGLUT1) human erythroleukemia K562 cells
Concentration: 0.001 μM; 0.01 μM; 0.1 μM; 1 μM; 10 μM
Incubation Time: 48 h, 72 h
Result: Exerted dose- and time-dependent anti-proliferative effects on GLUT1-knockdown K562 cells.
Showed significantly stronger inhibitory activity at 72 h compared to negative control (NC) cells.

Western Blot Analysis[1]

Cell Line: GLUT1-knockdown (shGLUT1) human erythroleukemia K562 cells
Concentration: 0.1 μM; 0.2 μM; 0.4 μM
Incubation Time: 48 h
Result: Modulated the expression of compensatory upregulated glycolytic enzymes HK2 and LDH in GLUT1-knockdown K562 cells, where GLUT1 knockdown caused compensatory upregulation of HK2 and LDH.
体内研究
(In Vivo)

FKL-137 (1-10 mg/kg；腹腔注射；每 48 小时 1 次；共 7 次给药) 可剂量依赖性地升高 Fr-MuLV 诱导的红白血病小鼠的血细胞比容，减轻脾肿大并降低脏器系数，改善组织病理学损伤，降低脾脏葡萄糖和乳酸水平，同时下调代谢蛋白表达；其中 10 mg/kg 剂量的作用最为显著[1]。

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

Animal Model: BALB/c (8-10 week old male and female; Fr-MuLV-induced erythroleukemia model established at 6 weeks of age)[1]
Dosage: 1 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.p.; every 48 hours; 7 total doses
Result: Increased hematocrit to ~42% at 1 mg/kg, ~43% at 5 mg/kg, and ~55% at 10 mg/kg.
Reduced spleen weight to ~0.9 g at 1 mg/kg, ~0.4 g at 5 mg/kg, and ~0.2 g at 10 mg/kg.
Significantly reduced liver and spleen organ ratios across all doses; no significant changes to heart, lung, or kidney organ ratios were observed.
Significantly reduced pathological mitosis and tumor cell infiltration foci in spleen tissue across all doses compared to the model group.
Significantly reduced white blood cell infiltration in liver tissue across all doses compared to the model group; no significant histopathological changes were observed in heart, lung, or kidney tissues.
Reduced spleen glucose content to ~0.22 mmol/g and lactate content to ~0.28 mmol/g at 1 mg/kg; reduced spleen glucose content to ~0.12 mmol/g and lactate content to ~0.3 mmol/g at 5 mg/kg; reduced spleen glucose content to ~0.08 mmol/g and lactate content to ~0.3 mmol/g at 10 mg/kg.
Downregulated the expression of HK2 and LDH proteins in spleen tissue across all doses compared to the model group.
分子量

392.37

Formula

C20H19F3N2O3
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

FKL-137 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

FKL-137FKL137FKL 137GLUTPI3KAktApoptosisGlucose transporter Phosphoinositide 3-kinasePKBProtein kinase BLX-2 liver cellsK562 erythroleukemia cellsHEL erythroleukemia cellsPI3K/AKT signaling pathwayerythroleukemiaglucose metabolism-related proteinsapoptosisFriend virusHepG2 hepatoma cellsGLUT1Inhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
FKL-137
目录号：
HY-183069
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z