2. JAK/STAT Signaling Stem Cell/Wnt Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  3. STAT Carbonic Anhydrase Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Caspase Bcl-2 Family
  4. STAT3/CAIX-IN-1

STAT3/CAIX-IN-1 是 STAT3 (Kd：60.03 μM) 和 CAIX (IC50：80.45 nM) 的双靶点抑制剂。STAT3/CAIX-IN-1 通过增加活性氧 (ROS) 和脂质过氧化物的水平来诱导铁死亡 (ferroptosis)。STAT3/CAIX-IN-1 抑制细胞迁移，诱导细胞凋亡 (apoptosis)，并导致 MDA-MB-231 细胞周期停滞。STAT3/CAIX-IN-1 可用于三阴性乳腺癌 (TNBC) 的研究。

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STAT3/CAIX-IN-1 Chemical Structure

STAT3/CAIX-IN-1 Chemical Structure

CAS No. : 3053583-60-8

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STAT3/CAIX-IN-1 相关抗体

Top Publications Citing Use of Products

查看 STAT 亚型特异性产品:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

查看 Carbonic Anhydrase 亚型特异性产品:

查看所有亚型
CA CA I CA Ⅱ CA IX CA XII

查看 Caspase 亚型特异性产品:

查看所有亚型
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

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC)[1].

IC50 & Target

CA IX

80.45 nM (IC50)

hCA VB

25.40 nM (IC50)

hCA II

349.30 nM (IC50)

STAT3

60.03 μM (Kd)

体外研究
(In Vitro)

STAT3/CAIX-IN-1 (compound 7m) (2-8 μM，24 小时) 可抑制 MDA-MB-231 细胞中的 STAT3 磷酸化[1]。

STAT3/CAIX-IN-1 (4 μM) 可与 STAT3 结合并增强其稳定性[1]。

STAT3/CAIX-IN-1 可增强肿瘤细胞系的增殖抑制，在 MDA-MB-231 细胞系中，IC50 分别为 2.18 μM (缺氧)和 4.21 μM (常氧) [1]。

STAT3/CAIX-IN-1 (4 μM，8 μM，24 小时) 通过 GPX4 通路诱导铁死亡，增加活性氧水平，上调 MDA-MB-231 细胞内脂质过氧化[1]。

STAT3/CAIX-IN-1 (2 μM M, 4 μM, 24-48 h) 抑制 MDA-MB-231 细胞迁移[1]。

STAT3/CAIX-IN-1 (4 μM, 8 μM, 24 h) 诱导 MDA-MB-231 细胞凋亡，并诱导 MDA-MB-231 细胞周期停滞于 G1/S 期[1]。

STAT3/CAIX-IN-1 具有抗肿瘤活性，IC50 为 4.21 μM (MDA-MB-231)、5.67 μM (MCF-7)、6.60 μM (MDA-MB-231/ADR)、14.19 μM (MCF-10A)[1]。

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

STAT3/CAIX-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2, 4, 8 μM
Incubation Time: 24 h
Result: Inhibited the levels of pSTAT3-S727 and pSTAT3-Y705.
No changed p-JAK1 levels.
Reduced GPX4 levels.
Downregulated the expression of Bcl-2 and Cyclin D1.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 4, 8 μM
Incubation Time: 24 h
Result: Accumulated in G1 phase cells, downregulated S phase cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 4, 8 μM
Incubation Time: 24 h
Result: Induced apoptosis in MDA-MB-231 cells.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells
Concentration: 2, 4, 8 μM
Incubation Time: 24 h, 48 h
Result: Reduced mobility.
体内研究
(In Vivo)

STAT3/CAIX-IN-1 (compound 7m) (5 mg/kg、10 mg/kg，48 小时) 表现出抗肿瘤活性，总应答率为 75%，且不改变体重或行为[1]。

STAT3/CAIX-IN-1 (10 mg/kg，腹腔注射，21 天，每 2 天一次) 可降低 Balb/c 裸鼠异种移植实验中磷酸化 STAT3 的表达[1]。

STAT3/CAIX-IN-1 (5 mg/kg、10 mg/kg，腹腔注射，21 天，每 2 天一次) 可抑制移植有 MDA-MB-231 异种移植瘤的 Balb/c 裸鼠的肿瘤生长[1]。

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

Animal Model: Balb/c nude mice with MDA-MB-231 xenograft tumors[1].
Dosage: 10 mg/kg
Administration: i.p.,21 days, every 2 days
Result: Reduced the fluorescence intensity of pSTAT3-S727 (green fluorescence) and pSTAT3-Y705 (red fluorescence).
分子量

687.63

Formula

C28H23F6N5O5S2
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

STAT3/CAIX-IN-1 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:

STAT3/CAIX-IN-13053583-60-8STATCarbonic AnhydraseFerroptosisApoptosisReactive Oxygen Species (ROS)CaspaseBcl-2 FamilyCarbonate dehydrataseSTAT3CAIXGPX4anti-tumorMDA-MB-231 cellsferroptosisBcl-2Inhibitorinhibitorinhibit

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