2. Anti-infection JAK/STAT Signaling Stem Cell/Wnt Metabolic Enzyme/Protease Apoptosis
  3. Parasite STAT Phosphatase MDM-2/p53 Apoptosis
  4. Fluacrypyrim

Fluacrypyrim 是一种酯类杀螨剂，同时也可作为 STAT3 抑制剂。Fluacrypyrim 显著提高蛋白质酪氨酸磷酸酶 (PTPs) 的活性。Fluacrypyrim 通过引发显著的 G1 期阻滞，并显著降低 cyclin D1 蛋白和 mRNA 水平，从而抑制白血病细胞生长。Fluacrypyrim 能够选择性抑制 STAT3 信号通路，在 STAT3 依赖性癌细胞中诱导生长阻滞和细胞凋亡 (apoptosis)。Fluacrypyrim 主要通过阻止造血干细胞 (HSCs) 凋亡来减轻辐射诱导的造血系统损伤。Fluacrypyrim 通过抑制子宫平滑肌收缩和炎症反应，显示出显著的镇痛和抗炎作用[1][2][3][4]。

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Fluacrypyrim

Fluacrypyrim Chemical Structure

CAS No. : 229977-93-9

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Fluacrypyrim 相关抗体

Top Publications Citing Use of Products

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fluacrypyrim, a Miticide, is a STAT3 inhibitor. Fluacrypyrim significantly increases the protein tyrosine phosphatases(PTPs) activity. Fluacrypyrim inhibits the growth of leukemia cells by a predominant G1 arrest with significant decrease of the protein and mRNA levels of cyclin D1. Fluacrypyrim selectively inhibits STAT3 signaling, inducing growth arrest and apoptosis in STAT3-dependent cancer cells. Fluacrypyrim mitigates IR-induced hematopoietic system injury mainly by preventing apoptosis in the HSCs. Fluacrypyrim demonstrates significant analgesic and anti-inflammatory effects by inhibiting uterine smooth muscle contraction and inflammatory responses[1][2][3][4].

体外研究
(In Vitro)

Fluacrypyrim (3-12 h) 可降低 6.5 Gy 辐照后骨髓有核细胞 (BMNCs) 及其亚群 (Lin⁻ 细胞、Lin⁻c-Kit⁺ 细胞、LK 细胞和 LSK 细胞) 的凋亡率[1]。

Fluacrypyrim (5 μM, 4-10 h) 通过调控 p53-PUMA 通路减少骨髓有核细胞的凋亡[1]。

Fluacrypyrim (0.1-12 μM, 0-72 h) 对 HL-60 细胞生长表现出强烈的浓度依赖性和时间依赖性抑制作用，IC50 为 3.8 μM[2]。

Fluacrypyrim (1.5-12 μM, 6-36 h) 通过下调 cyclin-D1 诱导 HL-60 细胞 G1 期阻滞[2]。

Fluacrypyrim (0.75-12 μM, 6-36 h) 显著抑制 HL-60 细胞中 STAT3 (tyr705) 的磷酸化水平，该效应可被过钒酸钠 (sodium pervanadate) 处理逆转[2]。

Fluacrypyrim (0.75-12 μM, 12 h) 在 HL-60 细胞中诱导酪氨酸磷酸酶活性的剂量依赖性升高[2]。

Fluacrypyrim (3-12 μM, 8-24 h) 显著抑制 IL-6 刺激的 HepG-2 细胞和 c-Src 转染的 NIH 3T3 细胞中STAT3 依赖的荧光素酶活性[2]。

Fluacrypyrim (0.75-12 μM, 24 h) 抑制组成型激活的 STAT3，从而阻断 HL-60 细胞中 cyclin D1 和 c-Myc 的表达[2]。

Fluacrypyrim (0.75-12 μM, 24 h) 优先抑制携带组成型激活 STAT3 的癌细胞生长，其 IC50 值分别为：3.8 μM (HL-60 细胞)、6.0 μM (K562 细胞)、8.2 μM (XG-7 细胞) 和 12.3 μM (Jurkat-T 细胞)[2]。

Fluacrypyrim (6-24 μM, 24 h) 在携带组成型激活 STAT3 的乳腺癌细胞 (MDA-MB-231 细胞) 中诱导 caspase 依赖性凋亡[2]。

Fluacrypyrim (0.62-10 μM, 60 min) 能显著抑制由 Dinoprost (PGF2α) (HY-12956)，Oxytocin (HY-17571)，acetylcholine (Ach) 和 KCL 诱导的子宫收缩，且呈剂量依赖性 (pD2 从 5.72 到 5.92)[2]。

Fluacrypyrim (2.5-10 μM) 可抑制子宫肌层细胞中 PGF2α 诱导的 MLC20 磷酸化[3]。

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

Fluacrypyrim 相关抗体:

Cell Cycle Analysis[2]

Cell Line: HL-60 cells and MDA-MB-231 cells
Concentration: 0, 0.75, 1.5, 3, 6, 12 μM
Incubation Time: 6, 12, 24, 36 h
Result: Induced G1 arrest in HL-60 cells and MDA-MB-231 cells(24 μM, 48 h)

Real Time qPCR[1]

Cell Line: BMNC cells
Concentration: 5 μM
Incubation Time: 10 h
Result: Downregulated the expression levels of Puma, Bax, and Noxa markedly.

Western Blot Analysis[1]

Cell Line: BMNC cells
Concentration: 5 μM
Incubation Time: 4 h
Result: Downregulated the expression level of protein of p-p53, p53, Puma, Bax, Noxa, and cleaved Caspase-3.

Western Blot Analysis[2]

Cell Line: HL-60, K562 and XG-7 cells
Concentration: 0, 0.75, 1.5, 3, 6, 12 μM
Incubation Time: 6, 12, 24, 36 h
Result: Decreased the level of pRb (ser807/881) in HL-60 cells (3, 6, 12 μM).
Reduced the expression of cyclin D3 and CDK4 slightly and significantly only in the higher concentrations in HL-60 cells (3, 6, 12 μM).
Decreased the cyclin D1 expression dose-dependently in HL-60 cells (3, 6, 12 μM).
Decreased the STAT3 tyr705 phosphorylation without affecting STAT3 ser727 phosphorylation and total STAT3 protein level in HL-60, K562 and XG-7 cells (0, 0.75, 1.5, 3, 6, 12 μM).
Reduced the expression of STAT5 only at the highest concentration and showed no alteration on STAT1 in HL-60 cells (0, 0.75, 1.5, 3, 6, 12 μM).
体内研究
(In Vivo)

Fluacrypyrim (20-75 mg/kg，腹腔注射，辐照前 3-48 h，单次给药) 减轻了 C57BL/6J (CD45.2) 小鼠和 B6.SJL/BoyJ (CD45.1) 小鼠中辐射诱导的造血系统损伤[1]。

Fluacrypyrim (50-200 mg/kg，腹腔注射，乙酸注射前1小时，单次给药) 可减少乙酸 (HY-Y0319) 诱导的小鼠扭体反应[3]。

Fluacrypyrim (100-200 mg/kg，腹腔注射，PGF2α注射前1小时，单次给药) 在小鼠和大鼠肿胀模型中能减轻炎症活性和疼痛反应[3]。

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

Animal Model: The male C57BL/6J (CD45.2) mice and male B6.SJL/BoyJ (CD45.1) mice(6-8 weeks) were subjected to either a sublethal dose (6.5 Gy) or lethal dose (8.0, 8.5, 9.0 Gy) of total body irradiation (TBI) using a 60Co γ-ray source at a dose rate of approximately 62 cGy/min[1]
Dosage: 20, 50, 75 mg/kg
Administration: i.p. 3, 24, and 48 h before irradiation
Result: Ameliorated pancytopenia in the mice subjected to irradiation (20, 50, 75 mg/kg) (6.5 Gy).
Improved the survival rate of mice after lethal irradiation(50 mg/kg) (8.0 Gy, 8.5 Gy, 9.0 Gy).
Alleviated irradiation-induced injury to BM (6.5 Gy).
Accelerated the recovery of HSPCs after irradiation exposure (6.5 Gy).
Enhanced the self-renewal capacity of HSCs after irradiation (CD45.2: 6.5 Gy) (CD45.1: 9.0 Gy)
Animal Model: KM male and female mice (22-28 g)[3]
Dosage: 50, 100, 200 mg/kg
Administration: i.p., 1 h before acid injection
Result: Reduced acetic acid-induced writhing response in mice
Animal Model: KM male and female mice (22-28 g) and female Sprague Dawley (SD) rats (120-140 g)[3]
Dosage: 50, 100, 200 mg/kg
Administration: i.p., 1 h before PGF2α injection
Result: Reduced inflammatory activities on mouse and rat swelling models.
Reduced PGF2α-induced pain response.
分子量

426.39

Formula

C20H21F3N2O5
CAS 号
中文名称

嘧螨酯
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

Fluacrypyrim 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:

Fluacrypyrim229977-93-9嘧螨酯ParasiteSTATPhosphataseMDM-2/p53ApoptosisMitcideSTAT3ionizing radiationhematopoietic stem cellsapoptosisp53-PUMAMDA-MB-231Inhibitorinhibitorinhibit

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