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

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.

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Fluacrypyrim Chemical Structure

Fluacrypyrim Chemical Structure

CAS No. : 229977-93-9

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Fluacrypyrim Related Antibodies

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STAT3 STAT5 STAT6 STAT1

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Description

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].

In Vitro

Fluacrypyrim (FAPM) (3-12 h) reduces the apoptosis rate of BMNCs and its subsets (Lin⁻, Lin⁻c-Kit⁺, LK, and LSK cells) after the 6.5 Gy irradiation[1].

Fluacrypyrim (5 μM, 4-10 h) decreases cell apoptosis by regulating the p53-PUMA pathway in the BMNC cells[1].

Fluacrypyrim (0.1-12 μM, 0-72 h) shows a strong concentration-dependent and time-dependent inhibition of HL-60 cells growth, with an IC50 of 3.8 μM[2].

Fluacrypyrim (1.5-12 μM, 6-36 h) induces G1 arrest of HL-60 cells with downregulation of cyclin-D1[2].

Fluacrypyrim (0.75-12 μM, 6-36 h) significantly inhibits constitutive phosphotyrosine levels of STAT3 (tyr705) in HL-60 cells, an effect that can be reversed by sodium pervanadate treatment[2].

Fluacrypyrim (0.75-12 μM, 12 h) induces a dose-dependent increase of tyrosine phosphatase activity in HL-60 cells[2].

Fluacrypyrim (3-12 μM, 8-24 h) significantly inhibits STAT3-dependent luciferase activity in both IL-6-stimulated HepG-2 cells and c-Src-transfected NIH 3T3 cells[2].

Fluacrypyrim (0.75-12 μM, 24 h) suppresses constitutively active STAT3, thereby blocking cyclin D1 and c-Myc expression in HL-60 cells[2].

Fluacrypyrim (0.75-12 μM, 24 h) preferentially suppresses growth of cancer cells harboring constitutively active STAT3, with IC50 s of 3.8 μM (HL-60 cells), 6.0 μM (K562 cells), 8.2 μM (XG-7 cells) and 12.3 μM (Jurkat-T cells)[2].

Fluacrypyrim (6-24 μM, 24 h) induces caspase-dependent apoptosis in breast carcinoma cells (MDA-MB-231 cells) that harbor constitutively activated STAT3[2].

Fluacrypyrim (0.62-10 μM, 60 min) significantly inhibits uterine contractions induced by Dinoprost (PGF2α) (HY-12956), Oxytocin (HY-17571), acetylcholine (Ach) and KCl in a dose-dependent manner (pD2 values ranging from 5.72 to 5.92)[3].

Fluacrypyrim (2.5-10 μM) inhibits PGF2α-induced MLC20 phosphorylation[3].

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

Fluacrypyrim Related Antibodies

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).
In Vivo

Fluacrypyrim (20-75 mg/kg, i.p., 3-48 h before irradiation, single dose) mitigates IR-induced hematopoietic system injury in the C57BL/6J (CD45.2) mice and B6.SJL/BoyJ (CD45.1) mice[1].

Fluacrypyrim (50-200 mg/kg, i.p., 1 h before acid injection, single dose) reduces Acetic acid (HY-Y0319)-induced writhing response in mice[3].

Fluacrypyrim (100-200 mg/kg, i.p., 1 h before PGF2α injection, single dose) reduces inflammatory activities and pain response on mouse and rat swelling models[3].

MedChemExpress (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: 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.
Molecular Weight

426.39

Formula

C20H21F3N2O5
CAS No.
SMILES

COC(/C(C1=C(C=CC=C1)COC2=NC(OC(C)C)=NC(C(F)(F)F)=C2)=C/OC)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Fluacrypyrim Related Classifications

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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:

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

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