2. PI3K/Akt/mTOR Immunology/Inflammation Anti-infection
  3. PI3K Akt Interleukin Related Bacterial
  4. FHND5032

FHND5032 is an orally active miR-124 inducer. FHND5032 significantly upregulates miR-124 expression in macrophages. FHND5032 disrupts inflammatory signaling, promotes macrophage reprogramming, and restores the epithelial barrier function by inhibiting the PIK3R2/PI3K/Akt axis. FHND5032 alleviates colitis and reduces inflammatory burden in ulcerative colitis mice. FHND5032 can be used for the study of ulcerative colitis.

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FHND5032

FHND5032 Chemical Structure

CAS No. : 3076057-63-8

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

FHND5032 Related Antibodies

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Description

FHND5032 is an orally active miR-124 inducer. FHND5032 significantly upregulates miR-124 expression in macrophages. FHND5032 disrupts inflammatory signaling, promotes macrophage reprogramming, and restores the epithelial barrier function by inhibiting the PIK3R2/PI3K/Akt axis. FHND5032 alleviates colitis and reduces inflammatory burden in ulcerative colitis mice. FHND5032 can be used for the study of ulcerative colitis[1].

In Vitro

FHND5032 (0-20 μM, 24 h) significantly exerts anti-inflammatory activity in THP-1 and RAW 264.7 cells by enhancing miR-124 expression[1].
FHND5032 (≤ 5 μM) activates miR-124-5p expression to regulate the PI3K/Akt pathway by targeting PIK3R2 in THP-1 and RAW 264.7 cells reprogramming[1].
FHND5032 decreases the expression of M1 marker CD86 while increasing the expression of M2 marker CD206 in RAW 264.7 cells[1].
FHND5032 promots the expression of the barrier-sealing proteins ZO-1 and occludin to facilitate Tight junction (TJ) assembly in Caco-2 cells[1].

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

FHND5032 Related Antibodies

Real Time qPCR[1]

Cell Line: THP-1 and RAW 264.7 cells
Concentration: 5, 10 μM
Incubation Time: /
Result: Upregulated miR-124 levels and induced miR-124 expression, which peaked at a concentration of 5 μM.
Decreased TNF-α, IL-1β, and IL-6 expression in LPS (HY-D1056)- and IFN-γ-stimulated THP-1 cells and LPS stimulated RAW 264.7 cells.
Decreased the expression of PIK3R2
In Vivo

FHND5032 (25-50 mg/kg, i.g., daily, 12 days) alleviates colitis and reduces inflammatory burden in Dextran sulfate sodium salt (DSS) (HY-116282C)-induced ulcerative colitis (UC) mice[1].

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

Animal Model: DSS-induced female C57BL/6J mice (18-20 g)[1]
Dosage: 25, 50 mg/kg
Administration: i.g. once daily for 12 days
Result: Restrained the body weight loss of DSS-induced colitis mice.
Reduced the hematochezia occurrence during treatment.
Showed longer colon length of mice.
Protected the colonic barrier from pathological damage.
Decreased the local level of UC-associated myeloperoxidase (MPO) in the colon.
Reduced the expression of pro-inflammatory cytokines, including IL-6, TNF-α, and IFN-γ.
Increased the expression of anti-inflammatory cytokines IL-10.
Prevented intestinal damage in UC through elevation of TJ proteins.
Prevented the FITC-dextran leakage.
Inhibited colonic inflammation and repaired the intestinal barrier in colitis mice.
Upregulated the miR-124 expression and decreased PIK3R2 expression.
Attenuated PIK3R2 upregulation and the hyperphosphorylation of PI3K and Akt.
Showed no significant discrepancies in serum physicochemical parameters (alanine aminotransferase (ALT), aspartate aminotransferase (AST), blood urea nitrogen (BUN), and creatinine (Cr)).
Decreased the abundance of Proteobacteria in colitis mice and effectively enhanced the relative abundance of Firmicutes.
Showed no increase on the abundance of Bacteroidota.
Molecular Weight

339.70

Formula

C15H9ClF3N3O
CAS No.
Appearance

Solid

SMILES

FC(F)(OC1=CC=C(C=C1)NC2=NC3=CC(Cl)=CC=C3C=N2)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (147.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9438 mL 14.7189 mL 29.4377 mL
5 mM 0.5888 mL 2.9438 mL 5.8875 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9438 mL 14.7189 mL 29.4377 mL 73.5943 mL
5 mM 0.5888 mL 2.9438 mL 5.8875 mL 14.7189 mL
10 mM 0.2944 mL 1.4719 mL 2.9438 mL 7.3594 mL
15 mM 0.1963 mL 0.9813 mL 1.9625 mL 4.9063 mL
20 mM 0.1472 mL 0.7359 mL 1.4719 mL 3.6797 mL
25 mM 0.1178 mL 0.5888 mL 1.1775 mL 2.9438 mL
30 mM 0.0981 mL 0.4906 mL 0.9813 mL 2.4531 mL
40 mM 0.0736 mL 0.3680 mL 0.7359 mL 1.8399 mL
50 mM 0.0589 mL 0.2944 mL 0.5888 mL 1.4719 mL
60 mM 0.0491 mL 0.2453 mL 0.4906 mL 1.2266 mL
80 mM 0.0368 mL 0.1840 mL 0.3680 mL 0.9199 mL
100 mM 0.0294 mL 0.1472 mL 0.2944 mL 0.7359 mL
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FHND5032 Related Classifications

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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:

FHND50323076057-63-8FHND 5032FHND-5032PI3KAktInterleukin RelatedBacterialPhosphoinositide 3-kinasePKBProtein kinase BILmiR-124ulcerative colitis,THP-1 cellsRAW 264.7 cellsInhibitorinhibitorinhibit

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