2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Epigenetics Membrane Transporter/Ion Channel Anti-infection
  3. HSP Epigenetic Reader Domain ATP-binding cassette (ABC) transporters Bacterial Fungal Antibiotic
  4. Isoxazole

Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor​.

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Isoxazole Chemical Structure

Isoxazole Chemical Structure

CAS No. : 288-14-2

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Based on 1 publication(s) in Google Scholar

Isoxazole Related Antibodies

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Description

Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor​[1][2][3][4][5].

IC50 & Target

Multidrug resistance proteins (MRPs)

 

In Vitro

Isoxazole (20 µM, 48 hours) improves β-cell function by inhibiting excessive proliferation of MIN6 cells (mouse pancreatic β-cells) and altering the gene expression profile of MIN6 cells (enhancing the neuroendocrine phenotype)[5].

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

Isoxazole Related Antibodies

Real Time qPCR[5]

Cell Line: MIN6 mouse β-cell line
Concentration: 20 µM
Incubation Time: 48 h
Result: Significantly upregulates gene expression of STMN2.

Western Blot Analysis[5]

Cell Line: MIN6 mouse β-cell line
Concentration: 20 µM
Incubation Time: 48 h
Result: Upregulates STMN2 protein expression.

Cell Proliferation Assay[5]

Cell Line: INS1E mouse β-cell line
Concentration: 20 µM
Incubation Time: 72 h
Result: Reduced cell number, indicating inhibition of cell proliferation.
In Vivo

Isoxazole (16 mg/kg, i.p., once daily for 4 weeks) improves β-cell function in diabetes mice model (PANIC-ATTAC mice model induced by dimerizer (e.g., AP20187, HY-13992)[5].

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

Animal Model: Diabetes model in PANIC-ATTAC mice induced by dimerizer (e.g., AP20187 (HY-13992))[5]
Dosage: 16 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 4 weeks
Result: Significant reduced blood glucose after oral glucose tolerance test (OGTT).
Caused that pancreas insulin content increased approaching significance.
Molecular Weight

69.06

Formula

C3H3NO
CAS No.
Appearance

Liquid (Density: 1.078 g/cm3)

Color

Colorless to light yellow

SMILES

C1=CON=C1
Shipping

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

DMSO : 100 mg/mL (1447.95 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 14.4795 mL 72.3977 mL 144.7953 mL
5 mM 2.8959 mL 14.4795 mL 28.9591 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.98%

SDS (466 KB)

COA (259 KB) HNMR (111 KB) GC (184 KB)

Handling Instructions (2659 KB)
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 14.4795 mL 72.3977 mL 144.7953 mL 361.9883 mL
5 mM 2.8959 mL 14.4795 mL 28.9591 mL 72.3977 mL
10 mM 1.4480 mL 7.2398 mL 14.4795 mL 36.1988 mL
15 mM 0.9653 mL 4.8265 mL 9.6530 mL 24.1326 mL
20 mM 0.7240 mL 3.6199 mL 7.2398 mL 18.0994 mL
25 mM 0.5792 mL 2.8959 mL 5.7918 mL 14.4795 mL
30 mM 0.4827 mL 2.4133 mL 4.8265 mL 12.0663 mL
40 mM 0.3620 mL 1.8099 mL 3.6199 mL 9.0497 mL
50 mM 0.2896 mL 1.4480 mL 2.8959 mL 7.2398 mL
60 mM 0.2413 mL 1.2066 mL 2.4133 mL 6.0331 mL
80 mM 0.1810 mL 0.9050 mL 1.8099 mL 4.5249 mL
100 mM 0.1448 mL 0.7240 mL 1.4480 mL 3.6199 mL
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Isoxazole Related Classifications

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:

Isoxazole288-14-2HSPEpigenetic Reader DomainATP-binding cassette (ABC) transportersBacterialFungalAntibioticHeat shock proteinsATP-binding cassette transporterslow cytotoxicitybroad biological activitiesagent scaffoldinhibitorInhibitorinhibit

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