2. NF-κB
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  4. Bezisterim

Bezisterim  (Synonyms: HE 3286; NE-3107)

Cat. No.: HY-108039 Purity: ≥95.0%
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Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis. Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

Bezisterim Chemical Structure

Bezisterim Chemical Structure

CAS No. : 1001100-69-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 950 In-stock
50 mg USD 1450 In-stock
100 mg USD 2250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Bezisterim Related Antibodies

Top Publications Citing Use of Products

View All NF-κB Isoform Specific Products:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

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Description

Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis[1][2][3]. Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

NF-κB[3]
In Vitro

Bezisterim attenuates NF-κB phosphorylation, but not influences IκB phosphorylation of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages[3].
Bezisterim (100 nM, overnight) partially blocks the activation of IKK, JNK, p38, and ERK of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages[3].

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

Bezisterim Related Antibodies

Western Blot Analysis[3]

Cell Line: LPS-induced murine macrophages
Concentration: 100 nM
Incubation Time: overnight
Result: Attenuated NF-κB phosphorylation.
Blocked the activation of IKK, JNK, p38, and ERK partially.
In Vivo

Bezisterim (25-50 mg/kg; oral gavage; daily for 22-49 days) reduces joint inflammation, synovial proliferation, and erosion of DBA/1 Lac male collagen-induced arthritis mice [1].
Bezisterim (40 mg/kg; intraperitoneal injection; daily for 40 days) suppresses inflammation, reduces demyelination and axonal loss, and promotes RGC survival during experimental optic neuritis of experimental autoimmune encephalomyelitis mice[2].
Bezisterim (80?mg/kg; 0-24h) freely penetrates the BBB in male CD-1 mice[4].
Bezisterim (40 mg/kg; gavage; twice-daily for 4 days) increases the numbers of tyrosine hydroxylase-positive cells and decreases the numbers of damaged neurons in Parkinson's disease mice[4].

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

330.46

Formula

C21H30O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O[C@@H]1[C@@]2([H])[C@@]3([H])[C@@]([C@@](C#C)(O)CC3)(CC[C@]2([H])[C@]4(C)C(C[C@@H](O)CC4)=C1)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (302.61 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 3.0261 mL 15.1304 mL 30.2609 mL
5 mM 0.6052 mL 3.0261 mL 6.0522 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 (sealed storage, away from moisture). 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 (sealed storage, away from moisture). 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 3.0261 mL 15.1304 mL 30.2608 mL 75.6521 mL
5 mM 0.6052 mL 3.0261 mL 6.0522 mL 15.1304 mL
10 mM 0.3026 mL 1.5130 mL 3.0261 mL 7.5652 mL
15 mM 0.2017 mL 1.0087 mL 2.0174 mL 5.0435 mL
20 mM 0.1513 mL 0.7565 mL 1.5130 mL 3.7826 mL
25 mM 0.1210 mL 0.6052 mL 1.2104 mL 3.0261 mL
30 mM 0.1009 mL 0.5043 mL 1.0087 mL 2.5217 mL
40 mM 0.0757 mL 0.3783 mL 0.7565 mL 1.8913 mL
50 mM 0.0605 mL 0.3026 mL 0.6052 mL 1.5130 mL
60 mM 0.0504 mL 0.2522 mL 0.5043 mL 1.2609 mL
80 mM 0.0378 mL 0.1891 mL 0.3783 mL 0.9457 mL
100 mM 0.0303 mL 0.1513 mL 0.3026 mL 0.7565 mL
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Bezisterim 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:

Bezisterim1001100-69-1HE 3286 NE-3107HE3286HE-3286NE3107NE 3107NE-3107NF-κBNuclear factor-κBNuclear factor-kappaBmacrophagesparkinson's diseaseexperimental autoimmune encephalomyelitis micerheumatismdiabetesInhibitorinhibitorinhibit

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