Cat. No.: HY-108039

Bezisterim

(Synonyms: HE 3286; NE-3107)

Customer Review

Based on 1 Customer Validation

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.

Purity: 95.0%
CAS No.: 1001100-69-1
Formula: C₂₁H₃₀O₃
Molecular Weight:330.46

Storage:

4°C, sealed storage, away from moisture

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

Bezisterim Chemical Structure

CAS No.: 1001100-69-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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]

All NF-κB Isoforms :

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1001100-69-1
Appearance Solid
Molecular Weight 330.46
Formula C₂₁H₃₀O₃
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
Synonyms

HE 3286; NE-3107
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0261 mL

15.1304 mL

30.2609 mL

5 mM

0.6052 mL

3.0261 mL

6.0522 mL

10 mM

0.3026 mL

1.5130 mL

3.0261 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Auci D, et al. A new orally bioavailable synthetic androstene inhibits collagen-induced arthritis in the mouse: androstene hormones as regulators of regulatory T cells. Ann N Y Acad Sci. 2007;1110:630-640. [Content Brief]

[2]. Khan RS, et al. HE3286 reduces axonal loss and preserves retinal ganglion cell function in experimental optic neuritis. Invest Ophthalmol Vis Sci. 2014;55(9):5744-5751. Published 2014 Aug 19. [Content Brief]

[3]. Lu M,et al. A new antidiabetic compound attenuates inflammation and insulin resistance in Zucker diabetic fatty rats. Am J Physiol Endocrinol Metab. 2010;298(5):E1036-E1048. [Content Brief]

[4]. Nicoletti F, et al. 17α-Ethynyl-androst-5-ene-3β,7β,17β-triol (HE3286) Is Neuroprotective and Reduces Motor Impairment and Neuroinflammation in a Murine MPTP Model of Parkinson's Disease. Parkinsons Dis. 2012;2012:969418. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alkyne Compound Library

All NF-κB Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bezisterim Related Classifications

HY-108039 Related Classifications