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Cat. No.: HY-118973

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LASSBio-1829 hydrochloride

LASSBio-1829 hydrochloride is an orally active IKK2 inhibitor with an IC₅₀ of 3.8 μM against the human target (Sf21 cells). LASSBio-1829 hydrochloride blocks signal transduction of the inflammation-associated NF-κB activation pathway. LASSBio-1829 hydrochloride reduces leukocyte migration, TNF-α biosynthesis, ROS production and NO production. LASSBio-1829 hydrochloride exhibits anti-inflammatory activity in a carrageenan-induced subcutaneous air pouch mouse model. LASSBio-1829 hydrochloride alleviates licking behavior during the inflammatory phase of the mouse formalin test. LASSBio-1829 hydrochloride can be used in inflammation-related research.

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

CAS No.: 1807810-16-7
Formula: C₂₅H₁₉ClN₄O
Molecular Weight:426.90

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

LASSBio-1829 hydrochloride Chemical Structure

CAS No.: 1807810-16-7

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

IKK2

TNF-α

All IKK Isoforms :

All NF-κB Isoforms :

All TNF Receptor Isoforms :

In Vitro

Innate Immunity

LASSBio-1829 hydrochloride potently inhibits the human recombinant IKK2 enzyme expressed in Sf21 cells, with an IC₅₀ value of 3.8 μM^[1].

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

In Vivo

Innate ImmunityCytokines & ChemokinesOxidative StressOthers

Innate Immunity

Cytokines & Chemokines

Oxidative Stress

LASSBio-1829 (10-100 µM/kg; p.o.; single administration) hydrochloride exhibits potent oral anti-inflammatory activity in the carrageenan-induced subcutaneous air pouch mice model, and reduces leukocyte migration by up to 35%, TNF-α production by 46%, as well as ROS production in a dose-dependent manner^[1].

Others

LASSBio-1829 (30 µM/kg; p.o.; single administration) hydrochloride alleviates inflammatory pain in mice in the formalin test, but shows no activity during the neuropathic pain phase^[1].

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

Animal Model:

Swiss Webster (female, 20-25 g)^[1]
Dosage:

10 µM/kg; 30 µM/kg; 100 µM/kg
Administration:

p.o.; single dose
Result:

Reduced leukocyte migration to the air pouch by 29% at 30 µmol/kg and 35% at 100 µmol/kg.
Inhibited TNF-α production in exudate by 46% at 30 µmol/kg.
Significantly reduced nitric oxide (NO) production in exudate at 10 µmol/kg; higher doses did not show this effect.
Significantly reduced reactive oxygen species (ROS) production in leukocytes stimulated with phorbol myristate acetate (PMA) at 10 and 30 µmol/kg, with a dose-dependent response.

Animal Model:

Swiss Webster (female, 20-25 g)^[1]
Dosage:

30 µM/kg
Administration:

p.o.; single dose
Result:

Showed no significant effect during the neurogenic first phase of the formalin-induced licking response model.
Significantly reduced paw licking time relative to vehicle controls during the inflammatory second phase.

Related Protocols :

Chemical Information

CAS No. 1807810-16-7
Molecular Weight 426.90
Formula C₂₅H₁₉ClN₄O
SMILES

O=C(C1=CC2=C(C=CC=C2)C=C1)N/N=C/C3=CC=C(C=C3)C4=C5C(NC=C5)=NC=C4.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Guedes IA, et al. LASSBio-1829 Hydrochloride: Development of a New Orally Active N-Acylhydrazone IKK2 Inhibitor with Anti-inflammatory Properties. ChemMedChem. 2016 Jan 19;11(2):234-44. [Content Brief]

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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.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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LASSBio-1829 hydrochloride

All IKK Isoforms

All NF-κB Isoforms

All TNF Receptor Isoforms