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GSK1362

GSK1362 is a selective inverse agonist of REV-ERB. GSK1362disrupts the interaction of REV-ERBα with repressive co-modulators (NCoR1, SMRT2, RIP140). GSK1362 exerts an inverse agonist effect by increasing the transcription of BMAL1 to relieve BMAL1 repression by endogenous REV-ERB ligands. GSK1362 suppresses LPS -induced inflammatory cytokine expression, inhibits IL-1β-induced Cxcl5 transcription in cells. GSK1362 can be used for the study of inflammatory diseases[1].

Product Specifications

CAS Number

2986733-57-5

UNSPSC

12352005

Target

REV-ERB

Related Pathways

Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Field of Research

Inflammation/Immunology

Purity

96.38

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

N#CC1=C(NCCOC)OC(C2=CC=C(N(CC3=CC=C(C=C3)Cl)C)C=C2)=N1

Molecular Formula

C21H21ClN4O2

Molecular Weight

396.87

References & Citations

[1]Pariollaud M, et al. Circadian clock component REV-ERBα controls homeostatic regulation of pulmonary inflammation. J Clin Invest. 2018 Jun 1;128 (6) :2281-2296.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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