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LT052

Cat. No. M10849

All AbMole products are for research use only, cannot be used for human consumption.

LT052 Structure

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Quality Control & Documentation
Biological Activity

LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory activity and can be used for the research of acute gout arthritis. 

LT052 (1 μM) inhibits NF-κB transcriptional activity in HUVECs cells and inhibit nitric oxide (NO) production (inhibition rate: 101.89%) in RAW264.7 cells. In the evaluation of in vitro inflammatory activity, LT052 maintains comparable or better anti-inflammatory activity than the pan-BET inhibitor (JQ1) compared to the protein weak activity. 

LT052 suppresses pyroptosis of macrophages in rat synovial tissues through regulating BRD4/NF-κB/NLRP3 signaling pathway.

Chemical Information
Molecular Weight 449.48
Formula C22H19N5O4S
CAS Number 2543545-44-2
Solubility (25°C) DMSO 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Fei Jiang, et al. J Med Chem. Discovery of Benzo[ cd]indol-2(1 H)-ones and Pyrrolo[4,3,2- de]quinolin-2(1 H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acu䲧璷Ỵ璸㧀璶羹瘬

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  Catalog
Abmole Inhibitor Catalog




Keywords: LT052 supplier, Epigenetic Reader Domain, inhibitors, activators

All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.


 
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