10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
LT052 is a highly selective BET BD1 inhibitor with an IC 50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC 50 =12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research
In Vitro
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 displays the highinhibitory activity against BRD4(1) (IC 50 : 87.7±4.9 nM), BRD3(1) (IC 50 : 246.3±20.2 nM), and BRDT(1) (IC 50 : 357.1±8.3 nM). LT052 also has inhibitory activities against BRPF1b (IC 50 : 567.5±16.9 nM). Additionlly, LT052 shows a 238-fold selectivity toward BD1 over BD2 with K d of 105 nM and >25 μM for BD1 and BD2, respectively. LT052 (1 μM; 1 hour) inhibits MSU-induced pyroptosis of THP-1 cells through BRD4/NF-κB/NLRP3 signaling pathways. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LT052 (1 mg/kg; intra-articular) suppresses synovial hyperplasia as well as severe neutrophil infiltration, and has a good therapeutic effect on MSU-induced acute gouty arthritis . LT052 suppresses pyroptosis of macrophages in rat synovial tissues through regulating BRD4/NF-κB/NLRP3 signaling pathway . LT052 has a high clearance rate in the range of 93.517 µL/min/mg proteins to 146.685 µL/min/mg proteins in liver microsomes of multiple species (human, monkey, dog, rat). Overall, LT052 exhibits moderately stable levels of in vitro liver microsomal metabolism . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Adult Sprague-Dawley rats (250-280 g) (acute gouty arthritis animal models) Dosage: 1 mg/kg Administration: Intra-articular injection Result: Restored the joint circumference to normal level.
IC50& Target:BRD4 BD1 87.7 nM (IC 50 ) BRD3 BD1 246.3 nM (IC 50 ) BRDT BD1 357.1 nM (IC 50 ) BRPF1b 567.5 nM (IC 50 )
| Isomeric SMILES | CC1=CN(C=N1)C2=NC3=C(C=CC4=C3C(=C2)C(=O)N4C)NS(=O)(=O)C5=CC=CC=C5OC |
|---|---|
| PubChem CID | 145925666 |
| Molecular Weight | 449.48 |
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