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LT052

CAS No. : 2543545-44-2

MCE 站：LT052

产品活性：LT052 是一种高选择性 BET BD1 抑制剂，其 IC₅₀ 为 87.7 nM。LT052 表现出纳摩尔级别的 BRD4 BD1 的抑制活性，选择性是 BRD4 BD2 的 138 倍 (IC₅₀=12.130 μM)。LT052 具有抗炎活性，可用于急性痛风性关节炎研究。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

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) (IC₅₀: 87.7±4.9 nM), BRD3(1) (IC₅₀: 246.3±20.2 nM), and BRDT(1) (IC₅₀: 357.1±8.3 nM). LT052 also has inhibitory activities against BRPF1b (IC₅₀: 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.

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 ?L/min/mg proteins to 146.685 ?L/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.

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