LT052 is a highly selectiveBETBD1inhibitor with anIC₅₀of 87.7 nM. LT052 exhibits nanomolarBRD4BD1 potency and 138-fold selectivity overBRD4BD2 (IC₅₀=12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research^[1].

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^[1].
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_dof 105 nM and >25 μM for BD1 and BD2, respectively^[1].
LT052 (1 μM; 1 hour) inhibits MSU-induced pyroptosis of THP-1 cells through BRD4/NF-κB/NLRP3 signaling pathways^[1].

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^[1].
LT052 suppresses pyroptosis of macrophages in rat synovial tissues through regulating BRD4/NF-κB/NLRP3 signaling pathway^[1].
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^[1].

449.48

Solid

C₂₂H₁₉N₅O₄S

2543545-44-2

Room temperature in continental US; may vary elsewhere.

DMSO : 10.42 mg/mL(23.18 mM;Need ultrasonic)

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