LT052

2543545-44-2

449.48

DMSO : 10.42 mg/mL (ultrasonic)

Epigenetics

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 uM). LT052 has anti-inflammatory?activity and can be used for acute gout arthritis research.
In Vitro: LT052 (1 uM) inhibits NF-kappaB 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 Kd of 105 nM and >25 uM for BD1 and BD2, respectively.
LT052 (1 uM; 1 hour) inhibits MSU-induced pyroptosis of THP-1 cells through BRD4/NF-kappaB/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-kappaB/NLRP3 signaling pathway.

LT052 has a high clearance rate in the range of 93.517 uL/min/mg proteins to 146.685 uL/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.