LT052,2543545-44-2

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

LT052

CAS No. : 2543545-44-2

MCE 国际站：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 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.

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  Histone Modification Research Compound Library  |  Reprogramming Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Diversity Library  |  Heterocyclic Compound Library  |  Highly Selective Inhibitors Library  |  (+)-JQ-1  |  Curcumin  |  A-485  |  C646  |  Revumenib  |  BRM/BRG1 ATP Inhibitor-1  |  BI 2536  |  dBET6  |  MZ 1  |  ARV-825  |  Inobrodib  |  Birabresib  |  666-15  |  SGC-CBP30  |  VTP50469  |  ACBI1  |  AU-15330  |  ARV-771  |  I-BET151  |  dBET1  |  dCBP-1  |  ABBV-744  |  Anacardic Acid  |  Molibresib  |  NSC 228155  |  KG-501  |  A-366  |  FHD-286  |  Mivebresib

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds