For research use only. Not for therapeutic Use.
LT052(CAT: I017380) is a highly selective BET bromodomain BD1 inhibitor with potent activity against BRD4 BD1 (IC50 = 87.7 nM) and remarkable selectivity (138-fold) over BRD4 BD2. It also shows activity against BRD3(1), BRDT(1), and BRPF1b at higher nanomolar ranges. LT052 exhibits strong anti-inflammatory effects, inhibiting NF-κB transcriptional activity, nitric oxide production, and MSU-induced pyroptosis in immune cells via the BRD4/NF-κB/NLRP3 signaling pathway. In vivo, intra-articular administration (1 mg/kg) reduces synovial hyperplasia and neutrophil infiltration in gout models, demonstrating therapeutic potential for acute gouty arthritis. LT052 is a valuable tool for epigenetics, inflammation, and gout disease research.
| CAS Number | 2543545-44-2 |
| Synonyms | 2-methoxy-N-[2-methyl-6-(4-methylimidazol-1-yl)-3-oxo-2,7-diazatricyclo[6.3.1.04,12]dodeca-1(12),4,6,8,10-pentaen-9-yl]benzenesulfonamide |
| Molecular Formula | C22H19N5O4S |
| Purity | ≥95% |
| IUPAC Name | 2-methoxy-N-[2-methyl-6-(4-methylimidazol-1-yl)-3-oxo-2,7-diazatricyclo[6.3.1.04,12]dodeca-1(12),4,6,8,10-pentaen-9-yl]benzenesulfonamide |
| InChI | InChI=1S/C22H19N5O4S/c1-13-11-27(12-23-13)19-10-14-20-16(26(2)22(14)28)9-8-15(21(20)24-19)25-32(29,30)18-7-5-4-6-17(18)31-3/h4-12,25H,1-3H3 |
| InChIKey | FSMTUHGXWGJNKK-UHFFFAOYSA-N |
| SMILES | CC1=CN(C=N1)C2=NC3=C(C=CC4=C3C(=C2)C(=O)N4C)NS(=O)(=O)C5=CC=CC=C5OC |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
