Product Name :
LT052
Description:
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 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research.
CAS:
2543545-44-2
Molecular Weight:
449.48
Formula:
C22H19N5O4S
Chemical Name:
2-methoxy-N-[2-methyl-6-(4-methyl-1H-imidazol-1-yl)-3-oxo-2,7-diazatricyclo[6.3.1.0⁴,¹²]dodeca-1(11),4(12),5,7,9-pentaen-9-yl]benzene-1-sulfonamide
Smiles :
CN1C2=CC=C(NS(=O)(=O)C3=CC=CC=C3OC)C3=NC(=CC(C1=O)=C32)N1C=NC(C)=C1
InChiKey:
FSMTUHGXWGJNKK-UHFFFAOYSA-N
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
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.Ursolic acid 130 μM).BT-13 LT052 has anti-inflammatory activity and can be used for acute gout arthritis research.PMID:32695810 |Product information|CAS Number: 2543545-44-2|Molecular Weight: 449.48|Formula: C22H19N5O4S|Chemical Name: 2-methoxy-N-[2-methyl-6-(4-methyl-1H-imidazol-1-yl)-3-oxo-2,7-diazatricyclo[6.3.1.0⁴,¹²]dodeca-1(11),4(12),5,7,9-pentaen-9-yl]benzene-1-sulfonamide|Smiles: CN1C2=CC=C(NS(=O)(=O)C3=CC=CC=C3OC)C3=NC(=CC(C1=O)=C32)N1C=NC(C)=C1|InChiKey: FSMTUHGXWGJNKK-UHFFFAOYSA-N|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|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 10.42 mg/mL (23.18 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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 Kd 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.|Products are for research use only. Not for human use.|