LT052
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[1].
Product Specifications
CAS Number
2543545-44-2
UNSPSC
12352005
Target
Epigenetic Reader Domain
Type
Reference compound
Related Pathways
Epigenetics
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/lt052.html
Purity
98.77
Solubility
DMSO : 10.42 mg/mL (ultrasonic)
Smiles
O=S(C1=CC=CC=C1OC)(NC2=C3N=C(N4C=C(C)N=C4)C=C5C3=C(N(C)C5=O)C=C2)=O
Molecular Formula
C22H19N5O4S
Molecular Weight
449.48
References & Citations
[1]Jiang F, et al. Discovery of Benzo[cd]indol-2 (1H) -ones and Pyrrolo[4,3,2-de]quinolin-2 (1H) -ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis. J Med Chem. 2019 Dec 26;62 (24) :11080-11107.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
BRD3; BRD4; BRDT; BRPF1
Available Sizes
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