1. Epigenetics
  2. Epigenetic Reader Domain
  3. LT052

LT052 

Cat. No.: HY-130622
Handling Instructions

LT052 is a highly selective BET BD1 inhibitor. LT052 displays inhibitory activity against BRD4 (BD1), BRD3 (BD1) and BRDT (BD1) with IC50s of 87.7, 246.3, and 357.1 nM, respectively. LT052 shows nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2. LT052 has inhibitory activities against BRPF1b (IC50=567.5 nM). LT052 has anti-inflammatory activity.

For research use only. We do not sell to patients.

LT052 Chemical Structure

LT052 Chemical Structure

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Description

LT052 is a highly selective BET BD1 inhibitor. LT052 displays inhibitory activity against BRD4 (BD1), BRD3 (BD1) and BRDT (BD1) with IC50s of 87.7, 246.3, and 357.1 nM, respectively. LT052 shows nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2. LT052 has inhibitory activities against BRPF1b (IC50=567.5 nM). LT052 has anti-inflammatory activity[1].

IC50 & Target[1]

BRD4 BD1

87.7 nM (IC50)

BRD3 BD1

246.3 nM (IC50)

BRDT BD1

357.1 nM (IC50)

BRPF1b

567.5 nM (IC50)

In Vitro

LT052 displays better activity in reducing NO production in RAW264.7 cells. LT052 displays good activity inhibiting NF-κB transcriptional activity in HUVECs. LT052 (1 μM; 1 hour) inhibits MSU-induced pyroptosis of THP-1 cells through BRD4/NF-κB/NLRP3 signaling pathways[1].

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[1].
LT052 suppresses pyroptosis of macrophages in rat synovial tissues through regulating BRD4/NF-κB/NLRP3 signaling pathway[1].
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[1].

Animal Model: Male Adult Sprague-Dawley rats (250-280 g) (acute gouty arthritis animal models)[1]
Dosage: 1 mg/kg
Administration: Intra-articular injection
Result: Restored the joint circumference to normal level.
Molecular Weight

449.48

Formula

C₂₂H₁₉N₅O₄S

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

LT052LT 052LT-052Epigenetic Reader Domainselectiveacutegoutyarthritisanti-inflammatorysynovialhyperplasiaRAW264.7cellsInhibitorinhibitorinhibit

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