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  2. Epigenetic Reader Domain
  3. LT052

LT052 

Cat. No.: HY-130622 Purity: 98.49%
Handling Instructions

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.

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

LT052 Chemical Structure

LT052 Chemical Structure

CAS No. : 2543545-44-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 550 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 550 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3000 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4600 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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[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 (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[1].
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[1].
LT052 (1 μM; 1 hour) inhibits MSU-induced pyroptosis of THP-1 cells through BRD4/NF-κB/NLRP3 signaling pathways[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

CAS No.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10.42 mg/mL (23.18 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2248 mL 11.1240 mL 22.2479 mL
5 mM 0.4450 mL 2.2248 mL 4.4496 mL
10 mM 0.2225 mL 1.1124 mL 2.2248 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

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

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