2. Epigenetics
  3. Epigenetic Reader Domain
  4. 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.

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

LT052 Chemical Structure

LT052 Chemical Structure

CAS No. : 2543545-44-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 550 In-stock
Solid
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10 mg USD 850 In-stock
25 mg USD 1800 In-stock
50 mg USD 3000 In-stock
100 mg USD 4600 In-stock
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Based on 1 publication(s) in Google Scholar

LT052 Related Antibodies

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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].

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

LT052 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

Yellow to orange

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2248 mL 11.1240 mL 22.2479 mL 55.6198 mL
5 mM 0.4450 mL 2.2248 mL 4.4496 mL 11.1240 mL
10 mM 0.2225 mL 1.1124 mL 2.2248 mL 5.5620 mL
15 mM 0.1483 mL 0.7416 mL 1.4832 mL 3.7080 mL
20 mM 0.1112 mL 0.5562 mL 1.1124 mL 2.7810 mL
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LT052 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LT0522543545-44-2LT 052LT-052Epigenetic Reader Domainselectiveacutegoutyarthritisanti-inflammatorysynovialhyperplasiaRAW264.7cellsInhibitorinhibitorinhibit

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