LT052

COA

级别和纯度:

≥98%

CAS编号: 2543545-44-2
分子式: C₂₂H₁₉N₅O₄S
分子量: 449.48
PubChem编号: 145925666

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货号 (SKU)	包装规格	是否现货
L647401-5mg	5mg	期货
L647401-10mg	10mg	期货
L647401-25mg	25mg	期货
L647401-50mg	50mg	期货
L647401-100mg	100mg	期货

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Epigenetic Reader Domain (784) 表观遗传学 (1497)

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基本描述

规格或纯度	≥98%
英文名称	LT052
生化机理	LT052 是一种高选择性 BET BD1 抑制剂，IC 50 为 87.7 nM。LT052 对 BRD4 BD1 具有纳摩尔效力，对 BRD4 BD2 具有 138 倍的选择性（IC 50 =12.130 μM）。LT052 具有抗炎活性，可用于急性痛风关节炎的再治疗。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	LT052 is a highly selective BET BD1 inhibitor with an IC 50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC 50 =12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research 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) (IC 50 : 87.7±4.9 nM), BRD3(1) (IC 50 : 246.3±20.2 nM), and BRDT(1) (IC 50 : 357.1±8.3 nM). LT052 also has inhibitory activities against BRPF1b (IC 50 : 567.5±16.9 nM). Additionlly, LT052 shows a 238-fold selectivity toward BD1 over BD2 with K d 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. 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 . 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 . 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) Dosage: 1 mg/kg Administration: Intra-articular injection Result: Restored the joint circumference to normal level. Form:Solid IC50& Target:BRD4 BD1 87.7 nM (IC 50 ) BRD3 BD1 246.3 nM (IC 50 ) BRDT BD1 357.1 nM (IC 50 ) BRPF1b 567.5 nM (IC 50 )
纯度	≥98%

关联靶点（人）

BRD4 Tchem 含溴结构域蛋白 4(Bromodomain-containing protein 4) (1 活性数据)

点击查看靶蛋白信息： BRD4

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

BRDT Tchem 溴结构域睾丸特异性蛋白(Bromodomain testis-specific protein) (1 活性数据)

点击查看靶蛋白信息： BRDT

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

BRD3 Tchem 含溴结构域蛋白 3(Bromodomain-containing protein 3) (1 活性数据)

点击查看靶蛋白信息： BRD3

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

BRPF1 Tchem 佩里格林(Peregrin) (1 活性数据)

点击查看靶蛋白信息： BRPF1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 (13122 活性数据)

点击查看靶蛋白信息： BRD4

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

BRD2 Tchem Bromodomain-containing protein 2 (1296 活性数据)

点击查看靶蛋白信息： BRD2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

BRDT Tchem Bromodomain testis-specific protein (576 活性数据)

点击查看靶蛋白信息： BRDT

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

BRD3 Tchem Bromodomain-containing protein 3 (1086 活性数据)

点击查看靶蛋白信息： BRD3

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

关联靶点（其它种属）

Rattus norvegicus (775804 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

RAW264.7 (28094 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	未知
IIUPAC Name	2-methoxy-N-[2-methyl-6-(4-methylimidazol-1-yl)-3-oxo-2,7-diazatricyclo[6.3.1.04,12]dodeca-1(12),4,6,8,10-pentaen-9-yl]benzenesulfonamide
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
InChi Key	FSMTUHGXWGJNKK-UHFFFAOYSA-N
Smiles	CC1=CN(C=N1)C2=NC3=C(C=CC4=C3C(=C2)C(=O)N4C)NS(=O)(=O)C5=CC=CC=C5OC
Isomeric SMILES	CC1=CN(C=N1)C2=NC3=C(C=CC4=C3C(=C2)C(=O)N4C)NS(=O)(=O)C5=CC=CC=C5OC
PubChem CID	145925666
分子量	449.48

化学和物理性质

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

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C of A & Other Certificates(BSE/TSE, COO):

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