GSK2593074A

COA

级别和纯度:

≥98%

CAS编号: 1337531-06-2
分子式: C₂₇H₂₃N₅OS
分子量: 465.57
PubChem编号: 53466951

有货

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭

货号 (SKU)	包装规格	是否现货
G651840-5mg	5mg	期货
G651840-10mg	10mg	期货
G651840-50mg	50mg	期货
G651840-100mg	100mg	期货

查看相关系列

Apoptosis (7108) Extrinsic Pathway (1228) RIP kinase (65)

Skip to the end of the images gallery

Skip to the beginning of the images gallery

基本描述

规格或纯度	≥98%
英文名称	GSK2593074A
生化机理	GSK2593074A （GSK'074）是一种坏死抑制剂，对 RIP1 和 RIP3 具有双重靶向能力。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3 In Vitro GSK2593074A (GSK’074; 0.01, 0.1, 1, 10, and 100 nM; 6 hours for MOVAS cells; 3 hours for L929 cells) completely rescues cells from necroptosis under different stimuli in both human and murine cells at IC 50 ~3 nM. In multiple cell types including mouse SMCs, fibroblasts (L929), bone marrow derived macrophages (BMDM), and human colon epithelial cells (HT29), GSK2593074A inhibits necroptosis with an IC 50 of ~3 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Mouse smooth muscle cell line MOVAS; Mouse fibroblast cell line L929 Concentration: 0.01, 0.1, 1, 10, and 100 nM Incubation Time: 6 hours for MOVAS cells; 3 hours for L929 cells Result: Inhibited MOVAS and L929 cells with the IC 50 of 3 nM. In Vivo GSK2593074A (GSK’074; 0.93 mg/kg/day; i.p. injection; 14 or 28 days) is administrated to Apoe -/- mice immediately following pump implantation. Compared to the DMSO group, GSK2593074A-treated mice show significantly alleviated aneurysm formation, reflected by a much smaller aortic dilatation (DMSO 85.39±15.76% vs GSK2593074A 36.28±5.76%; P<0.05) as well as a reduced abdominal aortic aneurysm (AAA) incidence (from 83.3 to 16.7%). GSK2593074A significantly decreases the extent of aortic expansion (DMSO 66.06±9.17% vs GSK2593074A 27.36±8.25%; P<0.05) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Apoe -/- female mice (9-10 months) Dosage: 0.93 mg/kg/day; 200 µL Administration: Daily i.p. injection; 14 or 28 days Result: Inhibited aneurysm formation in mouse models of aneurysms. Form:Solid IC50& Target:RIP1, RIP3
纯度	≥98%

关联靶点（人）

EIF2AK3 Tchem 真核翻译起始因子 2-α激酶 3(Eukaryotic translation initiation factor 2-alpha kinase 3) (1 活性数据)

点击查看靶蛋白信息： EIF2AK3

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

NEK2 Tchem Serine/threonine-protein kinase NEK2 (3514 活性数据)

点击查看靶蛋白信息： NEK2

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

NEK9 Tchem Serine/threonine-protein kinase NEK9 (1479 活性数据)

点击查看靶蛋白信息： NEK9

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

NEK6 Tchem Serine/threonine-protein kinase NEK6 (1986 活性数据)

点击查看靶蛋白信息： NEK6

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

NEK7 Tchem Serine/threonine-protein kinase NEK7 (1804 活性数据)

点击查看靶蛋白信息： NEK7

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

NEK5 Tchem Serine/threonine-protein kinase Nek5 (349 活性数据)

点击查看靶蛋白信息： NEK5

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

EIF2AK2 Tchem Interferon-induced, double-stranded RNA-activated protein kinase (504 活性数据)

点击查看靶蛋白信息： EIF2AK2

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

NEK4 Tchem Serine/threonine-protein kinase Nek4 (980 活性数据)

点击查看靶蛋白信息： NEK4

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

NEK1 Tchem Serine/threonine-protein kinase Nek1 (1886 活性数据)

点击查看靶蛋白信息： NEK1

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

NEK3 Tchem Serine/threonine-protein kinase Nek3 (902 活性数据)

点击查看靶蛋白信息： NEK3

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

NEK11 Tchem Serine/threonine-protein kinase Nek11 (645 活性数据)

点击查看靶蛋白信息： NEK11

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

EIF2AK1 Tchem Eukaryotic translation initiation factor 2-alpha kinase 1 (688 活性数据)

点击查看靶蛋白信息： EIF2AK1

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

EIF2AK3 Tchem Eukaryotic translation initiation factor 2-alpha kinase 3 (635 活性数据)

点击查看靶蛋白信息： EIF2AK3

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

NEK10 Tchem Serine/threonine-protein kinase Nek10 (176 活性数据)

点击查看靶蛋白信息： NEK10

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）

L929 (3802 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

MOVAS-1 (14 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	小分子
IIUPAC Name	1-[5-[4-amino-7-(1-methylpyrazol-4-yl)thieno[3,2-c]pyridin-3-yl]-2,3-dihydroindol-1-yl]-2-phenylethanone
INCHI	1S/C27H23N5OS/c1-31-15-20(13-30-31)21-14-29-27(28)25-22(16-34-26(21)25)18-7-8-23-19(12-18)9-10-32(23)24(33)11-17-5-3-2-4-6-17/h2-8,12-16H,9-11H2,1H3,(H2,28,29)
InChi Key	LIGGMBSSOOVGAE-UHFFFAOYSA-N
Smiles	CN1C=C(C=N1)C2=CN=C(C3=C2SC=C3C4=CC5=C(C=C4)N(CC5)C(=O)CC6=CC=CC=C6)N
Isomeric SMILES	CN1C=C(C=N1)C2=CN=C(C3=C2SC=C3C4=CC5=C(C=C4)N(CC5)C(=O)CC6=CC=CC=C6)N
PubChem CID	53466951
分子量	465.57

化学和物理性质

溶解性	DMSO : 41.67 mg/mL (89.50 mM; Need ultrasonic)
分子量	465.600 g/mol
XLogP3	4.100
氢键供体数Hydrogen Bond Donor Count	1
氢键受体数Hydrogen Bond Acceptor Count	5
可旋转键计数Rotatable Bond Count	4
精确质量Exact Mass	465.162 Da
单同位素质量Monoisotopic Mass	465.162 Da
拓扑极表面积Topological Polar Surface Area	105.000 Å²
重原子数Heavy Atom Count	34
形式电荷Formal Charge	0
复杂度Complexity	732.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

质检证书（CoA,COO,BSE/TSE 和分析图谱)

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

输入批号以搜索分析图谱:

溶液计算器

摩尔浓度计算器

计算溶液所需的质量、体积或浓度。

质量

浓度

体积

分子量

g/mol

稀释计算器

计算配制储备溶液所需的稀释度。

浓度1（C1）

体积 1 (V1)

浓度 2 (C2)

体积 2 (V2)

复溶计算器

复溶计算器允许您快速计算试剂的体积，以复溶小瓶。只需输入试剂的质量和目标浓度，计算器将确定其余部分。

体积（添加到小瓶中）

质量（小瓶）

所需的复溶浓度