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DASA-58, 丙酮酸激酶 M1/2 激活剂

PKM 活化剂

COA

级别和纯度:

Moligand™

≥98%

CAS编号: 1203494-49-8
分子式: C₁₉H₂₃N₃O₆S₂
分子量: 453.53
PubChem编号: 44543605
PubChem SID: 504770366

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货号 (SKU)	包装规格	是否现货
D413874-5mg	5mg	期货
D413874-25mg	25mg	期货
D413874-50mg	50mg	现货
D413874-100mg	100mg	现货

查看相关系列

Glucose Metabolism (3713) Metabolic Enzyme/Protease (4889) pyruvate kinase M1/2 Activator (4) 丙酮酸激酶 (19)

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基本描述

英文别名	3-[[4-[(2,3-dihydro-1,4-benzodioxin-6-yl)sulfonyl]hexahydro-1H-1,4-diazepin-1-yl]sulfonyl]-Benzenamine
规格或纯度	Moligand™, ≥98%
英文名称	DASA-58
生化机理	DASA-58 是一种特异性强效丙酮酸激酶 M2 (PKM2) 激活剂。
储存温度	-20°C储存
运输条件	超低温冰袋运输
作用类型	激活剂
作用机制	丙酮酸激酶 M1/2 激活剂
产品介绍	Information DASA-58 DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator. Targets PKM2 In vitro DASA-58 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes in primary BMDMs, and also inhibits glycolysis and the accumulation of succinate in LPS-activated macrophages. In PC3 cells, DASA-58 impairs stromal-induced EMT program by restoring PK activity and abrogating the nuclear translocation of PKM2, as well as its association with HIF-1α. DASA-58 also dramatically reduces (~6-fold) CAFs-induced lung metastases formation in PC3 cells. In vivo DASA-58 (40 μM) affects EMT of prostate cancers and tumor dissemination in SCID mice.
纯度	≥98%

产品属性

ALogP	0.632
hba_count	6
HBD Count	1
Rotatable Bond	4

关联靶点（人）

PKM Tchem 丙酮酸激酶PKM(Pyruvate kinase PKM) (0 活性数据)

点击查看靶蛋白信息： PKM

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

关联靶点（其它种属）

Pkm Pyruvate kinase isozymes M1/M2 (66 活性数据)

点击查看靶蛋白信息： Pkm

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

Pklr Pyruvate kinase isozymes R/L (113 活性数据)

点击查看靶蛋白信息： Pklr

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

PubChem SID	504770366
分子类型	小分子
IIUPAC Name	3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl]aniline
INCHI	1S/C19H23N3O6S2/c20-15-3-1-4-16(13-15)29(23,24)21-7-2-8-22(10-9-21)30(25,26)17-5-6-18-19(14-17)28-12-11-27-18/h1,3-6,13-14H,2,7-12,20H2
InChi Key	GMHIOMMKSMSRLY-UHFFFAOYSA-N
Smiles	C1CN(CCN(C1)S(=O)(=O)C2=CC=CC(=C2)N)S(=O)(=O)C3=CC4=C(C=C3)OCCO4
Isomeric SMILES	C1CN(CCN(C1)S(=O)(=O)C2=CC=CC(=C2)N)S(=O)(=O)C3=CC4=C(C=C3)OCCO4
分子量	453.53
Reaxy-Rn	20138512
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20138512&ln=

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 91 mg/mL (200.64 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility	91
DMSO(mM) Max Solubility	200.6482482
Water(mg / mL) Max Solubility	＜1
分子量	453.500 g/mol
XLogP3	1.100
氢键供体数Hydrogen Bond Donor Count	1
氢键受体数Hydrogen Bond Acceptor Count	9
可旋转键计数Rotatable Bond Count	4
精确质量Exact Mass	453.103 Da
单同位素质量Monoisotopic Mass	453.103 Da
拓扑极表面积Topological Polar Surface Area	136.000 Å²
重原子数Heavy Atom Count	30
形式电荷Formal Charge	0
复杂度Complexity	794.000
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)

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找到2个结果

批号(Lot Number)	证书类型	货号
G2221185	分析证书	D413874
G2221205	分析证书	D413874

引用文献

1. Walsh MJ, Brimacombe KR, Veith H, Bougie JM, Daniel T, Leister W, Cantley LC, Israelsen WJ, Vander Heiden MG, Shen M et al.. (2011) 2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.. Bioorg Med Chem Lett, 21 (21): (6322-7). [PMID:21958545]
2. Anastasiou D, Yu Y, Israelsen WJ, Jiang JK, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A et al.. (2012) Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.. Nat Chem Biol, 8 (10): (839-47). [PMID:22922757]