TAK-243 (MLN7243)

NF-κB 抑制剂

COA

级别和纯度:

≥97%

CAS编号: 1450833-55-2
分子式: C₁₉H₂₀F₃N₅O₅S₂
分子量: 519.52
PubChem编号: 71715374
PubChem SID: 504772201

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货号 (SKU)	包装规格	是否现货
T413978-2mg	2mg	现货
T413978-5mg	5mg	现货
T413978-10mg	10mg	现货
T413978-25mg	25mg	现货
T413978-50mg	50mg	现货

查看相关系列

Amino Acid/Protein Metabolism (4559) Apoptosis (7108) E1/E2/E3 Enzyme (112) Metabolic Enzyme/Protease (4889) NF-κB (756)

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基本描述

英文别名	BDBM329836 \| Z2327515161 \| AS-17418 \| HY-100487 \| TAK-243 (MLN7243) \| SCHEMBL15191794 \| A930232 \| AKOS037648830 \| MLN 7243 \| SR-01000075683 \| D70045 \| [(1R,2R,3S,4R)-2,3-dihydroxy-4-[[2-[3-(trifluoromethylsulfanyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amin
规格或纯度	≥97%
英文名称	TAK-243 (MLN7243)
生化机理	TAK-243（MLN7243）是一种基于机制的泛素活化酶（UAE）强效小分子抑制剂，在 UBCH10 E2 硫酯测定中的 IC50 为 1 ± 0.2 nM。它在一系列激酶和受体检测中的抑制活性极低，对人类 I 型和 II 型碳酸酐酶的抑制活性也很低。TAK-243 (MLN7243)可诱导ER应激，抑制NFκB通路的激活并促进细胞凋亡。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Information TAK-243 (MLN7243) TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II. TAK-243 (MLN7243) induces ER stress , abrogates NFκB pathway activation and promotes apoptosis . Targets NF-κB ; UAE (Cell-free assay) ; 1 nM In vitro TAK-243 treatment causes depletion of cellular ubiquitin conjugates, resulting in disruption of signaling events, induction of proteotoxic stress, and impairment of cell cycle progression and DNA damage repair pathways. TAK-243 has weaker inhibitory activity against other closely related E1 ubiquitin-like activating enzymes such as Fat10-activating enzyme (UBA6; 7 ± 3 nM), NEDD8-activating enzyme (NAE; 28 ± 11 nM), SUMO-activating enzyme (SAE; 850 ± 180 nM), ISG15-activating enzyme (UBA7; 5,300 ± 2,100 nM) and autophagy-activating enzyme (ATG7; >10,000 nM) than it does against UAE. TAK-243 inhibits UAE from transferring ubiquitin to an E2 enzyme. TAK-243 shows equally potent inhibition of the two E1 enzymes capable of activating ubiquitin (UBA6 and UAE), as indicated by comparable decreases in levels of charged USE1 and UBCH10. Downstream UAE pathway inhibition by TAK-243 is evident, as shown by a dose- and time-dependent loss of both polyubiquitin chains and mono-ubiquitylated histone H2B; however, TAK-243 treatment does not affect UAE (UBE1) protein levels. TAK-243 treatment also causes accumulation of short-lived proteins such as c-Jun, c-Myc, MCL1 and p53. In vivo TAK-243 treatment causes death of cancer cells and, in primary human xenograft studies. TAK-243 demonstrates broad antitumor activity in models of solid and hematological tumors. Cell Research(from reference) Cell lines：HCT-116 and WSU-DLCL2 cells Concentrations：0.01, 0.10 or 1.00 μM Incubation Time：1, 2, 4, 8, 16 and 24 h
纯度	≥97%

名称和识别符

PubChem SID	504772201
分子类型	小分子
IIUPAC Name	[(1R,2R,3S,4R)-2,3-dihydroxy-4-[[2-[3-(trifluoromethylsulfanyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]cyclopentyl]methyl sulfamate
INCHI	1S/C19H20F3N5O5S2/c20-19(21,22)33-12-3-1-2-10(6-12)13-8-16-24-5-4-15(27(16)26-13)25-14-7-11(17(28)18(14)29)9-32-34(23,30)31/h1-6,8,11,14,17-18,25,28-29H,7,9H2,(H2,23,30,31)/t11-,14-,17-,18+/m1/s1
InChi Key	KJDAGXLMHXUAGV-DGWLBADLSA-N
Smiles	C1C(C(C(C1NC2=CC=NC3=CC(=NN23)C4=CC(=CC=C4)SC(F)(F)F)O)O)COS(=O)(=O)N
Isomeric SMILES	C1[C@@H]([C@H]([C@H]([C@@H]1NC2=CC=NC3=CC(=NN23)C4=CC(=CC=C4)SC(F)(F)F)O)O)COS(=O)(=O)N
PubChem CID	71715374
分子量	519.52

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 100 mg/mL (192.48 mM); Ethanol: 25 mg/mL (48.12 mM); Water: Insoluble;
分子量	519.500 g/mol
XLogP3	2.000
氢键供体数Hydrogen Bond Donor Count	4
氢键受体数Hydrogen Bond Acceptor Count	13
可旋转键计数Rotatable Bond Count	7
精确质量Exact Mass	519.086 Da
单同位素质量Monoisotopic Mass	519.086 Da
拓扑极表面积Topological Polar Surface Area	186.000 Å²
重原子数Heavy Atom Count	34
形式电荷Formal Charge	0
复杂度Complexity	804.000
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	4
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

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批号(Lot Number)	证书类型	货号
F23061210	分析证书	T413978
F23061235	分析证书	T413978
F23061260	分析证书	T413978
F23061263	分析证书	T413978
F23061266	分析证书	T413978
F23061301	分析证书	T413978
F23061321	分析证书	T413978
F23061327	分析证书	T413978
F23061411	分析证书	T413978
F23061424	分析证书	T413978

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TAK-243 (MLN7243)

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