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ZAK inhibitor 6p

PubChem编号: 138393294

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货号 (SKU)	包装规格	是否现货	价格	数量
Z614939-5mg	5mg	期货
Z614939-25mg	25mg	期货

查看相关系列

ABL proto-oncogene 1，non-receptor tyrosine kinase Inhibitor BLK proto-oncogene，Src family tyrosine kinase Inhibitor LCK proto-oncogene，Src family tyrosine kinase Inhibitor LIM domain kinase 1 Inhibitor LIM domain kinase 2 Inhibitor receptor interacting serine/threonine kinase 2 Inhibitor ZAK sterile alpha motif and leucine zipper containing kinase AZK Inhibitor

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基本描述

英文名称	ZAK inhibitor 6p

名称和标识符

IUPAC Name	N-(2,4-Difluoro-3-(4-(3-methoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-1H-1,2,3-triazol-1-yl)phenyl)-[1,1'-biphenyl]-3-sulfonamide
INCHI	InChI=1S/C27H19F2N7O3S/c1-39-27-20-13-18(14-30-26(20)32-33-27)23-15-36(35-31-23)25-21(28)10-11-22(24(25)29)34-40(37,38)19-9-5-8-17(12-19)16-6-3-2-4-7-16/h2-15,34H,1H3,(H,30,32,33)
InChi Key	QRDCOOSKIFYKIQ-UHFFFAOYSA-N
Canonical SMILES	COc1n[nH]c2c1cc(cn2)c1nnn(c1)c1c(F)ccc(c1F)NS(=O)(=O)c1cccc(c1)c1ccccc1
PubChem CID	138393294

数据库链接

PubChem CID	138393294

关联配体

Ligand ID	10402
名称	ZAK inhibitor 6p
类别	Synthetic organic
学名	N-(2,4-Difluoro-3-(4-(3-methoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-1H-1,2,3-triazol-1-yl)phenyl)-[1,1'-biphenyl]-3-sulfonamide
生物活性评价	A KINOMEscan® screen identified abelson murine leukemia viral oncogene homolog 1 (ABL1), B lymphoid tyrosine kinase (BLK), FMS like tyrosine kinase 3 (FLT3 ITD, F691L), lymphocyte-specific protein tyrosine kinase (LCK), LIM domain kinase 1 (LIMK1), LIM domain kinase 2 (LIMK2) and receptor-interacting serine/threonine-protein kinase 2 (RIPK2) as off-targets of compound 6p (all inhibited >90% by 1μM compound) .
评价	This compound is reported as a potent, selective and orally active inhibitor of sterile alpha motif and leucine zipper containing kinase (ZAK) . It exhibits predicted antihypertrophic cardiomyopathy (HCM) efficacy in vivo in a spontaneous hypertensive rat (SHR) model.

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参考文献

1. Yang J, Shibu MA, Kong L, Luo J, BadrealamKhan F, Huang Y, Tu ZC, Yun CH, Huang CY, Ding K et al.. (2020) Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.. J Med Chem, 63 (5): (2114-2130). [PMID:31244114]

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