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NIK SMI1

PubChem编号: 117902000

有货

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库存信息

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货号 (SKU)	包装规格	是否现货	价格	数量
N612303-5mg	5mg	期货
N612303-25mg	25mg	期货

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leucine rich repeat kinase 2 Inhibitor mitogen-activated protein kinase kinase kinase 14 Inhibitor mitogen-activated protein kinase kinase kinase kinase 5 Inhibitor protein kinase D1 Inhibitor

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基本描述

英文名称	NIK SMI1

名称和标识符

IUPAC Name	6-(3-{2-[(3R)-3-hydroxy-1-methyl-2-oxopyrrolidin-3-yl]ethynyl}phenyl)-4-methoxypyridine-2-carboxamide
INCHI	InChI=1S/C20H19N3O4/c1-23-9-8-20(26,19(23)25)7-6-13-4-3-5-14(10-13)16-11-15(27-2)12-17(22-16)18(21)24/h3-5,10-12,26H,8-9H2,1-2H3,(H2,21,24)/t20-/m0/s1
InChi Key	LQSHXYHWYGKAMX-FQEVSTJZSA-N
Canonical SMILES	COc1cc(nc(c1)c1cccc(c1)C#C[C@]1(O)CCN(C1=O)C)C(=O)N
PubChem CID	117902000

数据库链接

PubChem CID	117902000

关联配体

Ligand ID	9964
名称	NIK SMI1
类别	Synthetic organic
学名	6-(3-{2-[(3R)-3-hydroxy-1-methyl-2-oxopyrrolidin-3-yl]ethynyl}phenyl)-4-methoxypyridine-2-carboxamide
生物活性评价	In a screening panel NIK SMI1 inhibited just 3 off-target kinases, KHS1 (MAP4K5), LRRK2, and PKD1 (PRKD1), by >75% at 1 μM, out of 222 kinases tested. K_i determination established NIK SMI1's selectivity over these off-targets .
评价	NIK SMI1 is a selective inhibitor of the NF-κB-inducing kinase, NIK (MAP3K14) . NIK is a kinase that operates downstream of several TNF family receptors, including BAFF (TNFRSF13C), TWEAK (TNFRSF12A), CD40 (TNFRSF5), and OX40 (TNFRSF4), and which mediates non-canonical NF-κB signaling. Inhibition of NIK recapitulates the inhibition of BAFF that is observed for example using the anti-BAFF, SLE approved biologic . The compound has no effect on canonical NF-κB signaling.

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参考文献

1. Brightbill HD, Suto E, Blaquiere N, Ramamoorthi N, Sujatha-Bhaskar S, Gogol EB, Castanedo GM, Jackson BT, Kwon YC, Haller S et al.. (2018) NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.. Nat Commun, 9 (1): (179). [PMID:29330524]

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