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NIK SMI1

NF-κB 抑制剂

规格或纯度: 98%

CAS编号: 1660114-31-7
分子式: C₂OH₁₉N₃O₄?
分子量: 365.38
PubChem编号: 117902000

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货号 (SKU)	包装规格	是否现货	价格	数量
N414283-1mg	1mg	现货
N414283-5mg	5mg	现货
N414283-10mg	10mg	现货
N414283-25mg	25mg	现货
N414283-50mg	50mg	现货

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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

规格或纯度	98%
英文名称	NIK SMI1
别名	(R)-6-(3-((3-Hydroxy-1-methyl-2-oxopyrrolidin-3-yl)-ethynyl)phenyl)-4-methoxypicolinamide, 6-[3-[2-[(3R)-3-Hydroxy-1-methyl-2-oxo-3-pyrrolidinyl]ethynyl]phenyl]-4-methoxy-2-pyridinecarboxamide, NIK small molecule inhibitor 1
英文别名	(R)-6-(3-((3-Hydroxy-1-methyl-2-oxopyrrolidin-3-yl)-ethynyl)phenyl)-4-methoxypicolinamide, 6-[3-[2-[(3R)-3-Hydroxy-1-methyl-2-oxo-3-pyrrolidinyl]ethynyl]phenyl]-4-methoxy-2-pyridinecarboxamide, NIK small molecule inhibitor 1
生化机理	NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM for NIK-catalyzed hydrolysis of ATP to ADP.NIK SMI1 is an orally active, ATP site-targeting, potent and selective NF-κB-inducing kinase inhibitor (h/m NIK IC50 = 230/395 pM; hKHS1/hPKD1/hLRRK2 = 49.6/75.2/247.8 nM) that selectively disrupts noncanonical NF-κB signaling (anti-LTβR-induced p52 nuclear translocation IC50 = 70 nM; TNFα-induced p65 RelA nuclear translocation IC50 >2 μM). SMI1 inhibits BAFF receptor- and CD40-mediated singling in cultures (human and murine B-cells) and shows in vivo efficacy in the NZB/W F1 murine experimental lupus model (6-400?mg/kg/day, b.i.d. p.o.).
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Information NIK SMI1 NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM for NIK-catalyzed hydrolysis of ATP to ADP. Targets NIK-catalyzed hydrolysis of ATP to ADP 0.23 nM(Ki) In vitro NIK SMI1 exhibits selective inhibition of LTβR-dependent p52 translocation and transcription of NF-κB2 related genes. NIK SMI1 is shown to have a favorable pharmacokinetic profile across species and to inhibit BAFF-induced B cell survival in vitro. In vivo NIK SMI1 inhibits BAFF signaling and reduces splenic marginal zone B cells in vivo. Cell Research(from reference) Cell lines：293 cells, HeLa cells, SF9 cell line, Human B cells, Mouse B cells? Concentrations：1 μM, different concentrations? Incubation Time：24 h, 5 h?

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	CN1CCC(C1=O)(C#CC2=CC(=CC=C2)C3=NC(=CC(=C3)OC)C(=O)N)O
PubChem CID	117902000
分子量	365.38

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 73 mg/mL (199.79 mM); Water: Insoluble; Ethanol: Insoluble;

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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