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NIK SMI1 - 98%, high purity , CAS No.1660114-31-7, Inhibitor of leucine rich repeat kinase 2;Inhibitor of mitogen-activated protein kinase kinase kinase 14;Inhibitor of mitogen-activated protein kinase kinase kinase kinase 5;Inhibitor of protein kinase D1

  • Moligand™
  • ≥98%
Item Number
N414283
Grouped product items
SKUSizeAvailabilityPrice Qty
N414283-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$42.90
N414283-5mg
5mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$228.90
N414283-10mg
10mg
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$365.90
N414283-25mg
25mg
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$731.90
N414283-50mg
50mg
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$1,263.90

NF-κB Inhibitors

Basic Description

Synonyms(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
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsNIK 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 I
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of leucine rich repeat kinase 2;Inhibitor of mitogen-activated protein kinase kinase kinase 14;Inhibitor of mitogen-activated protein kinase kinase kinase kinase 5;Inhibitor of protein kinase D1
Product Description

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 

Associated Targets

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RELA Tchem Transcription factor p65 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKD1 Tchem Serine/threonine-protein kinase D1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP3K14 Tchem Mitogen-activated protein kinase kinase kinase 14 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

LRRK2 Tchem Leucine-rich repeat serine/threonine-protein kinase 2 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

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
Isomeric SMILES CN1CC[C@](C1=O)(C#CC2=CC(=CC=C2)C3=NC(=CC(=C3)OC)C(=O)N)O
PubChem CID 117902000
Molecular Weight 365.38

Certificates

Certificate of Analysis(COA)

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6 results found

Lot NumberCertificate TypeDateItem
A2422145Certificate of AnalysisDec 18, 2023 N414283
A2422376Certificate of AnalysisDec 18, 2023 N414283
A2422377Certificate of AnalysisDec 18, 2023 N414283
A2422378Certificate of AnalysisDec 18, 2023 N414283
A2422379Certificate of AnalysisDec 18, 2023 N414283
A2422380Certificate of AnalysisDec 18, 2023 N414283

Chemical and Physical Properties

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

Related Documents

References

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,  (1): (179).  [PMID:29330524]

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