Home Other Building Blocks IKK Inhibitor III, BMS-345541

IKK Inhibitor III, BMS-345541

CAS No.:
445430-58-0
Catalog Number:
AG00DB56
Molecular Formula:
C14H17N5
Molecular Weight:
255.3183
Pack Size
Purity
Availability
Location
Price(USD)
Quantity
  
5mg
99%
1 week
United States
$226
- +
50mg
99%
1 week
United States
$1123
- +
Product Description
Catalog Number:
AG00DB56
Chemical Name:
IKK Inhibitor III, BMS-345541
CAS Number:
445430-58-0
Molecular Formula:
C14H17N5
Molecular Weight:
255.3183
MDL Number:
MFCD18089812
IUPAC Name:
N'-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
InChI:
InChI=1S/C14H17N5/c1-9-3-4-11-12(7-9)19-10(2)8-17-14(19)13(18-11)16-6-5-15/h3-4,7-8H,5-6,15H2,1-2H3,(H,16,18)
InChI Key:
PSPFQEBFYXJZEV-UHFFFAOYSA-N
SMILES:
NCCNc1nc2ccc(cc2n2c1ncc2C)C
UNII:
26SU0NEF5F
Properties
Complexity:
310  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
0
Defined Bond Stereocenter Count:
0
Exact Mass:
255.148g/mol
Formal Charge:
0
Heavy Atom Count:
19  
Hydrogen Bond Acceptor Count:
4  
Hydrogen Bond Donor Count:
2  
Isotope Atom Count:
0
Molecular Weight:
255.325g/mol
Monoisotopic Mass:
255.148g/mol
Rotatable Bond Count:
3  
Topological Polar Surface Area:
68.2A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
2.3  
Literature
Title Journal
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Sirtuin-1 (SIRT1) is required for promoting chondrogenic differentiation of mesenchymal stem cells. The Journal of biological chemistry 20140808
PDGF-D expression is down-regulated by TGFβ in fibroblasts. PloS one 20140101
Induction of apoptotic death and retardation of neuronal differentiation of human neural stem cells by sodium arsenite treatment. Experimental cell research 20130401
Sodium arsenite exposure inhibits AKT and Stat3 activation, suppresses self-renewal and induces apoptotic death of embryonic stem cells. Apoptosis : an international journal on programmed cell death 20130201
Inhibition of type I interferon-mediated antiviral action in human glioma cells by the IKK inhibitors BMS-345541 and TPCA-1. Journal of interferon & cytokine research : the official journal of the International Society for Interferon and Cytokine Research 20120801
Flavivirus infection induces indoleamine 2,3-dioxygenase in human monocyte-derived macrophages via tumor necrosis factor and NF-κB. Journal of leukocyte biology 20120401
Targeting IKK/NF-κB pathway reduces infiltration of inflammatory cells and apoptosis after spinal cord injury in rats. Neuroscience letters 20120305
IκB kinases modulate the activity of the androgen receptor in prostate carcinoma cell lines. Neoplasia (New York, N.Y.) 20120301
Activation of the IκB kinase complex by HTLV-1 Tax requires cytosolic factors involved in Tax-induced polyubiquitination. Journal of biochemistry 20111201
Comprehensive analysis of kinase inhibitor selectivity. Nature biotechnology 20111030
Targeting AML through DR4 with a novel variant of rhTRAIL. Journal of cellular and molecular medicine 20111001
Kinase inhibitors modulate huntingtin cell localization and toxicity. Nature chemical biology 20110529
AMP-activated protein kinase suppresses matrix metalloproteinase-9 expression in mouse embryonic fibroblasts. The Journal of biological chemistry 20110506
Improved intraportal islet transplantation outcome by systemic IKK-beta inhibition: NF-κB activity in pancreatic islets depends on oxygen availability. American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons 20110201
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis. Bioorganic & medicinal chemistry letters 20110101
IKKβ regulates the repair of DNA double-strand breaks induced by ionizing radiation in MCF-7 breast cancer cells. PloS one 20110101
IGF-1 and PDGF-bb suppress IL-1β-induced cartilage degradation through down-regulation of NF-κB signaling: involvement of Src/PI-3K/AKT pathway. PloS one 20110101
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chemistry & biology 20101124
Small molecule inhibitors of IkappaB kinase signaling inhibit osteoclast formation in vitro and prevent ovariectomy-induced bone loss in vivo. FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20101101
In CD28-costimulated human naïve CD4+ T cells, I-κB kinase controls the expression of cell cycle regulatory proteins via interleukin-2-independent mechanisms. Immunology 20101001
Up-regulation of bradykinin receptors in rat bronchi via I kappa B kinase-mediated inflammatory signaling pathway. European journal of pharmacology 20100525
Inhibitor of kappaB kinase beta regulates redox homeostasis by controlling the constitutive levels of glutathione. Molecular pharmacology 20100501
Characterizing the involvement of the nuclear factor-kappa B (NF kappa B) transcription factor in uveal melanoma. Investigative ophthalmology & visual science 20100401
Primary human acute myelogenous leukemia cells release matrix metalloproteases and their inhibitors: release profile and pharmacological modulation. European journal of haematology 20100301
Inhibition of IKK-beta: a new development in the mechanism of the anti-obesity effects of PTP1B inhibitors SA18 and SA32. Bioorganic & medicinal chemistry letters 20100201
Targeting the angiopoietin (Ang)/Tie-2 pathway in the crosstalk between acute myeloid leukaemia and endothelial cells: studies of Tie-2 blocking antibodies, exogenous Ang-2 and inhibition of constitutive agonistic Ang-1 release. Expert opinion on investigational drugs 20100201
A role for IL-17 in induction of an inflammation at the fetomaternal interface in preterm labour. Journal of reproductive immunology 20100101
Targeting the Fanconi anemia/BRCA pathway circumvents drug resistance in multiple myeloma. Cancer research 20091215
The effect of microenvironmental CD40 signals on TRAIL- and drug-induced apoptosis in follicular lymphoma cells. Scandinavian journal of immunology 20091201
Periodic, partial inhibition of IkappaB Kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis. The Journal of pharmacology and experimental therapeutics 20091101
Tumor necrosis factor-alpha (TNF-alpha) induces upregulation of RhoA via NF-kappaB activation in cultured human bronchial smooth muscle cells. Journal of pharmacological sciences 20090801
Inflammatory NF-kappaB activation promotes hepatic apolipoprotein B100 secretion: evidence for a link between hepatic inflammation and lipoprotein production. American journal of physiology. Gastrointestinal and liver physiology 20090601
p65 activity and ZAP-70 status predict the sensitivity of chronic lymphocytic leukemia cells to the selective IkappaB kinase inhibitor BMS-345541. Clinical cancer research : an official journal of the American Association for Cancer Research 20090415
Novel tricyclic inhibitors of IkappaB kinase. Journal of medicinal chemistry 20090409
Molecular determinants of melanoma malignancy: selecting targets for improved efficacy of chemotherapy. Molecular cancer therapeutics 20090301
Modulation of TNF-alpha-induced endothelial cell activation by glucosamine, a naturally occurring amino monosaccharide. International journal of molecular medicine 20081201
JNK- and IkappaB-dependent pathways regulate MCP-1 but not adiponectin release from artificially hypertrophied 3T3-L1 adipocytes preloaded with palmitate in vitro. American journal of physiology. Endocrinology and metabolism 20080501
The selectivity of protein kinase inhibitors: a further update. The Biochemical journal 20071215
Diverse TNFalpha-induced death pathways are enhanced by inhibition of NF-kappaB. International journal of oncology 20071201
Activin A is an anticatabolic autocrine cytokine in articular cartilage whose production is controlled by fibroblast growth factor 2 and NF-kappaB. Arthritis and rheumatism 20071101
The IKK inhibitor BMS-345541 affects multiple mitotic cell cycle transitions. Cell cycle (Georgetown, Tex.) 20071015
Antioxidants tiron and N-acetyl-L-cysteine differentially mediate apoptosis in melanoma cells via a reactive oxygen species-independent NF-kappaB pathway. Free radical biology & medicine 20070501
IFN-gamma-induced upregulation of Fcgamma-receptor-I during activation of monocytic cells requires the PKR and NFkappaB pathways. Molecular immunology 20070101
Duration and intensity of NF-kappaB activity determine the severity of endotoxin-induced acute lung injury. Journal of immunology (Baltimore, Md. : 1950) 20060415
BMS-345541 targets inhibitor of kappaB kinase and induces apoptosis in melanoma: involvement of nuclear factor kappaB and mitochondria pathways. Clinical cancer research : an official journal of the American Association for Cancer Research 20060201
IKK mediates ischemia-induced neuronal death. Nature medicine 20051201
Collagen and aggrecan degradation is blocked in interleukin-1-treated cartilage explants by an inhibitor of IkappaB kinase through suppression of metalloproteinase expression. The Journal of pharmacology and experimental therapeutics 20051001
Inhibition of IKK down-regulates antigen + IgE-induced TNF production by mast cells: a role for the IKK-IkappaB-NF-kappaB pathway in IgE-dependent mast cell activation. Journal of leukocyte biology 20050601
Features of selective kinase inhibitors. Chemistry & biology 20050601
Anti-inflammatory inhibitors of IkappaB kinase in asthma and COPD. Current opinion in investigational drugs (London, England : 2000) 20041101
A highly selective inhibitor of IkappaB kinase, BMS-345541, augments graft survival mediated by suboptimal immunosuppression in a murine model of cardiac graft rejection. Transplantation 20040415
An inhibitor of IkappaB kinase, BMS-345541, blocks endothelial cell adhesion molecule expression and reduces the severity of dextran sulfate sodium-induced colitis in mice. Inflammation research : official journal of the European Histamine Research Society ... [et al.] 20031201
A highly selective inhibitor of I kappa B kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice. Arthritis and rheumatism 20030901
BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice. The Journal of biological chemistry 20030117
Properties