SML1138
IKK-16 dihydrochloride
≥98% (HPLC), IKB kinase inhibitor, powder
别名:
N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamide dihydrochloride, IKK16 hydrochloride
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关于此项目
经验公式（希尔记法）:
C28H29N5OS · 2HCl
化学文摘社编号:
分子量:
556.55
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
产品名称
IKK-16 dihydrochloride, ≥98% (HPLC)
SMILES string
O=C(N1CCC(N2CCCC2)CC1)C3=CC=C(NC4=NC=CC(C5=CC(C=CC=C6)=C6S5)=N4)C=C3.C
InChI
1S/C28H29N5OS.CH4/c34-27(33-17-12-23(13-18-33)32-15-3-4-16-32)20-7-9-22(10-8-20)30-28-29-14-11-24(31-28)26-19-21-5-1-2-6-25(21)35-26;/h1-2,5-11,14,19,23H,3-4,12-13,15-18H2,(H,29,30,31);1H4
InChI key
YJGZKHHCMOHIFA-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
−20°C
Quality Level
Application
IKK-16 dihydrochloride has been used as an nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor kinase inhibitor (IκB) in B220+ CKO or CreWT naive B cells. It has also been used as a nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB inhibitor) in poly(I:C) transfection-induced retinoic acid-inducible gene (RIG-I), melanoma differentiation-associated gene 5 (MDA-5), and caspase-11 expressing mouse embryonic fibroblasts (MEFs).
Biochem/physiol Actions
IKK-16 is a selective inhibitor of IKB kinase (IKK), part of the upstream NF-KB signal transduction cascade involved in the cellular response to inflammation. IKK-16 has IC50 values of 40, 70 and 200 nM for IKKβ (IKK-2), IKK complex and IKKα (IKK-1) respectively. In a mouse sepsis model, IKK-16 reduced the multiple organ dysfunction, showing an antiinflammatory and endothelial protective effect likely mediated by inhibition of inflammation through NF-KB. IKK-16 has also been found to have some activity as an inhibitor of protein kinase D (PKD) and of multidrug resistance protein 1 (MDR1, ABCB1).
IKK-16 is a selective inhibitor of IKB kinase (IKK).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Robert R Haines et al.
Journal of immunology (Baltimore, Md. : 1950), 203(7), 1867-1881 (2019-09-08)
Marginal zone B cells (MZB) are a mature B cell subset that rapidly respond to blood-borne pathogens. Although the transcriptional changes that occur throughout MZB development are known, the corresponding epigenetic changes and epigenetic modifying proteins that facilitate these changes
Zhenyi Su et al.
Cell death and differentiation, 26(6), 1077-1088 (2018-10-21)
ABIN-1 (encoded by the gene Tnip1) is a ubiquitin-binding protein that can interact with ubiquitin-editing enzyme A20 (encoded by the gene TNFAIP3) to restrain the activation of necroptosis and NF-κB activation. Genetic variants in the genes Tnip1 and TNFAIP3 are
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