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SML1138

Sigma-Aldrich

IKK-16 dihydrochloride

≥98% (HPLC)

Sinonimo/i:

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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About This Item

Formula empirica (notazione di Hill):
C28H29N5OS · 2HCl
Numero CAS:
873225-46-8
Peso molecolare:
556.55
Codice UNSPSC:
12352200
ID PubChem:
329825674
NACRES:
NA.77

Saggio

≥98% (HPLC)

Forma fisica

powder

Condizioni di stoccaggio

desiccated

Colore

white to beige

Solubilità

DMSO: 20 mg/mL, clear

Temperatura di conservazione

−20°C

Stringa SMILE

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
YJGZKHHCMOHIFA-UHFFFAOYSA-N

Applicazioni

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).

Azioni biochim/fisiol

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).

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

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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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