SML1138

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
• 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

Proprietà

• Saggio: ≥98% (HPLC)
• Stato: 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

Descrizione

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.[1] 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).[2]

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).

IKK-16 is a selective inhibitor of IKB kinase (IKK).

Informazioni sulla sicurezza

• 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