SML2713

MU1210

≥98% (HPLC)

• Sinonimo/i: 1-Methyl-4-(9-(3-(pyridin-4-yl)-phenyl)-7-oxa-2-aza-bicyclo[4.3.0]nona-1,3,5,8-tetraen-3-yl)-1H-pyrazole, 5-(1-Methyl-1H-pyrazol-4-yl)-3-(3-(pyridin-4-yl)phenyl)furo[3,2-b]pyridine, VN339
• Formula empirica (notazione di Hill): C₂₂H₁₆N₄O
• Numero CAS: 2275601-87-9
• Peso molecolare: 352.39
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Stato: powder
• Colore: white to beige
• Solubilità: DMSO: 2 mg/mL, clear
• Temperatura di conservazione: −20°C
• Stringa SMILE: CN(N=C1)C=C1C2=CC=C3C(C(C4=CC=CC(C5=CC=NC=C5)=C4)=CO3)=N2
• InChI: 1S/C22H16N4O/c1-26-13-18(12-24-26)20-5-6-21-22(25-20)19(14-27-21)17-4-2-3-16(11-17)15-7-9-23-10-8-15/h2-14H,1H3; HEAGNKNMQVIVMM-UHFFFAOYSA-N

Descrizione

Azioni biochim/fisiol

ATP site-targeting, potent and selective inhibitor against cdc-like kinase (cdc2-like kinase) CLK1, CLK2, CLK4, and homeodomain-interacting protein kinase 2 (HIPK2), but not CLK3.

MU1210 is a potent and selective inhibitor against cdc-like kinase (cdc2-like kinase) CLK1, CLK2, CLK4 (CLK1/2/4 IC₅₀ = 8/20/12 nM; CLK1/2/4 K_i = 84/91/23 nM by NanoBRET) and HIPK2 (IC₅₀ = 29 nM) with good selectivity over HIPK1/3 (IC₅₀ = 187/159 nM), DYRK1a/1b/2 (IC₅₀ = 213/956/1309 nM), CLK3 (IC₅₀ >3 μM) and 194 other kinases. MU1210 enhances alternative spliced MDM4-S mRNA (10 μM, 24 h) and exhibits antiproliferation activity in MCF7 cultures (IC₅₀ in 72 h = 1.1 μM). Unlike most ATP site-targeting kinase inhibitors, X-ray crystallography shows that MU1210 is anchored to the back pocket instead of the hinge region of CLK1. MU140 serves as a negative control.

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