SML3958

AZ505

≥98% (HPLC)

• Synonim(y): AZ 505, AZ-505, N-Cyclohexyl-3-(3,4-dichlorophenethylamino)-N-(2-(2-(5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethylamino)ethyl)propanamide
• Wzór empiryczny (zapis Hilla): C₂₉H₃₈Cl₂N₄O₄
• Numer CAS: 1035227-43-0
• Masa cząsteczkowa: 577.54
• MDL number: MFCD28044083
• NACRES: NA.21
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder

Właściwości

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: , White to light brown
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C
• SMILES string: O=C1NC(C(O)=CC=C2CCNCCN(C3CCCCC3)C(CCNCCC4=CC(Cl)=C(Cl)C=C4)=O)=C2OC1
• InChI key: LIBVHXXKHSODII-UHFFFAOYSA-N

Opis

Biochem/physiol Actions

Potent and selective SMYD2 inhibitor in vitro and in vivo.

AZ505 is a potent and selective SET and MYND domain-containing protein SMYD2 inhibitor (IC50 = 120 nM) that targets the substrate-binding site in a peptide substrate-competitive and cofactor SAM-uncompetitive manner, exhibiting no activity against lysine methyltransferases (KMTs) SMYD3, DOT1L, EZH2, GLP, G9A and SET7/9 (IC50 >83.3 µM). AZ505 downregulates p53 K370 monomethylation in U2OS cells (10h 10 µM) and delays cyst growth in early- (5 mg/kg/day i.p. from P7-P27) as well as later-stage (10 mg/kg via i.p. 3x per wk from P42-3.5 months, then 1x per wk from 3.5–6 months) Pkd1 conditional knockout mouse models in vivo.

Ta strona może zawierać tekst przetłumaczony maszynowo.

Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• Co się dzieje?: WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable