| Identification | Back Directory | [Name]
AZ505 | [CAS]
1035227-43-0 | [Synonyms]
CS-2253
AZ-505;AZ 505
N-Cyclohexyl-N3-[2-(3,4-dichlorophenyl)ethyl]-N-(2-{[2-(5-hydroxy-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-8-yl)ethyl]amino}ethyl)-alaninamide
N-Cyclohexyl-3-(3,4-dichlorophenethylamino)-N-[2-[[2-[5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl]ethyl]amino]ethyl]propanamide
Propanamide, N-cyclohexyl-3-[[2-(3,4-dichlorophenyl)ethyl]amino]-N-[2-[[2-(3,4-dihydro-5-hydroxy-3-oxo-2H-1,4-benzoxazin-8-yl)ethyl]amino]ethyl]- | [Molecular Formula]
C29H38Cl2N4O4 | [MDL Number]
MFCD28044083 | [MOL File]
1035227-43-0.mol | [Molecular Weight]
577.54 |
| Chemical Properties | Back Directory | [Boiling point ]
782.5±60.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
crystalline solid | [pka]
8.59±0.20(Predicted) | [color ]
Off-white to light brown |
| Hazard Information | Back Directory | [Uses]
AZ505 is a potent inhibitor of SMYD2, which plays an important role in epigenetic signalling. Inhibiition of SMYD2 also functions as an activator of the tumor suppressor proteins. | [Biological Activity]
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) th at targets the substrate-binding site in a peptide substrate-competitive and cofactor SAM-uncompetitive mannerexhibiting no activity against lysine methyltransferases (KMTs) SMYD3DOT1LEZH2GLPG9A 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 monthsthen 1x per wk from 3.5–6 months) Pkd1 conditional knockout mouse models in vivo. | [IC 50]
SMYD2 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|