SML3958
AZ505
≥98% (HPLC)
Synonym(s):
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
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About This Item
Empirical Formula (Hill Notation):
C29H38Cl2N4O4
CAS Number:
Molecular Weight:
577.54
MDL number:
NACRES:
NA.21
InChI key
LIBVHXXKHSODII-UHFFFAOYSA-N
SMILES string
O=C1NC(C(O)=CC=C2CCNCCN(C3CCCCC3)C(CCNCCC4=CC(Cl)=C(Cl)C=C4)=O)=C2OC1
assay
≥98% (HPLC)
form
powder
color
, White to light brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Related Categories
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.
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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The lysine methyltransferase SMYD2 methylates the kinase domain of type II receptor BMPR2 and stimulates bone morphogenetic protein signaling.
Gao S, et al.
The Journal of Biological Chemistry, 292, 12702-12712 (2017)
Structural basis of substrate methylation and inhibition of SMYD2.
Ferguson AD
Structure, 19(9), 1262-1273 (2011)
Lysine methyltransferase SMYD2 promotes cyst growth in autosomal dominant polycystic kidney disease.
Linda Xiaoyan Li et al.
The Journal of clinical investigation, 127(7), 2751-2764 (2017-06-13)
Autosomal dominant polycystic kidney disease (ADPKD) is driven by mutations in PKD1 and PKD2 genes. Recent work suggests that epigenetic modulation of gene expression and protein function may play a role in ADPKD pathogenesis. In this study, we identified SMYD2
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