SML3958
AZ505
≥98% (HPLC)
别名:
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
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
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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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