Comparison

AZ505 (ditrifluoroacetate)

Item no. CS-1734-100mg
Manufacturer ChemScene
Amount 100mg
Category
Type Molecules
Specific against other
ECLASS 10.1 32169090
ECLASS 11.0 32169090
UNSPSC 12000000
Similar products 1035227-44-1
Available
CAS
1035227-44-1
Purity
>98%
Formula
C33H40Cl2F6N4O8
MWt
805.59
Solubility
DMSO : >= 125 mg/mL (155.17 mM)
Clinical Information
No Development Reported
Pathway
Epigenetics
Target
Histone Methyltransferase
Biological Activity
AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 uM. IC50 & Target: IC50: 0.12 uM (SMYD2)[1] In Vitro: AZ505 ditrifluoroacetate is highly selective and shows an activity at submicromolar concentrations in vitro. The IC50 of AZ505 ditrifluoroacetate for SMYD2 is 0.12 uM, which is >600-fold greater than the IC50s of AZ505 ditrifluoroacetate for other histone methyltransferases, such as SMYD3 (IC50>83.3 uM), DOT1L (IC50>83.3 uM) and AZ505 ditrifluoroacetate (IC50>83.3 uM)[1]. AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 uM. The human SMYD (SET and MYND domain-containing protein) family of protein lysine methyltransferases contains five members (SMYD1-5). Moreover, AZ505 ditrifluoroacetate fails to inhibit the enzymatic activities of a panel of protein lysine methyltransferases. AZ505 ditrifluoroacetate is nominated for ITC binding study with Kd of 0.5 uM. In contrast, the calculated Kd for the p53 substrate peptide is 3.7 uM. AZ505 ditrifluoroacetate binding to SMYD2 is driven primarily by entropy, which often suggests that binding is mediated by hydrophobic interactions with few specific hydrogen bonds[2].

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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 100mg
Available: In stock
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