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AZ505 ditrifluoroacetate

Catalog No. T10427 CAS 1035227-44-1

AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).

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AZ505 ditrifluoroacetate Chemical Structure

AZ505 ditrifluoroacetate, CAS 1035227-44-1

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).
Targets&IC50	SMYD2:0.12 μM
In vitro	AZ505 ditrifluoroacetate is highly selective and shows activity at submicromolar concentrations in vitro. The IC50 of AZ505 ditrifluoroacetate for SMYD2 is 0.12 μM, which is >600-fold greater than the IC50s for other histone methyltransferases, such as SMYD3 (IC50>83.3 μM), DOT1L (IC50>83.3 μM) [1]. AZ505 ditrifluoroacetate is nominated for ITC binding study (Kd: 0.5 μM). In contrast, the calculated Kd for the p53 substrate peptide is 3.7 μM. 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].

Molecular Weight	805.59
Formula	C33H40Cl2F6N4O8
CAS No.	1035227-44-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (155.17 mM)

References and Literature

1. Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20;112(2):357-64. 2. Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73.

Citations

1. Li X, Wang Y, Zhang Y, et al. Overexpression of MCAM induced by SMYD2-H3K36me2 in breast cancer stem cell properties. Breast Cancer. 2022: 1-15

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Keywords

AZ505 ditrifluoroacetate 1035227-44-1 Chromatin/Epigenetic Histone Methyltransferase AZ 505 AZ-505 Ditrifluoroacetate AZ505 Ditrifluoroacetate AZ-505 AZ 505 Ditrifluoroacetate AZ-505 ditrifluoroacetate AZ505 inhibitor inhibit

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