Fig. 1 · Structure

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UNC 0224

Cat. No. A15388 CAS 1197196-48-7

G9a inhibitor

UNC0224 is a potent and selective G9a inhibitor with IC50 of 15 nM in in the G9a Thioglo assay.

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Biological Activity

Target & Activity

Target Activity Value
EHMT1/GLP/KMT1D IC50 20-58 nM
G9a IC50 15 nM
G9a Ki 2.6 nM
G9a Kd 23 nM

Cellular Effect

Cell Line Activity Value Description Reference
MDA-MB-231 IC50 > 5 μM Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay [PMID: 21780790]
MDA-MB-231 EC50 34 μM Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay [PMID: 21780790]
Sf9 IC50 23 nM Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 m [PMID: 31350126]
Sf9 IC50 60 nM Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 m [PMID: 31350126]

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1197196-48-7
Applications G9a inhibitor
Formula C26H43N7O2
Molecular Weight 485.67
SMILES
CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)C)OC)OCCCN(C)C

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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