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Fig. 1 · Structure
Cat. No.
A16861
CAS No.
2086772-26-9
Formula
C22H23BrN6O2
Mol. Weight
483.37

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Onametostat (JNJ-64619178)

Cat. No. A16861 CAS 2086772-26-9

Histone Methyltransferase inhibitor

JNJ-64619178 is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
A549 IC50 0.25 nM Inhibition of PRMT5 in human A549 cells assessed as reduction in sDMA production after 48 hrs by Hoechst Stain/HCS CellMask Deep Red Stain based immunohistochemistry method [PMID: 30956011]
Sf9 IC50 0.13 nM Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infected Sf9 insect cells assessed as reduction of S-adenosyl-L-homocysteine formation using human recombinant [PMID: 30956011]
Sf9 IC50 0.14 nM Inhibition of full-length human N-terminal FLAG-tagged PRMT5 expressed in Sf9 insect cells using histone H2A as peptide after 120 mins in presence of SAM by high throughput mass spectrometer assay [PMID: 30366617]

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 2086772-26-9
Applications Histone Methyltransferase inhibitor
Formula C22H23BrN6O2
Molecular Weight 483.37
Synonyms JNJ64619178
SMILES
BrC1=C(N)N=C(C=C(CC[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C(N=CN=C4N)=C4C=C3)C2)C=C5)C5=C1

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 94 mg/mL (194.47 mM)

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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