| Field | Specification |
|---|---|
| Applications | |
| Molecular weight | |
| Molecular formula | C27H36Cl2N8O5 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PNMT-IN-1 is a specific inhibitor of phenylethanolamine N-methyltransferase (PNMT), with a Ki of 1.2 nM and an IC50 of 81 nM. It also inhibits DNMT1 and DNMT3b activity, with IC50 values of 61 μM and 17 μM, respectively, antagonizes epinephrine, and represents a second-generation inhibitor[1]. It has the molecular formula C27H36Cl2N8O5 and a molecular weight of 623.53 g/mol.
Physical & Chemical Properties
| Molecular Formula | C27H36Cl2N8O5 |
|---|---|
| Molecular Weight | 623.53 g/mol |
| SMILES | ClC1=C(Cl)C=CC2=C1CNCC2CCCCN(C[C@@H]3[C@@H](O)[C@@H](O)[C@H](N4C=NC5=C4N=CN=C5N)O3)CC[C@H](N)C(O)=O |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50:81 nM (Phenylethanolamine N-methyltransferase, PNMT )[1] IC50:61 nM (DNMT1)[1] IC50:17 nM (DNMT3b)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
PNMT-IN-1 (inhibitor 4) (0.01 μM, 4h) inhibits hPNMT activity (IC50= 81 nM) without affecting protein methylation[1].
Cell Viability Assay
| Cell Line | Overexpressed hPNMT in HEK293T cells using a lentiviral vector[1] |
|---|---|
| Concentration | 0-10 μM |
| Incubation Time | 24 h |
| Result | Inhibted the activity of hPNMT (IC50=81nM) |
Western Blot Analysis
| Cell Line | HT-29 cell[1] |
|---|---|
| Concentration | 10 μg |
| Incubation Time | 6 days |
| Result | Changed total SDMA, ADMA, and Me3-lysine not significant. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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