5.34356

PRMT5 Inhibitor, CMP5

• Synonym(s): PRMT5 Inhibitor, CMP5, 1-(9-Ethyl-9H-carbazol-3-yl)-N-(2-pyridinylmethyl)methanamine, 2HCl, 1-(9-Ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine, 2HCl
• Empirical Formula (Hill Notation): C₂₁H₂₁N₃ · 2HCl
• Molecular Weight: 388.33
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: yellow
• solubility: DMSO: 25 mg/mL; water: 50 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell-permeable carbazole based compound that selectively inhibits PRMT5 and not PRMT1, PRMT4 & PRMT7 activity. Shown to occupy hPRMT5 catalytic site and block symmetrically dimethylated S2Me-H4R3 & S2Me-H3R8 with no effect on the asymmetric methylation of H4R3 in lymphoblastoid cell lines at 40 µM. Prevents Epstein-Barr virus (EBV)-driven B cell immortalization and restores miR-96 transcriptional activity. Dose-dependently induces lymphoma cell death over normal resting B lymphocytes.

A cell-permeable carbazole based compound that selectively inhibits PRMT5 and not PRMT1, PRMT4 & PRMT7 activity. Shown to occupy hPRMT5 catalytic site and block symmetrically dimethylated S2Me-H4R3 & S2Me-H3R8 with no effect on the asymmetric methylation of H4R3 in lymphoblastoid cell lines at 40 µM. Prevents Epstein-Barr virus (EBV)-driven B cell immortalization and restores miR-96 transcriptional activity. Dose-dependently induces lymphoma cell death over normal resting B lymphocytes.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PRMT5

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

Supplied as HCl salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Alinari, L., et al. 2015. Blood.125, 2530.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable