HLCL-61 hydrochloride

SKU: orb1226897

Description

A novel potent and selective protein arginine methyltransferase PRMT5 inhibitor; shows no inhibitory activity against the type I (PRMT1 and PRMT4) and type II (PRMT7) PRMT family members; exhibits effective inhibition of symmetric arginine dimethylation (me2) of histones H3 and H4 in AML samples, significantly increases expression of miR-29b and consequent suppression of Sp1 and FLT3 in AML cells; inhibits the proliferation of AML cell lines and primary blasts with IC50 of 7.21-21.46 uM.

Key Properties

• CAS Number: 1158279-20-9
• MW: 380.9104
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₅ClN₂O
• SMILES: CCN1C2=C(C=C(C=C2)CNCC3=CC=CC=C3OC)C4=CC=CC=C41.Cl
• Target: HMTase
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• In Vitro:
  HLCL-61 hydrochloride (1-100 μM; 24-72 hours) reduces cells growth at dose-dependent manner with IC50s of 14.12, 16.74, 6.3, 8.72 μM for MV4-11 cells, THP-1 cells, FLT3-WT blast, and FLT3-ITD blast, respectively. HLCL-61 hydrochloride shows effective inhibition of symmetric arginine dimethylation (me2) of histones H3 and H4 in AML samples, starting at 12 h post-treatment and persisting after 48 h. Cell Viability Assay Cell line: MV4-11 cells, THP-1 cells, FLT3-WT blast (primary blasts from patients), FLT3-ITD blast (primary blasts from patients). Concentration: 1, 5, 10, 25, 50, 100 μM. Incubation time: 24, 48, 72 hours. Result: Dose-dependent reduction in cell viability with IC50s of 14.12, 16.74, 6.3, 8.72 μM for MV4-11 cells, THP-1 cells, FLT3-WT blast, and FLT3-ITD blast, respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HLCL61 hydrochloride | HLCL 61 hydrochloride

Quick Database Links

Gene Symbol

HMTase