HLCL-61 hydrochloride

Research use only, not for human use.

A novel potent and selective protein arginine methyltransferase PRMT5 inhibitor.

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.

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 AssayCell 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 μMIncubation 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.

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HLCL61 hydrochloride | HLCL 61 hydrochloride

Chromatin/Epigenetic

HMTase

PRMT5

Cancer

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1158279-20-9

380.9104

C23H25ClN2O

>98% (HPLC)

DMSO: ≥ 30 mg/mL

CCN1C2=C(C=C(C=C2)CNCC3=CC=CC=C3OC)C4=CC=CC=C41.Cl

9H-Carbazole-3-methanamine, 9-ethyl-N-[(2-methoxyphenyl)methyl]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years