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PJ-68

Names

[ CAS No. ]:
352544-59-3

[ Name ]:
PJ-68

[Synonym ]:
N-[(9-Ethyl-9H-carbazol-3-yl)methyl]-1,2,3,4-tetrahydro-1-naphthalenamine
9H-Carbazole-3-methanamine, 9-ethyl-N-(1,2,3,4-tetrahydro-1-naphthalenyl)-
(9-Ethyl-9H-carbazol-3-ylmethyl)-(1,2,3,4-tetrahydro-naphthalen-1-yl)-amine

Biological Activity

[Description]:

PJ-68 is a potent, selective inhibitor of arginine methyltransferase PRMT5 with IC50 of 517 nM, shows no inhibitory activity against type I PRMT family members ( (PRMT1, 3, 4, 6, and 8); markedly decreases BCR-ABL mRNA levels in both CD34+CD38-cells and CD34+CD38+ cells, reduces survival and self-renewal capacity of CML CD34+ cells, increases p15INK4B and p27KIP1 but not p16INK4A and p57KIP2 expression; reduces growth of CML LSCs and prolongs survival of CML mice.

[References]

References 1. Jin Y, et al. J Clin Invest. 2016 Oct 3;126(10):3961-3980. 2. Kaushik S, et al. Leukemia. 2018 Feb;32(2):499-509. View Related Products by Target Histone Methyltransferase (HMTase)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
553.4±42.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H26N2

[ Molecular Weight ]:
354.487

[ Flash Point ]:
288.5±27.9 °C

[ Exact Mass ]:
354.209595

[ LogP ]:
6.68

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.649


Related Compounds

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