You are here:Home-Chemical Inhibitors & Agonists-Epigenetics-Histone Methyltransferase (HMTase)-G9a/NSD2 dual inhibitor 16
G9a/NSD2 dual inhibitor 16

Chemical Structure : G9a/NSD2 dual inhibitor 16

CAS No.: 2761292-51-5

G9a/NSD2 dual inhibitor 16 (W4032)

Catalog No.: PC-22701Not For Human Use, Lab Use Only.

G9a/NSD2 dual inhibitor 16 (W4032) is a highly potent G9a/NSD2 dual inhibitor with IC50 of 241/17 nM respectively, shows potent cell growth inhibition against PANC-1 and MDA-MB-231 with IC50 values of 0.44 and 0.72 μM, respectively.

Packing Price Stock Quantity
25 mg Get quote
50 mg Get quote
100 mg Get quote

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC)

Biological Activity

G9a/NSD2 dual inhibitor 16 (W4032) is a highly potent G9a/NSD2 dual inhibitor with IC50 of 241/17 nM respectively, shows potent cell growth inhibition against PANC-1 and MDA-MB-231 with IC50 values of 0.44 and 0.72 μM, respectively.
G9a/NSD2 dual inhibitor 16 has an IC50 of 0.41 μM for the GLP, shows selectivity over PRMT1 (IC60=6.44 uM) and has no activity for PRMT4, PRMT5, EZH2, MLL1, MLL4 and DNMT1 up to 10 μM.
G9a/NSD2 dual inhibitor 16 significantly inhibis the colony formation of MDA-MB-231 and PANC-1 cells in a dose-dependent manner, induces apoptosis.
G9a/NSD2 dual inhibitor 16 inhibits invasion of MDA-MB-231 and PANC-1 cells dose-dependently.
G9a/NSD2 dual inhibitor 16 (4-16 mg/kg) exhibits vivo antitumor activity in PANC-1 cell-derived xenograft.

Physicochemical Properties

M.Wt 452.60
Formula C25H36N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-[(1-Isopropylpiperidin-4-yl)amino]-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline-2-carbonitrile

References

1. Chunju Yang, et al. J Med Chem. 2024 Jul 15. doi: 10.1021/acs.jmedchem.4c00640.

Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

Contact Us sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

Get Quote

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • Additional Information: