You are here:Home-Chemical Inhibitors & Agonists-Epigenetics-Histone Methyltransferase (HMTase)-KMI169
KMI169

Chemical Structure : KMI169

CAS No.:

KMI169 (KMI-169, KMI 169)

Catalog No.: PC-21606Not For Human Use, Lab Use Only.

KMI169 (KMI-169) is a potent and selective lysine methyltransferase 9 (KMT9) inhibitor with ITC Kd of 25 nM and enzymatic IC50 of 50 nM.

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

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    KMI169 (KMI-169) is a potent and selective lysine methyltransferase 9 (KMT9) inhibitor with ITC Kd of 25 nM and enzymatic IC50 of 50 nM.
    KMI169 displays high selectivity for KMT9 against a large panel of SET domain- or Rossmann fold-containing methyltransferases as well as protein kinases.
    KMI169 dispalys a linear dependence upon increasing SAM or substrate concentrations corroborating a competitive inhibition mode.
    KMI169 demonstrates cell membrane permeability and cellular target engagement, impairs tumour cell proliferation with GI50 of 120 nM in PC-3M cells, as well as in other prostate, bladder, lung, and colon tumour cells.
    KMI169 also impairs proliferation of castration- and enzalutamide-resistant prostate cancer cell lines such as PC-3M, DU145, LNCaP-abl, and LNCaP-abl EnzaR.
    KMI169 affects expression of genes involved in cell cycle regulation, including MYB proto-oncogene (MYB), aurora kinase B (AURKB), forkhead box A2 (FOXA2), cyclin dependent kinase 2 (CDK2), baculoviral iap repeat containing 5 (BIRC5), E2F transcription factor 1 (E2F1), E2F transcription factor 8 (E2F8), cell division cycle 6 (CDC6), and DNA ligase 1 (LIG1).
    KMI169 is a suitable tool to study cellular KMT9 functions.

    Physicochemical Properties

    M.Wt 604.54
    Formula C31H31Cl2N7O2
    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

    (1R,2S,3R,5R)-3-(4-amino-5-(1-benzyl-4-chloro-1H-pyrazol-3-yl)-2-chloro-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-(3-(azetidin-1-ylmethyl)phenyl)cyclopentane-1,2-diol

    References

    1. Sheng Wang, et al. Nat Commun. 2024 Jan 2;15(1):43.

    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: