LDN-192960 2HCl | Haspin and DYRK2/3 inhibitor

CAS:
184582-62-5
Catalog Number:
10-4836
Activity:
Haspin and DYRJ2/3 inhibitor
Chemical Names:
3-(2,7-Dimethoxyacridin-9-yl)sulfanylpropan-1-amine dihydrochloride
Molecular Weight:
401.35
Molecular Formula:
C18H20N2O2S·2HCl
Solubility:
Soluble in DMSO (>25 mg/ml); Water (2 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$55.00
25 mg$195.00

LDN-192960 (184582-62-5) is potent inhibitor of Haspin (IC50 = 10 nM), DYRK2 (IC50 = 2 nM), And DYRK3 (IC50 = 19 nM).1,2 It induced cytotoxicity and growth inhibition in multiple myeloma and triple negative breast cancer cells and triple negative breast cancer mouse allo/xenografts via partial inhibition of 26S proteasome activity.3

References/Citations:

  1. Patnaik et al. (2008), Identification of Small Molecules Inhibitors of the Mitotic Kinase Haspin by High Throughput Screening using a Homogenous Time-Resolved Fluorescence Resonance Transfer Assay; J. Biomol. Screen., 13 1025
  2. Cuny et al. (2010), Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase3 inhibitors; Bioorg. Med. Chem. Lett., 20 3491
  3. Banerjee et al. (2019), Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression; Proc. Natl. Acad. Sci. USA, 116 24881
CAS:
184582-62-5
Catalog Number:
10-4836
Activity:
Haspin and DYRJ2/3 inhibitor
Chemical Names:
3-(2,7-Dimethoxyacridin-9-yl)sulfanylpropan-1-amine dihydrochloride
Molecular Weight:
401.35
Molecular Formula:
C18H20N2O2S·2HCl
Solubility:
Soluble in DMSO (>25 mg/ml); Water (2 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee