LDN-192960 2HCl

Modify Date: 2024-01-08 07:08:48

LDN-192960 2HCl Structure
LDN-192960 2HCl structure
Common Name LDN-192960 2HCl
CAS Number 184582-62-5 Molecular Weight 328.429
Density 1.3±0.1 g/cm3 Boiling Point 536.1±40.0 °C at 760 mmHg
Molecular Formula C18H20N2O2S Melting Point N/A
MSDS N/A Flash Point 278.0±27.3 °C

 Use of LDN-192960 2HCl


LDN-192960 is a potent Haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase) inhibitor with an IC50 of 0.010 µM.

 Names

Name 3-((2,7-dimethoxyacridin-9-yl)thio)propan-1-amine
Synonym More Synonyms

 LDN-192960 2HCl Biological Activity

Description LDN-192960 is a potent Haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase) inhibitor with an IC50 of 0.010 µM.
Related Catalog
Target

IC50: 0.010 μM (Haspin)[1]

In Vitro A comparison of the profiles of LDN-192960 (compound 3) and 42 suggests that only six kinases, including haspin, are inhibited by both compounds ≥90% at 10 µM[1]. LDN-192960 alone does not cause detectable mitotic exit in the mitotic (phospho)-protein monoclonal-2 (MPM-2) assay in HeLa cells. In the presence of 1 µM ZM447439, even concentrations as low as 0.1 µM LDN-192960 cause substantial loss of MPM-2 epitopes, and similar results are obtained in the presence of Hesperadin. However, 10 µM LDN-192960 does not cause mitotic exit in combination with Aurora B inhibition, which is consistent with off-target effects at this higher dose[2].
Cell Assay U2OS cells and H2B-mRFP are used. For imaging, mitotic cells arrested in 5 µM nocodazole for ~8 h are harvested by “shake-off” and replated in 10% FBS, 25 mM Hepes, and phenol red-free DME containing 5 µM nocodazole in a 35-mm single chamber or 35-mm 4-chamber glass-bottom dishes coated with poly-d-lysine. Time-lapse confocal fluorescence imaging is performed using an inverted microscope. Immediately after kinase inhibitor (including LDN-192960) addition, two-color z stacks with 0.8 µm steps are collected with a 100-nm pinhole every 5 min for 15 h[2].
References

[1]. Cuny GD, et al. Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. Bioorg Med Chem Lett. 2012 Mar 1;22(5):2015-9.

[2]. Fangwei Wang, et al. Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation. J Cell Biol. 2012 Oct 15; 199(2): 251-268.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 536.1±40.0 °C at 760 mmHg
Molecular Formula C18H20N2O2S
Molecular Weight 328.429
Flash Point 278.0±27.3 °C
Exact Mass 328.124542
PSA 82.67000
LogP 3.52
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.672

 Safety Information

Hazard Codes Xi

 Synonyms

3-[(2,7-Dimethoxy-9-acridinyl)sulfanyl]-1-propanamine
1-Propanamine, 3-[(2,7-dimethoxy-9-acridinyl)thio]-
ldn-192960
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