1. Cell Cycle/DNA Damage
  2. Haspin Kinase

LDN-192960 

Cat. No.: HY-13455 Purity: 99.56%
Handling Instructions

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

For research use only. We do not sell to patients.

LDN-192960 Chemical Structure

LDN-192960 Chemical Structure

CAS No. : 184582-62-5

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & 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].

References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

328.43

Formula

C₁₈H₂₀N₂O₂S

CAS No.

184582-62-5

SMILES

NCCCSC1=C(C=C(OC)C=C2)C2=NC3=CC=C(OC)C=C31

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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LDN-192960
Cat. No.:
HY-13455
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LDN-192960

Cat. No.: HY-13455