LDN-209929 di-HCl is a potent and specific inhibitor of haspin kinase (IC50=55 nM), with 180-fold selectivity over DYRK2 (IC50=9.9 μM). LDN-209929 is the optimized product of LDN-192960.

Physicochemical Properties

Molecular Formula	C17H19CL3N2OS
Molecular Weight	405.769560098648
Exact Mass	404.028
CAS #	1784281-97-5
PubChem CID	90488975
Appearance	Yellow to orange solid powder
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	5
Heavy Atom Count	24
Complexity	360
Defined Atom Stereocenter Count	0
SMILES	ClC1C=CC2=C(C=1)C(=C1C=C(C=CC1=N2)OC)SCCCN.Cl.Cl
InChi Key	WOCCOXNODBCCGK-UHFFFAOYSA-N
InChi Code	InChI=1S/C17H17ClN2OS.2ClH/c1-21-12-4-6-16-14(10-12)17(22-8-2-7-19)13-9-11(18)3-5-15(13)20-16;;/h3-6,9-10H,2,7-8,19H2,1H3;2*1H
Chemical Name	3-(2-chloro-7-methoxyacridin-9-yl)sulfanylpropan-1-amine;dihydrochloride
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	IC50: 55 nM (haspin kinase) IC50: 9.9 μM (DYRK2)[1]
ln Vitro	Serine/threonine kinase Haspin, also known as Haploid Germ Cell-Specific Nuclear Protein Kinase, is expressed in a number of different tissues, including the testis, bone marrow, thymus, and spleen. Furthermore, haspin is crucial during mitosis, where it phosphorylates histone H3 at Thr-3 (H3T3) in G2/early prophase, reaches its peak in prometaphase/metaphase, and then starts to decline in anaphase[1]. DYRKs are ePKs that are a part of the CMGC family. They are further classified into two classes: class 2 kinases (DYRK2, 3, and 4) and class 1 kinases (DYRK1A and 1B). During synthesis, a critical activation loop tyrosine is autophosphorylated, which is necessary for DYRK activity[1].
References	[1]. Structure-activity Relationship Study of Acridine Analogs as Haspin and DYRK2 Kinase Inhibitors. Bioorg Med Chem Lett. [2]. Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin. Curr Med Chem. 2017;24(21):2276-2293.

Solubility Data

Solubility (In Vitro)

DMSO : 33.33 mg/mL (82.14 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4645 mL	12.3223 mL	24.6445 mL
	5 mM	0.4929 mL	2.4645 mL	4.9289 mL
	10 mM	0.2464 mL	1.2322 mL	2.4645 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.