LDN-192960 hydrochloride

Name: LDN-192960 hydrochloride
Brand: MedChemExpress
SKU: HY-13455A
Rating: 5.0 (2 reviews)

Cat. No.: HY-13455A Purity: 99.76%: Data Sheet
COA

SDS
Handling Instructions
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LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC₅₀s of 10 nM and 48 nM, respectively.

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

LDN-192960 hydrochloride Chemical Structure

CAS No. : 2309172-48-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of LDN-192960 hydrochloride:

LDN-192960 In-stock

2 Publications Citing Use of MCE LDN-192960 hydrochloride

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•Related Screening Libraries:

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View All DYRK Isoform Specific Products:

View All Isoforms

DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

Biological Activity
Purity & Documentation
References
Customer Review

Description

LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC₅₀s of 10 nM and 48 nM, respectively^[1].

IC₅₀ & Target

DYRK1

DYRK2

In Vitro

LDN-192960 hydrochloride (10 μM) is selective and inhibits ten of the other kinases by ≥90%, with only five being potently inhibited (IC₅₀<1 μM), including CLK1 (IC₅₀=0.21 μM), DYRK1A (IC₅₀= 0.10 μM), DYRK2 (IC₅₀=2 nM), DYRK3 (IC₅₀=19 nM) and PIM1 (IC₅₀=0.72 μM)^[1].
LDN-0192960 hydrochloride (0-5 μM; 2 hours) demonstrates that the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells overexpressing Haspin with an EC₅₀ of 1.17 μM^[2].
LDN-0192960 hydrochloride (0-1 μM; 1 hour incubation in the presence of nocodazole and MG132) demonstrates the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells synchronized in mitosis with an EC₅₀ of 0.02 μM^[2].

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

Molecular Weight

401.35

Formula

C₁₈H₂₂Cl₂N₂O₂S

CAS No.

2309172-48-1

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (249.16 mM; Need ultrasonic)

DMSO : 7.14 mg/mL (17.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4916 mL	12.4580 mL	24.9159 mL
5 mM	0.4983 mL	2.4916 mL	4.9832 mL
10 mM	0.2492 mL	1.2458 mL	2.4916 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.71 mg/mL (1.77 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.71 mg/mL (1.77 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 0.71 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (276 KB) SDS (394 KB)

COA (251 KB) RP-HPLC (245 KB) LCMS (256 KB)

Handling Instructions (2659 KB)

References

[1]. Cuny GD, et al. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3491-4. [Content Brief]

[2]. Gregory D Cuny, et al. Structure-activity Relationship Study of Acridine Analogs as Haspin and DYRK2 Kinase Inhibitors. Bioorg Med Chem Lett [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.4916 mL	12.4580 mL	24.9159 mL	62.2898 mL
	5 mM	0.4983 mL	2.4916 mL	4.9832 mL	12.4580 mL
	10 mM	0.2492 mL	1.2458 mL	2.4916 mL	6.2290 mL
	15 mM	0.1661 mL	0.8305 mL	1.6611 mL	4.1527 mL
H₂O	20 mM	0.1246 mL	0.6229 mL	1.2458 mL	3.1145 mL
	25 mM	0.0997 mL	0.4983 mL	0.9966 mL	2.4916 mL
	30 mM	0.0831 mL	0.4153 mL	0.8305 mL	2.0763 mL
	40 mM	0.0623 mL	0.3114 mL	0.6229 mL	1.5572 mL
	50 mM	0.0498 mL	0.2492 mL	0.4983 mL	1.2458 mL
	60 mM	0.0415 mL	0.2076 mL	0.4153 mL	1.0382 mL
	80 mM	0.0311 mL	0.1557 mL	0.3114 mL	0.7786 mL
	100 mM	0.0249 mL	0.1246 mL	0.2492 mL	0.6229 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.