LDN-209929 dihydrochloride

Name: LDN-209929 dihydrochloride
Brand: MedChemExpress
SKU: HY-110320
Rating: 4.5 (1 reviews)

Cat. No.: HY-110320 Purity: ≥99.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC₅₀=55 nM) with180-fold selectivity verses DYRK2 (IC₅₀=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 (HY-13455).

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

LDN-209929 dihydrochloride Chemical Structure

CAS No. : 1784281-97-5

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1550	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All DYRK Isoform Specific Products:

View All Isoforms

DYRK1 DYRK2 DYRK4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 55 nM (haspin kinase)
IC50: 9.9 μM (DYRK2)^[1]

In Vitro

Haspin: Haploid Germ Cell-Specific Nuclear Protein Kinase, is a serine/threonine kinase expressed in a variety of tissues (e.g., testis, bone marrow, thymus, and spleen). Haspin also plays an important role in mitosis, where it phosphorylates histone H3 at Thr-3 (H3T3) in G2/early prophase, becomes maximal during prometaphase/metaphase and then diminishes during anaphase^[1].
DYRKs belong to the CMGC family of ePKs and can be further divided into class 1 kinases DYRK1A and 1B, and class 2 kinases DYRK2, 3, and 4. The activity of DYRKs depends upon autophosphorylation of an essential activation loop tyrosine during synthesis^[1].

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

Molecular Weight

405.77

Formula

C₁₇H₁₉Cl₃N₂OS

CAS No.

1784281-97-5

Appearance

Solid

Color

Yellow to orange

SMILES

NCCCSC1=C(C=C(Cl)C=C2)C2=NC3=CC=C(OC)C=C31.[H]Cl.[H]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:

DMSO : 33.33 mg/mL (82.14 mM; ultrasonic and warming and heat to 60°C; 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	2.4645 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

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.

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

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: ≥ 2.5 mg/mL (6.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥99.0%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (251 KB) HNMR (105 KB) LCMS (241 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

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

[2]. Katrin Kestav, et al. Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin. Curr Med Chem. 2017;24(21):2276-2293. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4645 mL	12.3223 mL	24.6445 mL	61.6113 mL
	5 mM	0.4929 mL	2.4645 mL	4.9289 mL	12.3223 mL
	10 mM	0.2464 mL	1.2322 mL	2.4645 mL	6.1611 mL
	15 mM	0.1643 mL	0.8215 mL	1.6430 mL	4.1074 mL
	20 mM	0.1232 mL	0.6161 mL	1.2322 mL	3.0806 mL
	25 mM	0.0986 mL	0.4929 mL	0.9858 mL	2.4645 mL
	30 mM	0.0821 mL	0.4107 mL	0.8215 mL	2.0537 mL
	40 mM	0.0616 mL	0.3081 mL	0.6161 mL	1.5403 mL
	50 mM	0.0493 mL	0.2464 mL	0.4929 mL	1.2322 mL
	60 mM	0.0411 mL	0.2054 mL	0.4107 mL	1.0269 mL
	80 mM	0.0308 mL	0.1540 mL	0.3081 mL	0.7701 mL