LDN-192960 free base | CAS#2309172-48-1 | DYRK2 inhibitor

MedKoo Cat#: 462468 | Name: LDN-192960 free base

Description:

WARNING: This product is for research use only, not for human or veterinary use.

LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2)

Chemical Structure

LDN-192960 free base

CAS#184582-62-5 (free base)

Theoretical Analysis

MedKoo Cat#: 462468

Name: LDN-192960 free base

CAS#: 184582-62-5 (free base)

Chemical Formula: C18H20N2O2S

Exact Mass: 328.1245

Molecular Weight: 328.43

Elemental Analysis: C, 65.83; H, 6.14; N, 8.53; O, 9.74; S, 9.76

Price and Availability

Size	Price	Availability
10mg	USD 250.00	2 Weeks
25mg	USD 450.00	2 Weeks
50mg	USD 750.00	2 Weeks
100mg	USD 1,250.00	2 Weeks

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Related CAS #

184582-62-5 (free base) 2309172-48-1 (HCl)

Synonym

LDN-192960; LDN192960 ; LDN 192960

IUPAC/Chemical Name

3-((2,7-dimethoxyacridin-9-yl)thio)propan-1-amine

InChi Key

ZFOMCSNUEHMROO-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H20N2O2S/c1-21-12-4-6-16-14(10-12)18(23-9-3-8-19)15-11-13(22-2)5-7-17(15)20-16/h4-7,10-11H,3,8-9,19H2,1-2H3

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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

In vitro activity:

This study has analyzed haspin functions by either its chemical inhibition with LDN-192960 in cultured spermatocytes, or the ablation of the Haspin gene in Haspin-/- mice. These studies suggest that haspin kinase activity is required for proper chromosome congression both during meiotic divisions and for the recruitment of Aurora B and kinesin MCAK (also known as KIF2C) to meiotic centromeres. Reference: J Cell Sci. 2022 Jul 1;135(13):jcs259546. https://pubmed.ncbi.nlm.nih.gov/35694956/

In vivo activity:

Upon palpable tumor formation, parental and DYRK2 KO-bearing mice were randomized each into 2 groups and treated with vehicle or LDN192960 50 mg/kg. There was a dramatic reduction of tumor volume in parental xenografts upon LDN192960 treatment (Fig. 5 G and H) and a clear reduction of 26S proteasome activity in the tumor lysate as well (Fig. 5I). Reference: Proc Natl Acad Sci U S A. 2019 Dec 3;116(49):24881-24891. https://pubmed.ncbi.nlm.nih.gov/31754034/

	Solvent	mg/mL	mM
Solubility
	Water	66.0	200.96

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 328.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Berenguer I, López-Jiménez P, Mena I, Viera A, Page J, González-Martínez J, Maestre C, Malumbres M, Suja JA, Gómez R. Haspin participates in AURKB recruitment to centromeres and contributes to chromosome congression in male mouse meiosis. J Cell Sci. 2022 Jul 1;135(13):jcs259546. doi: 10.1242/jcs.259546. Epub 2022 Jul 11. PMID: 35694956. 2. Banerjee S, Wei T, Wang J, Lee JJ, Gutierrez HL, Chapman O, Wiley SE, Mayfield JE, Tandon V, Juarez EF, Chavez L, Liang R, Sah RL, Costello C, Mesirov JP, de la Vega L, Cooper KL, Dixon JE, Xiao J, Lei X. Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression. Proc Natl Acad Sci U S A. 2019 Dec 3;116(49):24881-24891. doi: 10.1073/pnas.1912033116. Epub 2019 Nov 21. PMID: 31754034; PMCID: PMC6900511.

In vitro protocol:

In vivo protocol:

1. Banerjee S, Wei T, Wang J, Lee JJ, Gutierrez HL, Chapman O, Wiley SE, Mayfield JE, Tandon V, Juarez EF, Chavez L, Liang R, Sah RL, Costello C, Mesirov JP, de la Vega L, Cooper KL, Dixon JE, Xiao J, Lei X. Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression. Proc Natl Acad Sci U S A. 2019 Dec 3;116(49):24881-24891. doi: 10.1073/pnas.1912033116. Epub 2019 Nov 21. PMID: 31754034; PMCID: PMC6900511.

1: Cuny GD, Robin M, Ulyanova NP, et al. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010;20(12):3491-3494. 2: Kestav K, Uri A, Lavogina D. Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin. Curr Med Chem. 2017;24(21):2276-2293. doi:10.2174/0929867324666170414155520