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MedKoo Cat#: 531197 | Name: LDN-192960 HCl
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Description:

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

LDN-192960 is a potent and selective inhibitor of haspin.

Chemical Structure

LDN-192960 HCl
LDN-192960 HCl
CAS#2309172-48-1 (HCl)

Theoretical Analysis

MedKoo Cat#: 531197

Name: LDN-192960 HCl

CAS#: 2309172-48-1 (HCl)

Chemical Formula: C18H22Cl2N2O2S

Exact Mass: 0.0000

Molecular Weight: 401.35

Elemental Analysis: C, 53.87; H, 5.53; Cl, 17.67; N, 6.98; O, 7.97; S, 7.99

Price and Availability

Size Price Availability Quantity
5mg USD 285.00 2 Weeks
10mg USD 450.00 2 Weeks
25mg USD 850.00 2 Weeks
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Related CAS #
184582-62-5 (free base) 2309172-48-1 (HCl)
Synonym
LDN-192960 HCl; LDN-192960 hydrochloride; LDN 192960; LDN192960; LDN-192960;
IUPAC/Chemical Name
3-(2,7-Dimethoxy-acridin-9-ylsulfanyl)-propylamine dihydrochloride
InChi Key
FNHCUCJBABESJB-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H20N2O2S.2ClH/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;2*1H
SMILES Code
NCCCSC1=C(C=C(OC)C=C2)C2=NC3=CC=C(OC)C=C31.[H]Cl.[H]Cl
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
>2 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
Certificate of Analysis
View CoA: current batch, Lot#A20O10B08
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
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.
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
DMSO 20.1 50.01
PBS (pH 7.2) 10.0 24.92
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 401.35 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.

Recalculate based on batch purity %
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:
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 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

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