585543-15-3
Chemical Structure
Losmapimod
Synonym(s): GSK-AHAB; GW856553X; SB856553
- CAS No.: 585543-15-3
- Formula:C22H26FN3O2
- Molecular Weight:383.46
IUPAC Name: 6-(5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl)-N-neopentylnicotinamide
InChIKey: KKYABQBFGDZVNQ-UHFFFAOYSA-N
SMILES: CC1=C(C2=NC=C(C(NCC(C)(C)C)=O)C=C2)C=C(C(NC3CC3)=O)C=C1F
Biological Activity: Losmapimod (GSK-AHAB; GW856553X) is an orally active p38α/β MAPK inhibitor, with pKi values of 8.1 and 7.6 for p38α and p38β, respectively. Losmapimod reduces DUX4 expression, thus exerting efficacy in facioscapulohumeral muscular dystrophy. By inhibiting MAPK/NF-κB, Losmapimod reduces apoptosis of epileptiform hippocampal neurons, and exhibits anti-allodynia and anti-hyperalgesic activities. Losmapimod blocks the entry and fusion of Lassa fever virus (LASV). Losmapimod overcomes tyrosine kinase inhibitor resistance in non-small cell lung cancer (NSCLC). Losmapimod inhibits myocardial senescence and inflammation, and possesses cardioprotective activity against cardiotoxicity[1][2][3][4][5][6].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Losmapimod | 99.94% | Losmapimod (GSK-AHAB; GW856553X) is an orally active p38α/β MAPK inhibitor, with pKi values of 8.1 and 7.6 for p38α and p38β, respectively. Losmapimod reduces DUX4 expression, thus exerting efficacy in facioscapulohumeral muscular dystrophy. By inhibiting MAPK/NF-κB, Losmapimod reduces apoptosis of epileptiform hippocampal neurons, and exhibits anti-allodynia and anti-hyperalgesic activities. Losmapimod blocks the entry and fusion of Lassa fever virus (LASV). Losmapimod overcomes tyrosine kinase inhibitor resistance in non-small cell lung cancer (NSCLC). Losmapimod inhibits myocardial senescence and inflammation, and possesses cardioprotective activity against cardiotoxicity. | ||||||||||||||||||||
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Losmapimod (Standard) | ≥98% | Losmapimod (GSK-AHAB; GW856553X) (Standard) is the analytical standard of Losmapimod (HY-10402). This product is intended for research and analytical applications. Losmapimod (GSK-AHAB; GW856553X) is an orally active p38α/β MAPK inhibitor, with pKi values of 8.1 and 7.6 for p38α and p38β, respectively. Losmapimod reduces DUX4 expression, thus exerting efficacy in facioscapulohumeral muscular dystrophy. By inhibiting MAPK/NF-κB, Losmapimod reduces apoptosis of epileptiform hippocampal neurons, and exhibits anti-allodynia and anti-hyperalgesic activities. Losmapimod blocks the entry and fusion of Lassa fever virus (LASV). Losmapimod overcomes tyrosine kinase inhibitor resistance in non-small cell lung cancer (NSCLC). Losmapimod inhibits myocardial senescence and inflammation, and possesses cardioprotective activity against cardiotoxicity. | ||||||||||||||||||||
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References
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[1]. Tawil R, et al. Safety and efficacy of losmapimod in facioscapulohumeral muscular dystrophy (ReDUX4): a randomised, double-blind, placebo-controlled phase 2b trial. Lancet Neurol. 2024 May;23(5):477-486.
[Content Brief] - [2]. Zhang X, et al. Identification of a clinical compound losmapimod that blocks Lassa virus entry. Antiviral research. 2019 Jul;167:68-77. [Content Brief]
- [3]. Dabour MS, et al. Losmapimod ameliorates doxorubicin-induced cardiotoxicity through attenuating senescence and inflammatory pathways. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2024 Oct;179:117288. [Content Brief]
- [4]. Yeung YT, et al. Losmapimod Overcomes Gefitinib Resistance in Non-small Cell Lung Cancer by Preventing Tetraploidization. EBioMedicine. 2018 Feb;28:51-61. [Content Brief]
- [5]. Li M, et al. Losmapimod Protected Epileptic Rats From Hippocampal Neuron Damage Through Inhibition of the MAPK Pathway. Frontiers in pharmacology. 2019;10:625. [Content Brief]
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[6]. Soued M, et al. Antinociceptive properties of losmapimod in two acute pain models in rats: behavioural analysis, immunohistochemistry, dose response, and comparison with usual analgesic drugs. BJA Open. 2022 Aug 17;3:100029.
[Content Brief]
