1246654-84-1
Chemical Structure
Losmapimod hydrochloride
Synonym(s): GSK-AHAB hydrochloride; GW856553X hydrochloride; SB856553 hydrochloride
- CAS No.: 1246654-84-1
- Formula:C22H27ClFN3O2
- Molecular Weight:419.92
IUPAC Name: 6-(5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl)-N-neopentylnicotinamide hydrochloride
InChIKey: ZSUHBVFLSGIBQS-UHFFFAOYSA-N
SMILES: O=C(C1=CN=C(C2=C(C)C(F)=CC(C(NC3CC3)=O)=C2)C=C1)NCC(C)(C)C.Cl
Biological Activity: Losmapimod (GSK-AHAB; GW856553X) hydrochloride is an orally active p38α/β MAPK inhibitor, with pKi values of 8.1 and 7.6 for p38α and p38β, respectively. Losmapimod hydrochloride reduces DUX4 expression, thus exerting efficacy in facioscapulohumeral muscular dystrophy. By inhibiting MAPK/NF-κB, Losmapimod hydrochloride reduces apoptosis of epileptiform hippocampal neurons, and exhibits anti-allodynia and anti-hyperalgesic activities. Losmapimod hydrochloride blocks the entry and fusion of Lassa fever virus (LASV). Losmapimod hydrochloride overcomes tyrosine kinase inhibitor resistance in non-small cell lung cancer (NSCLC). Losmapimod hydrochloride inhibits myocardial senescence and inflammation, and possesses cardioprotective activity against cardiotoxicity[1][2][3][4][5][6].
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Losmapimod hydrochloride | Losmapimod (GSK-AHAB; GW856553X) hydrochloride is an orally active p38α/β MAPK inhibitor, with pKi values of 8.1 and 7.6 for p38α and p38β, respectively. Losmapimod hydrochloride reduces DUX4 expression, thus exerting efficacy in facioscapulohumeral muscular dystrophy. By inhibiting MAPK/NF-κB, Losmapimod hydrochloride reduces apoptosis of epileptiform hippocampal neurons, and exhibits anti-allodynia and anti-hyperalgesic activities. Losmapimod hydrochloride blocks the entry and fusion of Lassa fever virus (LASV). Losmapimod hydrochloride overcomes tyrosine kinase inhibitor resistance in non-small cell lung cancer (NSCLC). Losmapimod hydrochloride 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]
