Losmapimod

Catalog No.S7215 Batch:S721502

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Technical Data

Formula

C22 H26 F N3 O2
Molecular Weight 383.46 CAS No. 585543-15-3
Solubility (25°C)* In vitro DMSO 76 mg/mL (198.19 mM)
Ethanol 76 mg/mL (198.19 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.
Targets
p38α [1]
(Cell-free assay)		 p38β [1]
(Cell-free assay)
8.1(pKi) 7.6(pKi)
In vitro

Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor.
In vivo

In spontaneously hypertensive stroke-prone rats (SHR-SP), Losmapimod significantly improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and subsequently attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1beta (IL-1beta). [1]

Protocol (from reference)

Kinase Assay:

[1]
  • In vitro assay

    Inhibition of p38α and p38β are determined by use of a ligand-displacement fluorescence polarization assay.
Cell Assay:

[2]
  • Cell lines

    MB135 iDUX4 myoblasts

  • Concentrations

    1 µM

  • Incubation Time

    2 h

  • Method

    Cells were treated with indicated concentration of drug for 2 h.
Animal Study:

[1]
  • Animal Models

    Spontaneously hypertensive stroke-prone rats

  • Dosages

    ~12 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Auton Autacoid Pharmacol, 2015, 35(3):32-40.]

Selleck's Losmapimod has been cited by 25 publications

Phosphorylation of human glioma-associated oncogene 1 on Ser937 regulates Sonic Hedgehog signaling in medulloblastoma [ Nat Commun, 2024, 15(1):987] PubMed: 38307877
Sustained activation of the FGF1-MEK-ERK pathway inhibits proliferation, invasion and migration and enhances radiosensitivity in mouse angiosarcoma cells [ J Radiat Res, 2024, rrae021] PubMed: 38637316
Preadipocytes in human granulation tissue: role in wound healing and response to macrophage polarization [ Inflamm Regen, 2023, 43(1):53] PubMed: 37904253
Preadipocytes in human granulation tissue: role in wound healing and response to macrophage polarization [ Inflamm Regen, 2023, 10.1186/s41232-023-00302-5] PubMed: 37904253
A human skeletal muscle stem/myotube model reveals multiple signaling targets of cancer secretome in skeletal muscle [ iScience, 2023, 26(4):106541] PubMed: 37102148
Apabetalone, a Clinical-Stage, Selective BET Inhibitor, Opposes DUX4 Target Gene Expression in Primary Human FSHD Muscle Cells [ Biomedicines, 2023, 11(10)2683] PubMed: 37893058
Apabetalone, a Clinical-Stage, Selective BET Inhibitor, Opposes DUX4 Target Gene Expression in Primary Human FSHD Muscle Cells [ Biomedicines, 2023, 11(10)2683] PubMed: 37893058
A Chemical Proteomics Approach to Discover Regulators of Innate Immune Signaling [ Viruses, 2023, 15(5)1112] PubMed: 37243198
AURKA and PLK1 inhibition selectively and synergistically block cell cycle progression in diffuse midline glioma [ iScience, 2022, 25(6):104398] PubMed: 35637734
Plasma membrane proteoglycans syndecan-2 and syndecan-4 engage with EGFR and RON kinase to sustain carcinoma cell cycle progression [ J Biol Chem, 2022, S0021-9258(22)00469-0] PubMed: 35569509

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.