Choose Your Country or Region

Losmapimod (GW856553X)

Name: Losmapimod (GW856553X)
Brand: Selleck Chemicals
SKU: S7215
Rating: 5 (13 reviews)

Catalog No.S7215 Synonyms: GW856553, GSK-AHAB

For research use only.

Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pK_i of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.

Losmapimod (GW856553X) Chemical Structure

CAS No. 585543-15-3

Selleck's Losmapimod (GW856553X) has been cited by 13 publications

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

Related Compound Libraries

Other p38 MAPK Products

Pexmetinib (ARRY-614)^New

Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
SB239063^New

SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
Ravoxertinib (GDC-0994)^New

Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
Adezmapimod (SB203580)

Adezmapimod (SB203580, RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.
Doramapimod (BIRB 796)

Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with K_d of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.
SB202190 (FHPI)

SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Ralimetinib (LY2228820) dimesylate

Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.
PH-797804

PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.
VX-702

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.
TAK-715

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.

Download Inhibitor Catalog

p38 MAPK Signaling Pathway Map

Biological Activity

Description

Targets

p38α ^[1] (Cell-free assay)	p38β ^[1] (Cell-free assay)
8.1(pKi)	7.6(pKi)

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

PBMC	NYiwcHlrTnWwY4Tpc44h[XO\|YYm=		Mlz5NUBp		M4S3Z2lvcGmkaYTpc44hd2ZicEO4ZYxxcGFvZHXw[Y5l\W62IGTOSoFteGijIIDyc4R2[3Srb36gbY4hcHWvYX6gVGJOSyCycnXpcoN2[mG2ZXSg[o9zKDFiaIKgZoVnd3KnIFzQV{BkcGGubHXu[4Uh[nliRVzJV2EtKEmFNUC9NE4yKM7:TR?=	Mln2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5N{KyPFcoRjF7N{eyNlg4RC:jPh?=

Click to View More Cell Line Experimental Data

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)

Animal Research: ^[1]	Animal Models: Spontaneously hypertensive stroke-prone rats Dosages: ~12 mg/kg Administration: p.o.

References

[1] Willette RN, et al. J Pharmacol Exp Ther. 2009, 330(3), 964-970.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	383.46
Formula	C₂₂ H₂₆ F N₃ O₂
CAS No.	585543-15-3
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=C(C=C(C=C1F)C(=O)NC2CC2)C3=NC=C(C=C3)C(=O)NCC(C)(C)C

Download Losmapimod (GW856553X) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04264442	Enrolling by invitation	Drug: Losmapimod	Facioscapulohumeral Muscular Dystrophy (FSHD)	Fulcrum Therapeutics	February 13 2020	Phase 2
NCT04004000	Active not recruiting	Drug: Losmapimod	Facioscapulohumeral Muscular Dystrophy 1	Fulcrum Therapeutics	August 23 2019	Phase 2
NCT04003974	Completed	Drug: Losmapimod\|Drug: Placebo oral tablet	Facioscapulohumeral Muscular Dystrophy (FSHD)	Fulcrum Therapeutics	August 9 2019	Phase 2
NCT02000440	Completed	Drug: Losmapimod	Glomerulosclerosis Focal Segmental	GlaxoSmithKline	July 1 2014	Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):