Doramapimod (BIRB 796)

Catalog No.S1574

Doramapimod (BIRB 796) Chemical Structure

Molecular Weight(MW): 527.66

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 Kd 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.

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Cited by 23 Publications

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Biological Activity

Description 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 Kd 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.
Features The first p38 MAPK inhibitor to be tested in a phase III clinical trial.
p38α [1]
(Cell-free assay)
p38α [7]
0.1 nM(Kd) 38 nM
In vitro

BIRB 796 shows no significant inhibition to ERK-1, SYK, IKK2β, ZAP-70, EGF receptor kinase, HER2, protein kinase A (PKA), PKC, PKC-α, PKC-β (I and II) and PKC-γ. BIRB 796 greatly improves binding affinity by forming a hydrogen bond between the morpholine oxygen and the ATP-binding domain of p38α. BIRB 796 represents one of the most potent and slowest dissociating inhibitors against human p38 MAP kinase now known. [1] BIRB 796 potently inhibits c-Raf-1 and Jnk2α2 with IC50 of 1.4 and 0.1 nM, respectively. [2] BIRB796 also inhibits the activity and the activation of SAPK3/p38γ at a higher concentration than it does in p38α. BIRB796 blocks the stress-induced phosphorylation of the scaffold protein SAP97, which is a physiological substrate of SAPK3/p38γ. BIRB796 blocks JNK1/2 activation and activity in HEK293 cells, while not inhibits the activation and activity of ERK1/ERK2 in Hela cells. Moreover, the binding of BIRB796 to the p38 MAPKs or JNK1/2 is impairing their phosphorylation by the upstream kinase MKK6 or MKK4 rather than enhancing their dephosphorylation. [3] BIRB 796 blocks baseline and bortezomib-triggered upregulation of p38 MAPK and Hsp27 phosphorylation, thereby enhancing cytotoxicity and caspase activation. BIRB 796 downregulates IL-6 and VEGF secretion in BMSCs triggered by TNF-α and TGF-β1. [4] BIRB-796 has a pyrazole scaffold that places a lipophilic t-butyl group into the lower selectivity site and a tolyl ring into the upper selectivity site. BIRB-796 also inhibits B-Raf and Abl with IC50 of 83 nM and 14.6 μM, respectively. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell NXXCN|NbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHjTWM2OD1yLkO0O|Y{KM7:TR?= NXLMW|V1W0GQR2LFVi=>
DU-145 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTNwOUO4NVEh|ryP NFfuSIlUSU6JUlXS
IST-MES1 M1L1e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPNTWM2OD15Lkm1OlM4KM7:TR?= MkHUV2FPT1KHUh?=
KP-N-YN M3;JVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfrVlFKSzVyPUiuNlAyQSEQvF2= NXznOY1RW0GQR2LFVi=>
T-24 M3XSSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjrPFFKSzVyPUiuOFA3PzNizszN NVXs[lVXW0GQR2LFVi=>
MPP-89 M{PCT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLDTWM2OD16LkS2NlUyKM7:TR?= NWTRNnNlW0GQR2LFVi=>
NCI-SNU-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTlwME[3N|kh|ryP M{LDRXNCVkeURWK=
BFTC-905 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr4RmxKSzVyPUGwMlEzOzNizszN MWnTRW5IWkWU
MS-1 MnGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFyLkiyN|Uh|ryP NF\Se|ZUSU6JUlXS
NBsusSR NGXxTYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvuXlRKSzVyPUGwMlgzOzVizszN NFXBbXNUSU6JUlXS
BEN MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF|LkGyOlQh|ryP MVrTRW5IWkWU
NCI-H1581 NVf5fpJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3jdHdFUUN3ME2xO{4xPDR5IN88US=> Ml63V2FPT1KHUh?=
ES8 MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPnTGRKSzVyPUG3MlE3PyEQvF2= NVq1Uos2W0GQR2LFVi=>
LC-2-ad NVnnUGtpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;TcGlEPTB;MUeuOFM3PiEQvF2= M{[xRXNCVkeURWK=
EW-13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPyflJzUUN3ME2xO{46PTF4IN88US=> NV\XUpZ[W0GQR2LFVi=>
AN3-CA M3vBbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIOxd3lKSzVyPUG4MlEh|ryP NXyyTGdxW0GQR2LFVi=>
DB MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjYWlcxUUN3ME2xPE44QTJ|IN88US=> MVfTRW5IWkWU
CAPAN-1 M{PiU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTJ{LkG4PFQh|ryP NWHOfYRUW0GQR2LFVi=>
NCI-H2228 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJ|Lk[2Olgh|ryP MYrTRW5IWkWU
HOP-92 M1P4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofhTWM2OD1{ND6zPFM5KM7:TR?= NV;RWYZuW0GQR2LFVi=>
KYSE-270 MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJ2LkW1O|Mh|ryP NYnQO3hvW0GQR2LFVi=>
HCC1806 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljKTWM2OD1{ND63O|k6KM7:TR?= MVjTRW5IWkWU
HuO-3N1 MnjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJ3LkixPFUh|ryP NYLRfVhwW0GQR2LFVi=>
HOS M{XIemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ3LkmyPVIh|ryP MWPTRW5IWkWU
KYSE-510 M2noXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnIfZdlUUN3ME2yOk4yPjF{IN88US=> NV;hR29zW0GQR2LFVi=>
H-EMC-SS NWr6NW52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\0emlEPTB;Mk[uPVI1PSEQvF2= NY\kSZRbW0GQR2LFVi=>
HCC1937 MliyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPSTWM2OD1{Nz6yNlM5KM7:TR?= NUDCfXFoW0GQR2LFVi=>
NCI-H2126 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;vWYl[UUN3ME2yO{4{QTd3IN88US=> NH7hW4JUSU6JUlXS
NCI-H1703 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPDTWM2OD1{OD6wOFE{KM7:TR?= NG\VWppUSU6JUlXS
U-2-OS M1nBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfKT4RKSzVyPUK4MlU2OTVizszN NX64RlNkW0GQR2LFVi=>
DBTRG-05MG M1;HW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVv3SHNbUUN3ME2yPE42PjVzIN88US=> NXe4dWl3W0GQR2LFVi=>
MHH-ES-1 M1zKPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnTUmc4UUN3ME2zNU46PDFizszN MUnTRW5IWkWU
HCC1419 NYLlO21sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7KdVkyUUN3ME2zNk4yOTF7IN88US=> NGjjVZVUSU6JUlXS
HOP-62 Mlv1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX3TWM2OD1|Mj6yO|AyKM7:TR?= NULvZXZlW0GQR2LFVi=>
AM-38 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTN{Lkm5N|Eh|ryP MWrTRW5IWkWU
NCI-H2009 NHfp[YhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTN|LkSwNFch|ryP MVTTRW5IWkWU
EM-2 NIPwXllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTSTWM2OD1|Mz61OVEyKM7:TR?= NVjNbnh5W0GQR2LFVi=>
SK-N-AS NFrEU5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TNO2lEPTB;M{WuNFcyPCEQvF2= NWi1PWt1W0GQR2LFVi=>
ChaGo-K-1 NEXaVVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37FWmlEPTB;M{WuOlA{OiEQvF2= NWq3V2J4W0GQR2LFVi=>
RT-112 MmXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfzWItlUUN3ME2zOU46QDd7IN88US=> M1O2enNCVkeURWK=
SK-NEP-1 M1vnNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33Rc2lEPTB;M{[uOlExPiEQvF2= MW\TRW5IWkWU
LB831-BLC Ml7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvZSmZKSzVyPUO3MlY2PDFizszN M2m1OnNCVkeURWK=
CTB-1 NF7iTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;1U4ROUUN3ME2zPE41PTF{IN88US=> M2HWOnNCVkeURWK=
MOLT-4 M4q2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTN6LkizPVEh|ryP NWXNdIdiW0GQR2LFVi=>
SW756 M3z3cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTRyLkmzPFUh|ryP NFf2OFVUSU6JUlXS
KNS-62 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnq5TWM2OD12Mj62Nlk3KM7:TR?= NUn6Z2t[W0GQR2LFVi=>
KARPAS-299 MnSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXi0c5I3UUN3ME20N{4{OjN|IN88US=> NG\0eZRUSU6JUlXS
HEL M2XqVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPmOHBKSzVyPUS1MlQ3PDZizszN NXiyWGVVW0GQR2LFVi=>
KP-4 Mn7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrOWmhyUUN3ME20Ok44OzZzIN88US=> M4\Od3NCVkeURWK=
G-402 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTIV5VKSzVyPUS4MlcxOTJizszN M{j6XnNCVkeURWK=

... Click to View More Cell Line Experimental Data

In vivo BIRB 796 (30 mg/kg) inhibits 84% of TNF-α in LPS-stimulated mice and demonstrates efficacy in a mouse model of established collagen-induced arthritis. [1] BIRB 796 has good pharmacokinetic performance even after oral administration in mice. [2]


Animal Research:


+ Expand
  • Animal Models: Collagen-induced arthritis in female Balb/c mice
  • Formulation: 70% PEG400 (intravenous) or 100% PEG400 (oral)
  • Dosages: 1 mg/kg (intravenous) or 10 mg/kg (oral)
  • Administration: Intravenous injection or by oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (189.51 mM)
Ethanol 100 mg/mL (189.51 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 527.66


CAS No. 285983-48-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02214888 Terminated Arthritis Rheumatoid Boehringer Ingelheim May 2003 Phase 2
NCT02214888 Terminated Arthritis Rheumatoid Boehringer Ingelheim May 2003 Phase 2
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2

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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID