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 44 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 NHy1dHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13XU2lEPTB;MD6zOFc3OyEQvF2= MkXWV2FPT1KHUh?=
DU-145 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2mySWlEPTB;Mz65N|gyOSEQvF2= MXvTRW5IWkWU
GOTO M{LYPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jYeWlEPTB;Nj6zPVE3OSEQvF2= M1nXe3NCVkeURWK=
NCI-H358 NUnPeIY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz0TWM2OD15LkWzPEDPxE1? M{XvXnNCVkeURWK=
IST-MES1 M{LSd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLF[IVKSzVyPUeuPVU3OzdizszN NYjZdnJ3W0GQR2LFVi=>
T-24 NHXDVoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7RTWM2OD16LkSwOlc{KM7:TR?= NGTqXIdUSU6JUlXS
MPP-89 M1S4OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn6UI5nUUN3ME24MlQ3OjVzIN88US=> M1PkTnNCVkeURWK=
NCI-SNU-1 NH6wZ|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTlwME[3N|kh|ryP M3\JNXNCVkeURWK=
BFTC-905 NFfNfVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLrW3ZKSzVyPUGwMlEzOzNizszN M2HGR3NCVkeURWK=
MS-1 MmXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz3[3VKSzVyPUGwMlgzOzVizszN MXHTRW5IWkWU
NBsusSR MnPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHxW5ZXUUN3ME2xNE45OjN3IN88US=> NXi0cGdkW0GQR2LFVi=>
BEN MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\uTWM2OD1zMz6xNlY1KM7:TR?= NEjnOIJUSU6JUlXS
NCI-H1581 M1THcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[y[5RKSzVyPUG3MlA1PDdizszN NY[5OFIzW0GQR2LFVi=>
ES8 NETxeJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7iTWM2OD1zNz6xOlch|ryP MXHTRW5IWkWU
LC-2-ad NFj0NllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LZZmlEPTB;MUeuOFM3PiEQvF2= M4nuOXNCVkeURWK=
EW-13 MmTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTF5Lkm1NVYh|ryP M4HrcXNCVkeURWK=
AN3-CA MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTF6LkGg{txO Mmi5V2FPT1KHUh?=
DB M3LOVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LVcmlEPTB;MUiuO|kzOyEQvF2= MoW3V2FPT1KHUh?=
SK-MEL-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXT3OZY5UUN3ME2yNE4{Pjh|IN88US=> MoDNV2FPT1KHUh?=
CAPAN-1 NV3uemltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrzRYpKSzVyPUKyMlE5QDRizszN NWPCd3FsW0GQR2LFVi=>
NCI-H2228 NEf5NXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDFToN[UUN3ME2yN{43PjZ6IN88US=> M{TUWnNCVkeURWK=
HOP-92 NFfMe5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXxV413UUN3ME2yOE4{QDN6IN88US=> NV[yTVlNW0GQR2LFVi=>
HCC1806 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFT4cJpKSzVyPUK0Mlc4QTlizszN MnrxV2FPT1KHUh?=
HuO-3N1 NU\sbmNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTJ3LkixPFUh|ryP MlTMV2FPT1KHUh?=
HOS NIfoc3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLzTWM2OD1{NT65NlkzKM7:TR?= M2rO[nNCVkeURWK=
KYSE-510 Mkm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJ4LkG2NVIh|ryP M2fESXNCVkeURWK=
COLO-741 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTJ4LkOzNlkh|ryP NGfVPZFUSU6JUlXS
H-EMC-SS NFH1SpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTJ4LkmyOFUh|ryP NVf4fXllW0GQR2LFVi=>
HCC1937 NFe3dGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M12xN2lEPTB;MkeuNlI{QCEQvF2= MmfoV2FPT1KHUh?=
NCI-H2126 M3f1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\obHhKSzVyPUK3MlM6PzVizszN M1vOcHNCVkeURWK=
NCI-H1703 M2Tz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJ6LkC0NVMh|ryP MVHTRW5IWkWU
MHH-ES-1 M335UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTNzLkm0NUDPxE1? Mof3V2FPT1KHUh?=
HOP-62 NHfqXJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\sSmlEPTB;M{KuNlcxOSEQvF2= NY\2fZVvW0GQR2LFVi=>
AM-38 MonLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz6V3VKUUN3ME2zNk46QTNzIN88US=> NITjdZZUSU6JUlXS
NCI-H2009 M2\HeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO5TWM2OD1|Mz60NFA4KM7:TR?= NUTYV5JHW0GQR2LFVi=>
EM-2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTN|LkW1NVEh|ryP NXW2SW9sW0GQR2LFVi=>
SW1116 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTN2LkS4N|gh|ryP NH64[oVUSU6JUlXS
SK-N-AS M{fyO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTN3LkC3NVQh|ryP NHH5VnpUSU6JUlXS
ChaGo-K-1 MkDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXmTWM2OD1|NT62NFMzKM7:TR?= NG[zUoxUSU6JUlXS
RT-112 NF3WOpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvvTWM2OD1|NT65PFc6KM7:TR?= M2PrVXNCVkeURWK=
HTC-C3 M2HZfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTN4LkKzOVUh|ryP NWrxWFFtW0GQR2LFVi=>
SK-NEP-1 M3e0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fDcGlEPTB;M{[uOlExPiEQvF2= MmDtV2FPT1KHUh?=
LB831-BLC MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTN5Lk[1OFEh|ryP NXSyXYpJW0GQR2LFVi=>
CTB-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnqRYhKSzVyPUO4MlQ2OTJizszN M{nDWnNCVkeURWK=
CAL-72 M4\5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLWU4hEUUN3ME20Nk4xOyEQvF2= MmDDV2FPT1KHUh?=
KARPAS-299 M2XHb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorsTWM2OD12Mz6zNlM{KM7:TR?= M4HtSnNCVkeURWK=
HEL MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXmNHg3UUN3ME20OU41PjR4IN88US=> NX;4WolNW0GQR2LFVi=>
KP-4 NYK1c3lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEG1e2hKSzVyPUS2Mlc{PjFizszN NVf6RoxqW0GQR2LFVi=>
G-402 MlPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TVVGlEPTB;NEiuO|AyOiEQvF2= M4W5T3NCVkeURWK=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-p38 / p38 ; 

PubMed: 23349819     

The inhibitory effect of phosphorylated p38 in KB, KBV200 (B) and in MCF-7, MCF-7/ADR (C) treated with BIRB796 at various concentrations after 24 h. 

mTOR / p-S6K / S6K / p-MK2 / MK2 / p-Hsp27 / Hsp27 ; 

PubMed: 26844273     

CRC cells were treated with 4 μM LY2228820, 10 μM BIRB796 or 10 μM SB202190 for 2 h and p38 and mTORC1 signaling was analyzed by immunoblot.

p-p38 / γ-H2AX ; 

PubMed: 27082306     

The expression of p-P38 was tested via protein gel blot after the cells were treated with BIRB796.

23349819 26844273 27082306
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:


- Collapse
  • 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID