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 32 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 MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXre|hyUUN3ME2wMlM1PzZ|IN88US=> MmjzV2FPT1KHUh?=
DU-145 NELXPJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zLRWlEPTB;Mz65N|gyOSEQvF2= M1ToTHNCVkeURWK=
GOTO M2ix[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTZwM{mxOlEh|ryP MUDTRW5IWkWU
NCI-H358 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\nS2NEUUN3ME23MlU{QCEQvF2= NFi5VmRUSU6JUlXS
IST-MES1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTdwOUW2N|ch|ryP M3;qXXNCVkeURWK=
T-24 NWXH[IZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLUTWM2OD16LkSwOlc{KM7:TR?= Mk\XV2FPT1KHUh?=
MPP-89 M3f3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWG4c5VQUUN3ME24MlQ3OjVzIN88US=> MUnTRW5IWkWU
NCI-SNU-1 NHrBXYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTlwME[3N|kh|ryP Mn;HV2FPT1KHUh?=
BFTC-905 Moq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3lVXRzUUN3ME2xNE4yOjN|IN88US=> M4\XS3NCVkeURWK=
MS-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFyLkiyN|Uh|ryP M331SXNCVkeURWK=
BEN M{XyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{CwdGlEPTB;MUOuNVI3PCEQvF2= M4L1WnNCVkeURWK=
HMV-II M4PDd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrVXnVKSzVyPUG0MlI{ODlizszN NYf6cIY3W0GQR2LFVi=>
NCI-H1581 NEXmUYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLvc4lKSzVyPUG3MlA1PDdizszN NUK5R4t5W0GQR2LFVi=>
ES8 NH[xbXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHYZWJ7UUN3ME2xO{4yPjdizszN MkDtV2FPT1KHUh?=
LC-2-ad MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF5LkSzOlYh|ryP MmjoV2FPT1KHUh?=
EW-13 Mni5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLyUJZKSzVyPUG3Mlk2OTZizszN NHfPbHZUSU6JUlXS
AN3-CA MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\nXWdtUUN3ME2xPE4yKM7:TR?= NGfXOnpUSU6JUlXS
SK-MEL-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrVTWM2OD1{MD6zOlg{KM7:TR?= MoPhV2FPT1KHUh?=
CAPAN-1 M1LYZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XxT2lEPTB;MkKuNVg5PCEQvF2= M2XiWXNCVkeURWK=
NCI-H2228 NIfK[ZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJ|Lk[2Olgh|ryP NITz[JlUSU6JUlXS
HOP-92 M{HVPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\ZV2lEPTB;MkSuN|g{QCEQvF2= NIDyS4dUSU6JUlXS
KYSE-270 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJ2LkW1O|Mh|ryP MULTRW5IWkWU
HCC1806 NXXLSXBJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoL3TWM2OD1{ND63O|k6KM7:TR?= Mn3SV2FPT1KHUh?=
HuO-3N1 M4XlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1W0XGlEPTB;MkWuPFE5PSEQvF2= MmHyV2FPT1KHUh?=
HOS M3L5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\QcmlEPTB;MkWuPVI6OiEQvF2= Ml\NV2FPT1KHUh?=
KYSE-510 M37xZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHznZ3lKSzVyPUK2MlE3OTJizszN M4rTNHNCVkeURWK=
COLO-741 NFLi[2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJ4LkOzNlkh|ryP Mo\XV2FPT1KHUh?=
HCC1937 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPFbGFGUUN3ME2yO{4zOjN6IN88US=> MVrTRW5IWkWU
NCI-H1703 NGLRdWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluzTWM2OD1{OD6wOFE{KM7:TR?= MmmzV2FPT1KHUh?=
U-2-OS Ml\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3ZdnlKSzVyPUK4MlU2OTVizszN M1ezXHNCVkeURWK=
DBTRG-05MG NH30fVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HCSGlEPTB;MkiuOVY2OSEQvF2= M3fubnNCVkeURWK=
MHH-ES-1 MoT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDofm1KSzVyPUOxMlk1OSEQvF2= NVyye4k4W0GQR2LFVi=>
HCC1419 NWnoSYdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLS[mt{UUN3ME2zNk4yOTF7IN88US=> MlrwV2FPT1KHUh?=
HOP-62 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTN{LkK3NFEh|ryP MofYV2FPT1KHUh?=
AM-38 MkHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfXTWM2OD1|Mj65PVMyKM7:TR?= M{DMenNCVkeURWK=
NCI-H2009 NEPPb41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLubGpnUUN3ME2zN{41ODB5IN88US=> MmHCV2FPT1KHUh?=
SW1116 Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoC2TWM2OD1|ND60PFM5KM7:TR?= NYPHPW1DW0GQR2LFVi=>
HTC-C3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXnO4FFUUN3ME2zOk4zOzV3IN88US=> M3rvd3NCVkeURWK=
SK-NEP-1 NH6ySXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmX6TWM2OD1|Nj62NVA3KM7:TR?= M3PKcXNCVkeURWK=
LB831-BLC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzlNphYUUN3ME2zO{43PTRzIN88US=> NF;Pdo5USU6JUlXS
CTB-1 MoT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\lZmFiUUN3ME2zPE41PTF{IN88US=> M4TU[XNCVkeURWK=
SW756 MluzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTRyLkmzPFUh|ryP MUfTRW5IWkWU
CAL-72 NWj6cZVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTR{LkCzJO69VQ>? M3;3UXNCVkeURWK=
KNS-62 NYraSG94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zndGlEPTB;NEKuOlI6PiEQvF2= Mnj6V2FPT1KHUh?=
KARPAS-299 Ml7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTR|LkOyN|Mh|ryP MnG4V2FPT1KHUh?=
KP-4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrJTWM2OD12Nj63N|YyKM7:TR?= NWC0T5cxW0GQR2LFVi=>
NEC8 NF3aZnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED4U|VKSzVyPUS3MlE3PjFizszN M4H6bHNCVkeURWK=
G-402 NG\rbphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{OzbGlEPTB;NEiuO|AyOiEQvF2= NXjTSYZtW0GQR2LFVi=>

... 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:


+ 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID