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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In DMSO USD 294 In stock
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Cited by 18 Publications

5 Customer Reviews

  • Lympho-myeloid potential assessed by FACS analysis of human CD19 (B-lymphoid cells) and CD33/CD15 (myeloid cells) in bone marrow of NSG recipient mice, 17 weeks after transplantation. Each plot represents an animal from the experiment presented in panel.

    Blood 2012 119(26), 6255-8. Doramapimod (BIRB 796) purchased from Selleck.

    Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.

    Int J Cancer 2014 134(3), 575-86. Doramapimod (BIRB 796) purchased from Selleck.

  • A p38α/ERK crosstalk exists in CRC cells and tissues. Use of a structurally and functionally different p38α inhibitor (BIRB-796) confirms ERK1/2 phospho-activation. Using BIRB-796 for up to 72 h triggers MEK-ERK1/2 signaling in HT-29 cells.

    Cancer Lett 2012 324(1), 98-108. Doramapimod (BIRB 796) purchased from Selleck.

    Inhibition of p38 MAPK activity prevents induction of autophagy by glucose. NIH 3T3 cells were incubated in KH medium without glucose in the presence of the p38 MAPK inhibitor BIRB796 (50 nM, middle panels). After 30 min, glucose (10 mM) and lysosomal inhibitors were added to the indicated samples and cells were further incubated for 2 h. Cell lysates were collected and processed for SDS/PAGE. LC3 levels were detected and actin served as a loading control. The values shown in the histograms represent means盨.D. from three independent experiments with the LC3-II levels normalized to actin and expressed as a percentage of the values of KH medium without glucose. *P<0.05. Glc, glucose; w/o, without.

    Biochem J 2014 449(2), 497-506. Doramapimod (BIRB 796) purchased from Selleck.

  • Doramapimod (BIRB 796) purchased from Selleck.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

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.
Targets
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 NY\sN2hzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwM{S3OlMh|ryP MonGV2FPT1KHUh?=
DU-145 M3\Femdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTNwOUO4NVEh|ryP Mn[1V2FPT1KHUh?=
GOTO NVTKO4NDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjlNnpNUUN3ME22MlM6OTZzIN88US=> M1u2[XNCVkeURWK=
NCI-H358 NITHW|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDpPHhKSzVyPUeuOVM5KM7:TR?= M{G4ZXNCVkeURWK=
IST-MES1 NVntSnRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3aU2pKSzVyPUeuPVU3OzdizszN NVfQOlV5W0GQR2LFVi=>
KP-N-YN NVm0NXVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPZO29bUUN3ME24MlIxOTlizszN NYK2Vol7W0GQR2LFVi=>
T-24 NEe4Z4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rrfGlEPTB;OD60NFY4OyEQvF2= MorNV2FPT1KHUh?=
MPP-89 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRThwNE[yOVEh|ryP Ml3FV2FPT1KHUh?=
NCI-SNU-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPWc3JPUUN3ME25MlA3PzN7IN88US=> NFXuT25USU6JUlXS
BFTC-905 NHvOS5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\ETWM2OD1zMD6xNlM{KM7:TR?= MXLTRW5IWkWU
MS-1 NFX5TmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTFyLkiyN|Uh|ryP MYjTRW5IWkWU
NBsusSR NHvNXlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTvTWM2OD1zMD64NlM2KM7:TR?= NYPV[IEyW0GQR2LFVi=>
BEN M{nBT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XXSmlEPTB;MUOuNVI3PCEQvF2= MnLnV2FPT1KHUh?=
HMV-II MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXCN5ZzUUN3ME2xOE4zOzB7IN88US=> Mm\OV2FPT1KHUh?=
NCI-H1581 MmrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jz[mlEPTB;MUeuNFQ1PyEQvF2= NXnjRm52W0GQR2LFVi=>
ES8 M1XXOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ztfGlEPTB;MUeuNVY4KM7:TR?= NWniclljW0GQR2LFVi=>
LC-2-ad NFPIUlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTF5LkSzOlYh|ryP M3PvfXNCVkeURWK=
EW-13 M3;OSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T0SWlEPTB;MUeuPVUyPiEQvF2= MX\TRW5IWkWU
AN3-CA NXXMeWRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXxNIVKSzVyPUG4MlEh|ryP NG\PZY9USU6JUlXS
DB NGH2d4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVf0Ung2UUN3ME2xPE44QTJ|IN88US=> MnraV2FPT1KHUh?=
SK-MEL-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHETWM2OD1{MD6zOlg{KM7:TR?= NWD0Z5VEW0GQR2LFVi=>
CAPAN-1 NEn3PI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTJ{LkG4PFQh|ryP MXjTRW5IWkWU
NCI-H2228 NFqwWoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:xWm9HUUN3ME2yN{43PjZ6IN88US=> M1HOeHNCVkeURWK=
HOP-92 NW[3RoxUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJ2LkO4N|gh|ryP MU\TRW5IWkWU
KYSE-270 NV\JNHl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfRclQ6UUN3ME2yOE42PTd|IN88US=> NWXQZ5BnW0GQR2LFVi=>
HCC1806 MmnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzKOY1KSzVyPUK0Mlc4QTlizszN M2XzR3NCVkeURWK=
HuO-3N1 NEDZT5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\neINFUUN3ME2yOU45OTh3IN88US=> MXTTRW5IWkWU
HOS MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\QTWM2OD1{NT65NlkzKM7:TR?= NHXvNHFUSU6JUlXS
KYSE-510 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTLTWM2OD1{Nj6xOlEzKM7:TR?= M4DiR3NCVkeURWK=
COLO-741 Mk\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTvTWM2OD1{Nj6zN|I6KM7:TR?= NV3UNpp2W0GQR2LFVi=>
H-EMC-SS M1H1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzWRWpxUUN3ME2yOk46OjR3IN88US=> M3THOnNCVkeURWK=
HCC1937 M1zaXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILIOmZKSzVyPUK3MlIzOzhizszN NGfYPYZUSU6JUlXS
NCI-H2126 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rBVWlEPTB;MkeuN|k4PSEQvF2= NVuzZ2E4W0GQR2LFVi=>
NCI-H1703 Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rtbWlEPTB;MkiuNFQyOyEQvF2= MnfzV2FPT1KHUh?=
U-2-OS MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrabnNRUUN3ME2yPE42PTF3IN88US=> MXLTRW5IWkWU
DBTRG-05MG M2D3Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXwTo5jUUN3ME2yPE42PjVzIN88US=> MVHTRW5IWkWU
MHH-ES-1 MkG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfSVVRkUUN3ME2zNU46PDFizszN NXPoPYZNW0GQR2LFVi=>
HCC1419 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HnTWlEPTB;M{KuNVEyQSEQvF2= MkPPV2FPT1KHUh?=
HOP-62 M1TYWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTN{LkK3NFEh|ryP NHTyS3NUSU6JUlXS
AM-38 Mny0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Lad2lEPTB;M{KuPVk{OSEQvF2= MVLTRW5IWkWU
NCI-H2009 MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPWPFhEUUN3ME2zN{41ODB5IN88US=> MV7TRW5IWkWU
EM-2 Mn7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrBb2RKSzVyPUOzMlU2OTFizszN MkjOV2FPT1KHUh?=
SW1116 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPNfW5KSzVyPUO0MlQ5OzhizszN MYnTRW5IWkWU
SK-N-AS M1nwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrhd5ZKSzVyPUO1MlA4OTRizszN NHLmeI1USU6JUlXS
ChaGo-K-1 NHLMd3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PuTmlEPTB;M{WuOlA{OiEQvF2= Mn74V2FPT1KHUh?=
RT-112 M1PBPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnETWM2OD1|NT65PFc6KM7:TR?= MkjJV2FPT1KHUh?=
HTC-C3 NEm3bFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HxUWlEPTB;M{[uNlM2PSEQvF2= MnTtV2FPT1KHUh?=
SK-NEP-1 NGHySVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;qNVFYUUN3ME2zOk43OTB4IN88US=> MlfrV2FPT1KHUh?=
LB831-BLC M3fVTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X5bmlEPTB;M{euOlU1OSEQvF2= MULTRW5IWkWU
CTB-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPJTWM2OD1|OD60OVEzKM7:TR?= MknuV2FPT1KHUh?=
MOLT-4 NYDNTZF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDOTWM2OD1|OD64N|kyKM7:TR?= NFfySlRUSU6JUlXS
SW756 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LSXWlEPTB;NECuPVM5PSEQvF2= M{eySHNCVkeURWK=
CAL-72 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInSTGlKSzVyPUSyMlA{KM7:TR?= M4eyRnNCVkeURWK=
KNS-62 M2TONWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH3fHpKSzVyPUSyMlYzQTZizszN NIPXb3JUSU6JUlXS
KARPAS-299 Mn;IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlmxTWM2OD12Mz6zNlM{KM7:TR?= M{HYVXNCVkeURWK=
HEL MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmCzTWM2OD12NT60OlQ3KM7:TR?= M1nlPXNCVkeURWK=
KP-4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH5VHVZUUN3ME20Ok44OzZzIN88US=> M2ToeHNCVkeURWK=
NEC8 MmPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LtVWlEPTB;NEeuNVY3OSEQvF2= NX23OoJPW0GQR2LFVi=>
G-402 NXXWc5E{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PjSGlEPTB;NEiuO|AyOiEQvF2= M3P4OHNCVkeURWK=

... 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]

Protocol

Animal Research:

[2]

+ 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
Formula

C31H37N5O3

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

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

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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID