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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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.

    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.

  • 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.

    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 M1XtNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvqVIVxUUN3ME2wMlM1PzZ|IN88US=> NFfk[WNUSU6JUlXS
DU-145 NEfucVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\mW4c2UUN3ME2zMlk{QDFzIN88US=> MoezV2FPT1KHUh?=
GOTO M3LqNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojWTWM2OD14LkO5NVYyKM7:TR?= M2q4VHNCVkeURWK=
NCI-H358 NGPMRZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7LTWM2OD15LkWzPEDPxE1? NULtPZVHW0GQR2LFVi=>
IST-MES1 NHXTUYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rWZWlEPTB;Nz65OVY{PyEQvF2= MVfTRW5IWkWU
KP-N-YN M4\GdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLTNmJpUUN3ME24MlIxOTlizszN M3HOenNCVkeURWK=
T-24 NHK5SYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRThwNEC2O|Mh|ryP M{DLVXNCVkeURWK=
MPP-89 NXrzdHM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XJS2lEPTB;OD60OlI2OSEQvF2= MXLTRW5IWkWU
NCI-SNU-1 NE[yeJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXIVJB6UUN3ME25MlA3PzN7IN88US=> MmP1V2FPT1KHUh?=
BFTC-905 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LB[GlEPTB;MUCuNVI{OyEQvF2= MoXrV2FPT1KHUh?=
MS-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Xhb2lEPTB;MUCuPFI{PSEQvF2= MoLwV2FPT1KHUh?=
NBsusSR MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHyTWM2OD1zMD64NlM2KM7:TR?= M1WxdnNCVkeURWK=
BEN M{fmUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPMSmU3UUN3ME2xN{4yOjZ2IN88US=> NGHOSldUSU6JUlXS
HMV-II MnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;UNoRKSzVyPUG0MlI{ODlizszN NF3xRXRUSU6JUlXS
NCI-H1581 NHn4S5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\iTWM2OD1zNz6wOFQ4KM7:TR?= MV7TRW5IWkWU
ES8 MnmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnNRnBKSzVyPUG3MlE3PyEQvF2= NYLkWHdLW0GQR2LFVi=>
LC-2-ad M16zXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnSRVhKSzVyPUG3MlQ{PjZizszN MUfTRW5IWkWU
EW-13 M4XmdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDSTWM2OD1zNz65OVE3KM7:TR?= NYfXfVh7W0GQR2LFVi=>
AN3-CA M2jMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF6LkGg{txO MorzV2FPT1KHUh?=
DB Ml3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3H0[GlEPTB;MUiuO|kzOyEQvF2= MVTTRW5IWkWU
SK-MEL-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfqTWM2OD1{MD6zOlg{KM7:TR?= NXzCVZV2W0GQR2LFVi=>
CAPAN-1 MmTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnvRoZbUUN3ME2yNk4yQDh2IN88US=> NFK4dZhUSU6JUlXS
NCI-H2228 M4XPUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{CyNmlEPTB;MkOuOlY3QCEQvF2= M4P1[XNCVkeURWK=
HOP-92 MnTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljTTWM2OD1{ND6zPFM5KM7:TR?= NETpTlFUSU6JUlXS
KYSE-270 MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1z1[WlEPTB;MkSuOVU4OyEQvF2= MonqV2FPT1KHUh?=
HCC1806 M1HNZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEniUWtKSzVyPUK0Mlc4QTlizszN M4H5bXNCVkeURWK=
HuO-3N1 MlLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLINnVxUUN3ME2yOU45OTh3IN88US=> NXz5PXBIW0GQR2LFVi=>
HOS MkmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJ3LkmyPVIh|ryP MlLCV2FPT1KHUh?=
KYSE-510 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7iTWM2OD1{Nj6xOlEzKM7:TR?= NWTNVZVHW0GQR2LFVi=>
COLO-741 NYD5cmN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDyTGNEUUN3ME2yOk4{OzJ7IN88US=> NFHIbVNUSU6JUlXS
H-EMC-SS MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjtdFlpUUN3ME2yOk46OjR3IN88US=> NFTMRZZUSU6JUlXS
HCC1937 NH;qRotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ5LkKyN|gh|ryP NYHSfHFsW0GQR2LFVi=>
NCI-H2126 NUj4OpgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonaTWM2OD1{Nz6zPVc2KM7:TR?= M4\Rb3NCVkeURWK=
NCI-H1703 NEnRSVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJ6LkC0NVMh|ryP NGrrTG5USU6JUlXS
U-2-OS NFfxfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;BTWM2OD1{OD61OVE2KM7:TR?= Mmj5V2FPT1KHUh?=
DBTRG-05MG NITNcJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTXboFKSzVyPUK4MlU3PTFizszN MnTrV2FPT1KHUh?=
MHH-ES-1 NXn5VmY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvsTWM2OD1|MT65OFEh|ryP NWDvXIgyW0GQR2LFVi=>
HCC1419 MkPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGxTWM2OD1|Mj6xNVE6KM7:TR?= MnHHV2FPT1KHUh?=
HOP-62 NUPF[HZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN{LkK3NFEh|ryP M33zRXNCVkeURWK=
AM-38 NEHmXI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm[wTWM2OD1|Mj65PVMyKM7:TR?= NF;kWYVUSU6JUlXS
NCI-H2009 M2niOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjre41KSzVyPUOzMlQxODdizszN NXuyWFFsW0GQR2LFVi=>
EM-2 NVLtcWlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTN|LkW1NVEh|ryP MUXTRW5IWkWU
SW1116 M4OzOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIey[lVKSzVyPUO0MlQ5OzhizszN M1rBeHNCVkeURWK=
SK-N-AS NIjze29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTN3LkC3NVQh|ryP M2DCOHNCVkeURWK=
ChaGo-K-1 M2X5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX22O5FWUUN3ME2zOU43ODN{IN88US=> Mn7IV2FPT1KHUh?=
RT-112 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PMWGlEPTB;M{WuPVg4QSEQvF2= NYW4UJhuW0GQR2LFVi=>
HTC-C3 NUjuOZZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e2WmlEPTB;M{[uNlM2PSEQvF2= NHznWXZUSU6JUlXS
SK-NEP-1 NULG[3ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHYeHFKSzVyPUO2MlYyODZizszN NYjMcZdZW0GQR2LFVi=>
LB831-BLC NUTkUmZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\FbXplUUN3ME2zO{43PTRzIN88US=> NIX0bHpUSU6JUlXS
CTB-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEmxOoFKSzVyPUO4MlQ2OTJizszN NEP1dFFUSU6JUlXS
MOLT-4 NX\X[2FCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TubmlEPTB;M{iuPFM6OSEQvF2= NG\WUYZUSU6JUlXS
SW756 NFrkbmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTRyLkmzPFUh|ryP MonYV2FPT1KHUh?=
CAL-72 NEfjTnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDEVJNKSzVyPUSyMlA{KM7:TR?= M3zBWnNCVkeURWK=
KNS-62 NEnMOo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrZWoJKSzVyPUSyMlYzQTZizszN M{\rUXNCVkeURWK=
KARPAS-299 M134e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPrR|lKSzVyPUSzMlMzOzNizszN NF3qOWZUSU6JUlXS
HEL Ml3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTR3LkS2OFYh|ryP MoLNV2FPT1KHUh?=
KP-4 MonoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\GZWlEPTB;NE[uO|M3OSEQvF2= MYfTRW5IWkWU
NEC8 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTETWM2OD12Nz6xOlYyKM7:TR?= M1LXdnNCVkeURWK=
G-402 Ml:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHSUmRKSzVyPUS4MlcxOTJizszN M{fZ[nNCVkeURWK=

... 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
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
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2
NCT02209805 Completed Healthy Boehringer Ingelheim January 2001 Phase 1

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID