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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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 NXKzcIE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwM{S3OlMh|ryP MULTRW5IWkWU
DU-145 M1ro[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGr5UI5KSzVyPUOuPVM5OTFizszN MXzTRW5IWkWU
GOTO MoTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTZwM{mxOlEh|ryP NYrHS2l5W0GQR2LFVi=>
NCI-H358 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HFS2lEPTB;Nz61N|gh|ryP NVvM[WM1W0GQR2LFVi=>
IST-MES1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLNS2NKSzVyPUeuPVU3OzdizszN MnnhV2FPT1KHUh?=
KP-N-YN MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LhOGlEPTB;OD6yNFE6KM7:TR?= MlO1V2FPT1KHUh?=
T-24 NGO5fohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi1OHpiUUN3ME24MlQxPjd|IN88US=> MX3TRW5IWkWU
MPP-89 NXW2ToVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRThwNE[yOVEh|ryP M3zGcHNCVkeURWK=
NCI-SNU-1 NXfnSXNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHGTWM2OD17LkC2O|M6KM7:TR?= NVPIXFJXW0GQR2LFVi=>
BFTC-905 Mn72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;qWmlEPTB;MUCuNVI{OyEQvF2= NHPx[IhUSU6JUlXS
MS-1 M{j5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFG0O|FKSzVyPUGwMlgzOzVizszN MWPTRW5IWkWU
NBsusSR M2O4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LhbGlEPTB;MUCuPFI{PSEQvF2= MnvWV2FPT1KHUh?=
BEN MnjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfycVNKSzVyPUGzMlEzPjRizszN MmjxV2FPT1KHUh?=
HMV-II M{PNVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXYTWM2OD1zND6yN|A6KM7:TR?= MVnTRW5IWkWU
NCI-H1581 NGHMRYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTF5LkC0OFch|ryP MkLaV2FPT1KHUh?=
ES8 M3ezPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnvZ5hjUUN3ME2xO{4yPjdizszN NXX4OIViW0GQR2LFVi=>
LC-2-ad MmH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHe2[VhKSzVyPUG3MlQ{PjZizszN NFTteYZUSU6JUlXS
EW-13 MmfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\YTWM2OD1zNz65OVE3KM7:TR?= Mm\VV2FPT1KHUh?=
AN3-CA Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nzNWlEPTB;MUiuNUDPxE1? M1vPZXNCVkeURWK=
DB MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHERpJHUUN3ME2xPE44QTJ|IN88US=> NV7j[I5OW0GQR2LFVi=>
SK-MEL-1 NHnPcI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJyLkO2PFMh|ryP MkjnV2FPT1KHUh?=
CAPAN-1 M2rvXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\tWJRJUUN3ME2yNk4yQDh2IN88US=> NXvxWpFKW0GQR2LFVi=>
NCI-H2228 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS0dVNIUUN3ME2yN{43PjZ6IN88US=> M4q0U3NCVkeURWK=
HOP-92 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7nU3BiUUN3ME2yOE4{QDN6IN88US=> Mn;TV2FPT1KHUh?=
KYSE-270 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPiNINCUUN3ME2yOE42PTd|IN88US=> NXfaOnFvW0GQR2LFVi=>
HCC1806 NGHmfJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTJ2Lke3PVkh|ryP NInsN45USU6JUlXS
HuO-3N1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7iOZRKSzVyPUK1MlgyQDVizszN NIS0SpNUSU6JUlXS
HOS NV7yTINXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHETWM2OD1{NT65NlkzKM7:TR?= MmXPV2FPT1KHUh?=
KYSE-510 NIjvSYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljxTWM2OD1{Nj6xOlEzKM7:TR?= MknDV2FPT1KHUh?=
COLO-741 NI\0fmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHz[WdWUUN3ME2yOk4{OzJ7IN88US=> MWDTRW5IWkWU
H-EMC-SS NIXWRm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWH3NotEUUN3ME2yOk46OjR3IN88US=> M{HzS3NCVkeURWK=
HCC1937 NHr1cWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPBTWM2OD1{Nz6yNlM5KM7:TR?= MmrmV2FPT1KHUh?=
NCI-H2126 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DlTmlEPTB;MkeuN|k4PSEQvF2= M3XUfHNCVkeURWK=
NCI-H1703 NV\nOXNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJ6LkC0NVMh|ryP M3G3Z3NCVkeURWK=
U-2-OS NGO3PWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnQTWM2OD1{OD61OVE2KM7:TR?= MVjTRW5IWkWU
DBTRG-05MG NV7GVmtpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTJ6LkW2OVEh|ryP NUfEUZFOW0GQR2LFVi=>
MHH-ES-1 NFPPXWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3GwbWlEPTB;M{GuPVQyKM7:TR?= M3Tp[nNCVkeURWK=
HCC1419 NVnMWVQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXmWJlKUUN3ME2zNk4yOTF7IN88US=> NF7HcohUSU6JUlXS
HOP-62 MkfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmntTWM2OD1|Mj6yO|AyKM7:TR?= M{PqRnNCVkeURWK=
AM-38 M2nBZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTN{Lkm5N|Eh|ryP MnLxV2FPT1KHUh?=
NCI-H2009 M3v1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrsTWM2OD1|Mz60NFA4KM7:TR?= NVT2OVlpW0GQR2LFVi=>
EM-2 NYXqW4NCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4K3NmlEPTB;M{OuOVUyOSEQvF2= MXjTRW5IWkWU
SW1116 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnuWHFpUUN3ME2zOE41QDN6IN88US=> M1\yRnNCVkeURWK=
SK-N-AS MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTN3LkC3NVQh|ryP MoHTV2FPT1KHUh?=
ChaGo-K-1 NECwPWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfuWmF7UUN3ME2zOU43ODN{IN88US=> M3G0fnNCVkeURWK=
RT-112 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLhV2tKSzVyPUO1Mlk5PzlizszN MorhV2FPT1KHUh?=
HTC-C3 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPuSZRKSzVyPUO2MlI{PTVizszN MWPTRW5IWkWU
SK-NEP-1 NESwNVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2T3VWlEPTB;M{[uOlExPiEQvF2= M3rhVHNCVkeURWK=
LB831-BLC NUj1VmFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LGdmlEPTB;M{euOlU1OSEQvF2= NVL4fGM1W0GQR2LFVi=>
CTB-1 NFHRO5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPCTWM2OD1|OD60OVEzKM7:TR?= NFz3VI1USU6JUlXS
MOLT-4 M2\nT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\jcoNKSzVyPUO4Mlg{QTFizszN NIDaN4VUSU6JUlXS
SW756 NFrWZodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTuTWM2OD12MD65N|g2KM7:TR?= NVvQXY5zW0GQR2LFVi=>
CAL-72 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL0TWM2OD12Mj6wN{DPxE1? Mn3uV2FPT1KHUh?=
KNS-62 NYe1dHB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV20UGw2UUN3ME20Nk43Ojl4IN88US=> M{\DbHNCVkeURWK=
KARPAS-299 MlW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTR|LkOyN|Mh|ryP NIDweYJUSU6JUlXS
HEL NIPWUGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vWbGlEPTB;NEWuOFY1PiEQvF2= MVnTRW5IWkWU
KP-4 NGG0[VVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DWXmlEPTB;NE[uO|M3OSEQvF2= NY\uW5V1W0GQR2LFVi=>
NEC8 NX;UU4ZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;tXmlEPTB;NEeuNVY3OSEQvF2= NViwXYh{W0GQR2LFVi=>
G-402 NX\6eWJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v2b2lEPTB;NEiuO|AyOiEQvF2= NYDO[45{W0GQR2LFVi=>

... 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
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.

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