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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USD 270 In stock
USD 470 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.

    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 Mk\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwM{S3OlMh|ryP Mn3hV2FPT1KHUh?=
DU-145 MlThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXLeYNKSzVyPUOuPVM5OTFizszN M4mxe3NCVkeURWK=
GOTO MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTZwM{mxOlEh|ryP NHTWfVBUSU6JUlXS
NCI-H358 MlrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXjPG5KSzVyPUeuOVM5KM7:TR?= NF;oUGtUSU6JUlXS
IST-MES1 Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTdwOUW2N|ch|ryP NEnnTIJUSU6JUlXS
KP-N-YN M{Dk[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojOTWM2OD16LkKwNVkh|ryP MnXIV2FPT1KHUh?=
T-24 Mlj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jTbmlEPTB;OD60NFY4OyEQvF2= M2jCd3NCVkeURWK=
MPP-89 MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXYTWM2OD16LkS2NlUyKM7:TR?= M3\HVnNCVkeURWK=
NCI-SNU-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1qzO2lEPTB;OT6wOlc{QSEQvF2= MmrxV2FPT1KHUh?=
BFTC-905 NWTyR|luT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nFemlEPTB;MUCuNVI{OyEQvF2= NULueZZYW0GQR2LFVi=>
MS-1 NHf5R5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3WyWmlEPTB;MUCuPFI{PSEQvF2= NGnlOFVUSU6JUlXS
NBsusSR NX;RZXlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\j[XZKSzVyPUGwMlgzOzVizszN MVzTRW5IWkWU
BEN NXH2PY1zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTF|LkGyOlQh|ryP NHfwUFlUSU6JUlXS
HMV-II NXq5bGF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnNVldUUUN3ME2xOE4zOzB7IN88US=> NFq5NWRUSU6JUlXS
NCI-H1581 MnTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDqZ21KSzVyPUG3MlA1PDdizszN MWLTRW5IWkWU
ES8 M{fvVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTF5LkG2O{DPxE1? M1f3eHNCVkeURWK=
LC-2-ad NEe3PIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jM[WlEPTB;MUeuOFM3PiEQvF2= MlP4V2FPT1KHUh?=
EW-13 NHHHXIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHnSYRKSzVyPUG3Mlk2OTZizszN NWOzSHFTW0GQR2LFVi=>
AN3-CA NVXYVGdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXtTWM2OD1zOD6xJO69VQ>? MXPTRW5IWkWU
DB MonnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\wd2lEPTB;MUiuO|kzOyEQvF2= M{PG[HNCVkeURWK=
SK-MEL-1 MoXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTJyLkO2PFMh|ryP NI\KV41USU6JUlXS
CAPAN-1 NFP3cGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJ{LkG4PFQh|ryP NF3lZ5VUSU6JUlXS
NCI-H2228 NInZb25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;2dWlEPTB;MkOuOlY3QCEQvF2= Mni3V2FPT1KHUh?=
HOP-92 NFTISpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmewTWM2OD1{ND6zPFM5KM7:TR?= MXrTRW5IWkWU
KYSE-270 M4W3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzDcG12UUN3ME2yOE42PTd|IN88US=> M4DmNXNCVkeURWK=
HCC1806 NYi1XXV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLHWI1KSzVyPUK0Mlc4QTlizszN M4W2cnNCVkeURWK=
HuO-3N1 MoLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1:5emlEPTB;MkWuPFE5PSEQvF2= MVnTRW5IWkWU
HOS MnLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPSTWM2OD1{NT65NlkzKM7:TR?= M4njdnNCVkeURWK=
KYSE-510 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\ZSY1KSzVyPUK2MlE3OTJizszN M2i0S3NCVkeURWK=
COLO-741 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFS3Z2xKSzVyPUK2MlM{OjlizszN NHzSXGxUSU6JUlXS
H-EMC-SS MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWqweVhbUUN3ME2yOk46OjR3IN88US=> M1f0SHNCVkeURWK=
HCC1937 NWq0[VVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHZTWM2OD1{Nz6yNlM5KM7:TR?= NXrwSm83W0GQR2LFVi=>
NCI-H2126 MlXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJ5LkO5O|Uh|ryP MWjTRW5IWkWU
NCI-H1703 M4jEfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJ6LkC0NVMh|ryP Ml\NV2FPT1KHUh?=
U-2-OS Ml7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3eyV2lEPTB;MkiuOVUyPSEQvF2= NYrJS3p4W0GQR2LFVi=>
DBTRG-05MG NEDUNJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInqUpdKSzVyPUK4MlU3PTFizszN MYTTRW5IWkWU
MHH-ES-1 NUTXVZJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLpTWM2OD1|MT65OFEh|ryP NVrse3FTW0GQR2LFVi=>
HCC1419 Mk\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPBWXoyUUN3ME2zNk4yOTF7IN88US=> NYqwcZFQW0GQR2LFVi=>
HOP-62 M2jqZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTN{LkK3NFEh|ryP Mn3DV2FPT1KHUh?=
AM-38 M{PzPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;3e2lEPTB;M{KuPVk{OSEQvF2= M3\rW3NCVkeURWK=
NCI-H2009 NHXlbZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXj[49KSzVyPUOzMlQxODdizszN M3u0UnNCVkeURWK=
EM-2 NVS3NHBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7pTWM2OD1|Mz61OVEyKM7:TR?= NFzWbo5USU6JUlXS
SW1116 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mme1TWM2OD1|ND60PFM5KM7:TR?= MlP1V2FPT1KHUh?=
SK-N-AS NV3rcpFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTN3LkC3NVQh|ryP M2XCVXNCVkeURWK=
ChaGo-K-1 MmLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLrR41KSzVyPUO1MlYxOzJizszN M3z4fXNCVkeURWK=
RT-112 NHj1OopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTETWM2OD1|NT65PFc6KM7:TR?= M4WxPHNCVkeURWK=
HTC-C3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrwXW5JUUN3ME2zOk4zOzV3IN88US=> M{XRWHNCVkeURWK=
SK-NEP-1 NFPxN5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\ybYlKSzVyPUO2MlYyODZizszN MWTTRW5IWkWU
LB831-BLC NYnD[4lzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17VOWlEPTB;M{euOlU1OSEQvF2= M3qyZ3NCVkeURWK=
CTB-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlu0TWM2OD1|OD60OVEzKM7:TR?= MYrTRW5IWkWU
MOLT-4 M1zRVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3WxfmlEPTB;M{iuPFM6OSEQvF2= M3HNXnNCVkeURWK=
SW756 M{P5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLMeY1yUUN3ME20NE46Ozh3IN88US=> NEHsXIlUSU6JUlXS
CAL-72 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[yOlF7UUN3ME20Nk4xOyEQvF2= MXXTRW5IWkWU
KNS-62 NGS3XJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXJb2JKSzVyPUSyMlYzQTZizszN NV\4[Y9iW0GQR2LFVi=>
KARPAS-299 NXPvXWtyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXuwSWxkUUN3ME20N{4{OjN|IN88US=> MlPlV2FPT1KHUh?=
HEL NUK2d|dsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln3TWM2OD12NT60OlQ3KM7:TR?= MW\TRW5IWkWU
KP-4 M2\WR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTR4LkezOlEh|ryP MX;TRW5IWkWU
NEC8 Ml;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTR5LkG2OlEh|ryP M4DHZnNCVkeURWK=
G-402 NX\MfZlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHriWmdKSzVyPUS4MlcxOTJizszN NHuxSHVUSU6JUlXS

... 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:
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
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