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 NX\H[5RzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjjeGZKSzVyPUCuN|Q4PjNizszN M1;DdnNCVkeURWK=
DU-145 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jGXmlEPTB;Mz65N|gyOSEQvF2= M2HnWXNCVkeURWK=
GOTO NVfJOZFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmf1TWM2OD14LkO5NVYyKM7:TR?= Mn7lV2FPT1KHUh?=
NCI-H358 NV7SS3lrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[2TWM2OD15LkWzPEDPxE1? MnjzV2FPT1KHUh?=
IST-MES1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmixTWM2OD15Lkm1OlM4KM7:TR?= NWOw[XRvW0GQR2LFVi=>
KP-N-YN M3Ls[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TGU2lEPTB;OD6yNFE6KM7:TR?= M{ThfHNCVkeURWK=
T-24 MljzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rQbWlEPTB;OD60NFY4OyEQvF2= NWj3cnVtW0GQR2LFVi=>
MPP-89 NULsUmVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3LTWM2OD16LkS2NlUyKM7:TR?= MlmyV2FPT1KHUh?=
NCI-SNU-1 NYDUb3pvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\wTWM2OD17LkC2O|M6KM7:TR?= M17lR3NCVkeURWK=
BFTC-905 NUX4U5ZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoT3TWM2OD1zMD6xNlM{KM7:TR?= NHm2dVRUSU6JUlXS
MS-1 M1rCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfNWFV3UUN3ME2xNE45OjN3IN88US=> NXrZU3pEW0GQR2LFVi=>
NBsusSR MkPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7zSFllUUN3ME2xNE45OjN3IN88US=> NXfFZVZsW0GQR2LFVi=>
BEN MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\oNHc6UUN3ME2xN{4yOjZ2IN88US=> M4DyWXNCVkeURWK=
HMV-II MljwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHq1WoFKSzVyPUG0MlI{ODlizszN NF;ocWtUSU6JUlXS
NCI-H1581 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\SV41KSzVyPUG3MlA1PDdizszN NF\5T|hUSU6JUlXS
ES8 M4LzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlu5TWM2OD1zNz6xOlch|ryP NITUNHhUSU6JUlXS
LC-2-ad MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHK2N29KSzVyPUG3MlQ{PjZizszN MkfkV2FPT1KHUh?=
EW-13 M3nq[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHvXoJ3UUN3ME2xO{46PTF4IN88US=> M3;XR3NCVkeURWK=
AN3-CA MkX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzmTWM2OD1zOD6xJO69VQ>? NX7PV2xlW0GQR2LFVi=>
DB MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn3TWM2OD1zOD63PVI{KM7:TR?= NWjxUY1LW0GQR2LFVi=>
SK-MEL-1 NX;QO|EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJyLkO2PFMh|ryP MXfTRW5IWkWU
CAPAN-1 NVvmeGpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPYSlZKSzVyPUKyMlE5QDRizszN NGL5NXlUSU6JUlXS
NCI-H2228 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLCT29zUUN3ME2yN{43PjZ6IN88US=> M3LmU3NCVkeURWK=
HOP-92 NFzDUYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XXU2lEPTB;MkSuN|g{QCEQvF2= NWG5VJdsW0GQR2LFVi=>
KYSE-270 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlr0TWM2OD1{ND61OVc{KM7:TR?= NHjPR|RUSU6JUlXS
HCC1806 M3XJcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LoV2lEPTB;MkSuO|c6QSEQvF2= M1TMfHNCVkeURWK=
HuO-3N1 M2rxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDpTWM2OD1{NT64NVg2KM7:TR?= NUXPdm5CW0GQR2LFVi=>
HOS Ml;pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVi5[JNYUUN3ME2yOU46Ojl{IN88US=> M2m3dXNCVkeURWK=
KYSE-510 M3TofGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\XTWM2OD1{Nj6xOlEzKM7:TR?= Ml3UV2FPT1KHUh?=
COLO-741 NXzzRVZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT1O4xKSzVyPUK2MlM{OjlizszN MkG1V2FPT1KHUh?=
H-EMC-SS Mkj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPjPVhKSzVyPUK2MlkzPDVizszN NVnZUGZPW0GQR2LFVi=>
HCC1937 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHiU|FKSzVyPUK3MlIzOzhizszN MojsV2FPT1KHUh?=
NCI-H2126 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\OVYl2UUN3ME2yO{4{QTd3IN88US=> NUTnVpFlW0GQR2LFVi=>
NCI-H1703 NV[zSGozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\tTWM2OD1{OD6wOFE{KM7:TR?= NWfyUJRJW0GQR2LFVi=>
U-2-OS M4i1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLFTWM2OD1{OD61OVE2KM7:TR?= M{TwVXNCVkeURWK=
DBTRG-05MG NUTqRZFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfQZYRKSzVyPUK4MlU3PTFizszN MnfkV2FPT1KHUh?=
MHH-ES-1 M4HObmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjZNldKSzVyPUOxMlk1OSEQvF2= NUPLe5BFW0GQR2LFVi=>
HCC1419 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3m4OGlEPTB;M{KuNVEyQSEQvF2= NXnlOINSW0GQR2LFVi=>
HOP-62 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\iXmhrUUN3ME2zNk4zPzBzIN88US=> MWLTRW5IWkWU
AM-38 NX7aT|hNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4X6VWlEPTB;M{KuPVk{OSEQvF2= NYXCNZFnW0GQR2LFVi=>
NCI-H2009 NEXLUlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTN|LkSwNFch|ryP MnnRV2FPT1KHUh?=
EM-2 NF;uW3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PC[WlEPTB;M{OuOVUyOSEQvF2= MYfTRW5IWkWU
SW1116 NX;pfWZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTN2LkS4N|gh|ryP MV;TRW5IWkWU
SK-N-AS MnHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDyUWtKSzVyPUO1MlA4OTRizszN NV7lbIo{W0GQR2LFVi=>
ChaGo-K-1 NVP3VWlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTN3Lk[wN|Ih|ryP M13zVHNCVkeURWK=
RT-112 NFjmeY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7mZY1{UUN3ME2zOU46QDd7IN88US=> MnXjV2FPT1KHUh?=
HTC-C3 NXzjfoV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjpW2lKSzVyPUO2MlI{PTVizszN MY\TRW5IWkWU
SK-NEP-1 M4jmbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTN4Lk[xNFYh|ryP NEftUWhUSU6JUlXS
LB831-BLC MoXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1POdmlEPTB;M{euOlU1OSEQvF2= M3\tfnNCVkeURWK=
CTB-1 NWLPeJJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTN6LkS1NVIh|ryP M3zxXHNCVkeURWK=
MOLT-4 M1XXN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTN6LkizPVEh|ryP M3[1cnNCVkeURWK=
SW756 NVywTHpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlyzTWM2OD12MD65N|g2KM7:TR?= NH7sNmRUSU6JUlXS
CAL-72 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PkcGlEPTB;NEKuNFMh|ryP Mo\xV2FPT1KHUh?=
KNS-62 M3r3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvpTWM2OD12Mj62Nlk3KM7:TR?= M2rQOHNCVkeURWK=
KARPAS-299 NFzoXFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7zTWM2OD12Mz6zNlM{KM7:TR?= Ml;kV2FPT1KHUh?=
HEL MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jMSGlEPTB;NEWuOFY1PiEQvF2= MX\TRW5IWkWU
KP-4 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjvZZJ[UUN3ME20Ok44OzZzIN88US=> Mln5V2FPT1KHUh?=
NEC8 NYqzb|dnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfUTmVpUUN3ME20O{4yPjZzIN88US=> M1OyOnNCVkeURWK=
G-402 NF7kXG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PBWGlEPTB;NEiuO|AyOiEQvF2= NVTFZ3V7W0GQR2LFVi=>

... 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 106 mg/mL (200.88 mM)
Ethanol 106 mg/mL (200.88 mM)
Water slightly soluble or 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
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID