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.

    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 NFHTO4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrTTWM2OD1yLkO0O|Y{KM7:TR?= NEmzSWpUSU6JUlXS
DU-145 M3nGXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGniNGhKSzVyPUOuPVM5OTFizszN MkTuV2FPT1KHUh?=
GOTO NGHxUZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzQfVdlUUN3ME22MlM6OTZzIN88US=> M2TRenNCVkeURWK=
NCI-H358 MkPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{joW2lEPTB;Nz61N|gh|ryP MkPmV2FPT1KHUh?=
IST-MES1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TlTGlEPTB;Nz65OVY{PyEQvF2= NYDxd2N[W0GQR2LFVi=>
KP-N-YN MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRThwMkCxPUDPxE1? M3vLZXNCVkeURWK=
T-24 NWPjfm5wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRThwNEC2O|Mh|ryP M3[5U3NCVkeURWK=
MPP-89 MkPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4n6OmlEPTB;OD60OlI2OSEQvF2= NYHrZlhYW0GQR2LFVi=>
NCI-SNU-1 M1\xUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHJemtKSzVyPUmuNFY4OzlizszN M1:3VHNCVkeURWK=
BFTC-905 M{\UOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LZ[mlEPTB;MUCuNVI{OyEQvF2= MVnTRW5IWkWU
MS-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTOflYyUUN3ME2xNE45OjN3IN88US=> MoXMV2FPT1KHUh?=
NBsusSR MoDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LY[GlEPTB;MUCuPFI{PSEQvF2= MYnTRW5IWkWU
BEN MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTF|LkGyOlQh|ryP NV:2bVdGW0GQR2LFVi=>
HMV-II NFfMbHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTF2LkKzNFkh|ryP NVrs[3RxW0GQR2LFVi=>
NCI-H1581 M1jjPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTyTWM2OD1zNz6wOFQ4KM7:TR?= MmXRV2FPT1KHUh?=
ES8 M4GwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XIVmlEPTB;MUeuNVY4KM7:TR?= NU\H[Xh1W0GQR2LFVi=>
LC-2-ad Mn7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHKyfHBKSzVyPUG3MlQ{PjZizszN MoPRV2FPT1KHUh?=
EW-13 M{PTSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPITWM2OD1zNz65OVE3KM7:TR?= NEPjRXBUSU6JUlXS
AN3-CA M2nuS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPPXWNEUUN3ME2xPE4yKM7:TR?= NV\GdHJGW0GQR2LFVi=>
DB M2GxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn4S3lKSzVyPUG4Mlc6OjNizszN NYnMSohiW0GQR2LFVi=>
SK-MEL-1 NIPwPItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJyLkO2PFMh|ryP NHjwU|RUSU6JUlXS
CAPAN-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLwWppKSzVyPUKyMlE5QDRizszN MV;TRW5IWkWU
NCI-H2228 NEDIUHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TZUWlEPTB;MkOuOlY3QCEQvF2= MWTTRW5IWkWU
HOP-92 M2PBRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfHR|VMUUN3ME2yOE4{QDN6IN88US=> M2DveHNCVkeURWK=
KYSE-270 M{e5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC1S4VKSzVyPUK0MlU2PzNizszN M4XycXNCVkeURWK=
HCC1806 M1jOTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPiW3UzUUN3ME2yOE44Pzl7IN88US=> NIjhNXRUSU6JUlXS
HuO-3N1 NUnxb2dKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\NeW9KSzVyPUK1MlgyQDVizszN MWjTRW5IWkWU
HOS MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj2NXVKSzVyPUK1MlkzQTJizszN MlS1V2FPT1KHUh?=
KYSE-510 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fo[mlEPTB;Mk[uNVYyOiEQvF2= NXXRfHFUW0GQR2LFVi=>
COLO-741 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrR[GlKSzVyPUK2MlM{OjlizszN MljLV2FPT1KHUh?=
H-EMC-SS NXvJTHhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mom5TWM2OD1{Nj65NlQ2KM7:TR?= Ml\BV2FPT1KHUh?=
HCC1937 M363Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjTc4JQUUN3ME2yO{4zOjN6IN88US=> Mon0V2FPT1KHUh?=
NCI-H2126 NVfVRXdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlWyTWM2OD1{Nz6zPVc2KM7:TR?= MlzMV2FPT1KHUh?=
NCI-H1703 NIHKSJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDneWpKSzVyPUK4MlA1OTNizszN MmPlV2FPT1KHUh?=
U-2-OS NUTm[ZhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ew[mlEPTB;MkiuOVUyPSEQvF2= NXfUZmdyW0GQR2LFVi=>
DBTRG-05MG NWnrVnY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlmzTWM2OD1{OD61OlUyKM7:TR?= NVe0VIlmW0GQR2LFVi=>
MHH-ES-1 NWrPVXhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLHfodsUUN3ME2zNU46PDFizszN NHPVe4JUSU6JUlXS
HCC1419 M1[zT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXGwbWJ2UUN3ME2zNk4yOTF7IN88US=> MnnLV2FPT1KHUh?=
HOP-62 MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT2TWM2OD1|Mj6yO|AyKM7:TR?= MkfnV2FPT1KHUh?=
AM-38 NFrKboRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TWbGlEPTB;M{KuPVk{OSEQvF2= M1;D[3NCVkeURWK=
NCI-H2009 NF:ycW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HzZWlEPTB;M{OuOFAxPyEQvF2= Mlq1V2FPT1KHUh?=
EM-2 M162b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDkW3lYUUN3ME2zN{42PTFzIN88US=> NYKxZWJtW0GQR2LFVi=>
SW1116 M3H6emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTN2LkS4N|gh|ryP M3TqeHNCVkeURWK=
SK-N-AS Mn7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHj0UnJKSzVyPUO1MlA4OTRizszN M3PTW3NCVkeURWK=
ChaGo-K-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHTSnVKSzVyPUO1MlYxOzJizszN NUjT[|VsW0GQR2LFVi=>
RT-112 NIn6e4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTN3Lkm4O|kh|ryP MmjuV2FPT1KHUh?=
HTC-C3 NYCyVldiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmX2TWM2OD1|Nj6yN|U2KM7:TR?= MlfsV2FPT1KHUh?=
SK-NEP-1 NVzF[mhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH0b5JxUUN3ME2zOk43OTB4IN88US=> NGDRb25USU6JUlXS
LB831-BLC NIfaSJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DmSGlEPTB;M{euOlU1OSEQvF2= NFPZNoRUSU6JUlXS
CTB-1 MoLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfk[|BKSzVyPUO4MlQ2OTJizszN MoXNV2FPT1KHUh?=
MOLT-4 NGX6bmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M335bGlEPTB;M{iuPFM6OSEQvF2= NYThT2RHW0GQR2LFVi=>
SW756 M4mxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDZVGZDUUN3ME20NE46Ozh3IN88US=> NIHOUphUSU6JUlXS
CAL-72 NGX5N5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHac5lKSzVyPUSyMlA{KM7:TR?= NFGxOHBUSU6JUlXS
KNS-62 NVrhcJo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYf3dXNpUUN3ME20Nk43Ojl4IN88US=> Mm\hV2FPT1KHUh?=
KARPAS-299 NYi1WFdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmf5TWM2OD12Mz6zNlM{KM7:TR?= M2C1TXNCVkeURWK=
HEL NXvn[FN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;nfpBFUUN3ME20OU41PjR4IN88US=> NXLh[4g5W0GQR2LFVi=>
KP-4 M3LTbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\UWWlEPTB;NE[uO|M3OSEQvF2= NHPTSY1USU6JUlXS
NEC8 MorIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7zdppKSzVyPUS3MlE3PjFizszN NXvpXmlzW0GQR2LFVi=>
G-402 M{\hRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzDc5NCUUN3ME20PE44ODF{IN88US=> NYPkVmRoW0GQR2LFVi=>

... 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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID