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 MnzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXpOHVKSzVyPUCuN|Q4PjNizszN NGL2cVlUSU6JUlXS
DU-145 MmLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXjTWM2OD1|LkmzPFEyKM7:TR?= MkLEV2FPT1KHUh?=
GOTO MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITwO|FKSzVyPU[uN|kyPjFizszN NFrOWW5USU6JUlXS
NCI-H358 M4f5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTdwNUO4JO69VQ>? NGrMN5JUSU6JUlXS
IST-MES1 NWjFdFMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTdwOUW2N|ch|ryP NGj4T3dUSU6JUlXS
KP-N-YN NITJZlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HVeWlEPTB;OD6yNFE6KM7:TR?= NF[3bVZUSU6JUlXS
T-24 NYK3bYEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2mxdWlEPTB;OD60NFY4OyEQvF2= M4q3bnNCVkeURWK=
MPP-89 NYXZeZZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfuPFlKSzVyPUiuOFYzPTFizszN NYK3Om9yW0GQR2LFVi=>
NCI-SNU-1 NEjFPXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHNS|JJUUN3ME25MlA3PzN7IN88US=> MYrTRW5IWkWU
BFTC-905 NFfBb4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWr0T2ZxUUN3ME2xNE4yOjN|IN88US=> NFvhVJlUSU6JUlXS
MS-1 M4HRUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFyLkiyN|Uh|ryP MnXUV2FPT1KHUh?=
NBsusSR M1f6e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HLOGlEPTB;MUCuPFI{PSEQvF2= MVHTRW5IWkWU
BEN MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHTfWRKSzVyPUGzMlEzPjRizszN NVzEbZB5W0GQR2LFVi=>
HMV-II NG\3S2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUn0VFRuUUN3ME2xOE4zOzB7IN88US=> MoS1V2FPT1KHUh?=
NCI-H1581 NHPpfnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlewTWM2OD1zNz6wOFQ4KM7:TR?= MXHTRW5IWkWU
ES8 MmPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnHVFlVUUN3ME2xO{4yPjdizszN NUSyRmhPW0GQR2LFVi=>
LC-2-ad Ml7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfiTWM2OD1zNz60N|Y3KM7:TR?= MYXTRW5IWkWU
EW-13 M{Szbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzTSFJKSzVyPUG3Mlk2OTZizszN MlGwV2FPT1KHUh?=
AN3-CA MmDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jxRmlEPTB;MUiuNUDPxE1? M2HjTnNCVkeURWK=
DB M{C3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nWW2lEPTB;MUiuO|kzOyEQvF2= MnfTV2FPT1KHUh?=
SK-MEL-1 MlLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTJyLkO2PFMh|ryP MmfMV2FPT1KHUh?=
CAPAN-1 NUTvfm9wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTJ{LkG4PFQh|ryP NU\kVodKW0GQR2LFVi=>
NCI-H2228 NHHoWpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXtcYVGUUN3ME2yN{43PjZ6IN88US=> M4nKcHNCVkeURWK=
HOP-92 MnG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvMSJNKSzVyPUK0MlM5OzhizszN M2X6enNCVkeURWK=
KYSE-270 NFXzRXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvOTWM2OD1{ND61OVc{KM7:TR?= M2jvOXNCVkeURWK=
HCC1806 NYDLfZY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvRPYZwUUN3ME2yOE44Pzl7IN88US=> MkS2V2FPT1KHUh?=
HuO-3N1 MnK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XEd2lEPTB;MkWuPFE5PSEQvF2= M3LXR3NCVkeURWK=
HOS NI\sR3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTQUFBoUUN3ME2yOU46Ojl{IN88US=> NVXPZZpmW0GQR2LFVi=>
KYSE-510 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTJ4LkG2NVIh|ryP NGDtTmNUSU6JUlXS
COLO-741 MnfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUmzToJqUUN3ME2yOk4{OzJ7IN88US=> MUjTRW5IWkWU
H-EMC-SS NXPnW3dbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXRTWM2OD1{Nj65NlQ2KM7:TR?= M2XKWXNCVkeURWK=
HCC1937 MmT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zlR2lEPTB;MkeuNlI{QCEQvF2= MVLTRW5IWkWU
NCI-H2126 MknUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJ5LkO5O|Uh|ryP MXLTRW5IWkWU
NCI-H1703 M3zpRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrlTI9KSzVyPUK4MlA1OTNizszN MXnTRW5IWkWU
U-2-OS MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Hv[2lEPTB;MkiuOVUyPSEQvF2= MUjTRW5IWkWU
DBTRG-05MG M4\v[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlexTWM2OD1{OD61OlUyKM7:TR?= Mlm2V2FPT1KHUh?=
MHH-ES-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoT5TWM2OD1|MT65OFEh|ryP Mmn2V2FPT1KHUh?=
HCC1419 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTN{LkGxNVkh|ryP MmPNV2FPT1KHUh?=
HOP-62 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTkfFBKSzVyPUOyMlI4ODFizszN MVPTRW5IWkWU
AM-38 M3vVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHewTVVKSzVyPUOyMlk6OzFizszN MlHsV2FPT1KHUh?=
NCI-H2009 NV\1ZnExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrMXpZKSzVyPUOzMlQxODdizszN MYjTRW5IWkWU
EM-2 M3fBfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHH4O|FKSzVyPUOzMlU2OTFizszN MUfTRW5IWkWU
SW1116 NVjXc5ZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1[0bWlEPTB;M{SuOFg{QCEQvF2= NXTh[5NRW0GQR2LFVi=>
SK-N-AS M1XO[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jIR2lEPTB;M{WuNFcyPCEQvF2= NVLDfII3W0GQR2LFVi=>
ChaGo-K-1 NI\USZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XEPWlEPTB;M{WuOlA{OiEQvF2= Mk[wV2FPT1KHUh?=
RT-112 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTN3Lkm4O|kh|ryP NY\veYdyW0GQR2LFVi=>
HTC-C3 NEPrNZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zzfWlEPTB;M{[uNlM2PSEQvF2= MX\TRW5IWkWU
SK-NEP-1 Mn3IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTN4Lk[xNFYh|ryP NUnBNm83W0GQR2LFVi=>
LB831-BLC NVTjTG9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvSXYFnUUN3ME2zO{43PTRzIN88US=> NH\qdVlUSU6JUlXS
CTB-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUi5cndXUUN3ME2zPE41PTF{IN88US=> MUXTRW5IWkWU
MOLT-4 M1PCSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmH4TWM2OD1|OD64N|kyKM7:TR?= M2SwNHNCVkeURWK=
SW756 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\jTWM2OD12MD65N|g2KM7:TR?= NVzyWGdWW0GQR2LFVi=>
CAL-72 MojXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTR{LkCzJO69VQ>? MYPTRW5IWkWU
KNS-62 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojPTWM2OD12Mj62Nlk3KM7:TR?= MV3TRW5IWkWU
KARPAS-299 MlrhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{ntcWlEPTB;NEOuN|I{OyEQvF2= NI\ofJVUSU6JUlXS
HEL M{TxUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;PdnhFUUN3ME20OU41PjR4IN88US=> NVzrNFRrW0GQR2LFVi=>
KP-4 NWizWoRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjRUldEUUN3ME20Ok44OzZzIN88US=> NIrzNFdUSU6JUlXS
NEC8 MmOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrRUHptUUN3ME20O{4yPjZzIN88US=> NYHLOlZQW0GQR2LFVi=>
G-402 M4\RdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTR6LkewNVIh|ryP NHjZ[mZUSU6JUlXS

... 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.

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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID