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 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\Tc|liUUN3ME2wMlM1PzZ|IN88US=> MXHTRW5IWkWU
DU-145 M1jWNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTlTWM2OD1|LkmzPFEyKM7:TR?= NIXYbGZUSU6JUlXS
GOTO M4ezcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLYS3hKSzVyPU[uN|kyPjFizszN MoPYV2FPT1KHUh?=
NCI-H358 NYC0VFFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml31TWM2OD15LkWzPEDPxE1? NEezZ25USU6JUlXS
IST-MES1 NH3nPIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTdwOUW2N|ch|ryP MoDnV2FPT1KHUh?=
KP-N-YN NGLPfZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Thd2lEPTB;OD6yNFE6KM7:TR?= NHnMOJdUSU6JUlXS
T-24 MmPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnDe45vUUN3ME24MlQxPjd|IN88US=> MXfTRW5IWkWU
MPP-89 Mo\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzYTWM2OD16LkS2NlUyKM7:TR?= NX7aN4ZsW0GQR2LFVi=>
NCI-SNU-1 MmPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTlwME[3N|kh|ryP NVPjXHB6W0GQR2LFVi=>
BFTC-905 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFyLkGyN|Mh|ryP NYLPfohUW0GQR2LFVi=>
MS-1 MknYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfmTWM2OD1zMD64NlM2KM7:TR?= NELZb4RUSU6JUlXS
NBsusSR MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTFyLkiyN|Uh|ryP NULmUHl3W0GQR2LFVi=>
BEN NUDOVIFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e2fmlEPTB;MUOuNVI3PCEQvF2= MV7TRW5IWkWU
HMV-II MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7UeodlUUN3ME2xOE4zOzB7IN88US=> NV7KOoNQW0GQR2LFVi=>
NCI-H1581 NF[yRnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfsS5RvUUN3ME2xO{4xPDR5IN88US=> NV;we2IyW0GQR2LFVi=>
ES8 MkjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF74WnRKSzVyPUG3MlE3PyEQvF2= MWPTRW5IWkWU
LC-2-ad MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17zOWlEPTB;MUeuOFM3PiEQvF2= NGj3cVNUSU6JUlXS
EW-13 MnHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\wUmRKSzVyPUG3Mlk2OTZizszN NX3PeItPW0GQR2LFVi=>
AN3-CA MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTF6LkGg{txO MWXTRW5IWkWU
DB MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTF6Lke5NlMh|ryP MXjTRW5IWkWU
SK-MEL-1 NVnGc3ZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4n6fmlEPTB;MkCuN|Y5OyEQvF2= Mkj6V2FPT1KHUh?=
CAPAN-1 NFHLb3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJ{LkG4PFQh|ryP NHfWelJUSU6JUlXS
NCI-H2228 M3TObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTJ|Lk[2Olgh|ryP MmrLV2FPT1KHUh?=
HOP-92 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV6z[JNSUUN3ME2yOE4{QDN6IN88US=> MoLEV2FPT1KHUh?=
KYSE-270 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\aR29bUUN3ME2yOE42PTd|IN88US=> NXO3RlltW0GQR2LFVi=>
HCC1806 NIW3eYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfoOY14UUN3ME2yOE44Pzl7IN88US=> M4XybHNCVkeURWK=
HuO-3N1 NY\CeJY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXZTWM2OD1{NT64NVg2KM7:TR?= MUnTRW5IWkWU
HOS M333cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjxUWxKSzVyPUK1MlkzQTJizszN NWXme|g3W0GQR2LFVi=>
KYSE-510 NXzKSmJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvjXpRkUUN3ME2yOk4yPjF{IN88US=> NFLFe3JUSU6JUlXS
COLO-741 MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLsZ2hKSzVyPUK2MlM{OjlizszN NWLvU4d3W0GQR2LFVi=>
H-EMC-SS M4CzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHv[5pKSzVyPUK2MlkzPDVizszN NG\wbmdUSU6JUlXS
HCC1937 MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2KxbmlEPTB;MkeuNlI{QCEQvF2= MlW4V2FPT1KHUh?=
NCI-H2126 M4DPeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojKTWM2OD1{Nz6zPVc2KM7:TR?= NV\LW2xQW0GQR2LFVi=>
NCI-H1703 NXfDcpBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PLUWlEPTB;MkiuNFQyOyEQvF2= MULTRW5IWkWU
U-2-OS MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn:2TWM2OD1{OD61OVE2KM7:TR?= MVnTRW5IWkWU
DBTRG-05MG MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYCx[pVMUUN3ME2yPE42PjVzIN88US=> MoPvV2FPT1KHUh?=
MHH-ES-1 MnW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3r3W2lEPTB;M{GuPVQyKM7:TR?= MXzTRW5IWkWU
HCC1419 M{LZ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrvc|RKSzVyPUOyMlEyOTlizszN NWXqeWtXW0GQR2LFVi=>
HOP-62 M{\CTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTvRnE3UUN3ME2zNk4zPzBzIN88US=> M2DVenNCVkeURWK=
AM-38 NHfrcnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXkTWM2OD1|Mj65PVMyKM7:TR?= MkLCV2FPT1KHUh?=
NCI-H2009 MoPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T6bGlEPTB;M{OuOFAxPyEQvF2= MnK1V2FPT1KHUh?=
EM-2 NHfqeXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHIUldKSzVyPUOzMlU2OTFizszN MoTUV2FPT1KHUh?=
SW1116 NYXZPWN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfUb2lGUUN3ME2zOE41QDN6IN88US=> NIT6cYVUSU6JUlXS
SK-N-AS NFyyUnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1e2OGlEPTB;M{WuNFcyPCEQvF2= MWDTRW5IWkWU
ChaGo-K-1 MmG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PZRWlEPTB;M{WuOlA{OiEQvF2= M2DCUnNCVkeURWK=
RT-112 NVn5XoxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTZTWM2OD1|NT65PFc6KM7:TR?= M4X2TnNCVkeURWK=
HTC-C3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTN4LkKzOVUh|ryP MXHTRW5IWkWU
SK-NEP-1 NUTSd3NzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXKbpdKSzVyPUO2MlYyODZizszN MnmyV2FPT1KHUh?=
LB831-BLC M1LGVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX5SFdKSzVyPUO3MlY2PDFizszN MlL4V2FPT1KHUh?=
CTB-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3flTGlEPTB;M{iuOFUyOiEQvF2= M4PSVXNCVkeURWK=
MOLT-4 MlfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTxO3FKUUN3ME2zPE45OzlzIN88US=> MWLTRW5IWkWU
SW756 NUGzOVF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnHTWM2OD12MD65N|g2KM7:TR?= MXnTRW5IWkWU
CAL-72 M2XKRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfaVXNCUUN3ME20Nk4xOyEQvF2= MVHTRW5IWkWU
KNS-62 NUnNfYpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XLTmlEPTB;NEKuOlI6PiEQvF2= NXnPT45HW0GQR2LFVi=>
KARPAS-299 M2HJVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[zTWM2OD12Mz6zNlM{KM7:TR?= NYfNbFhZW0GQR2LFVi=>
HEL MkT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmC4TWM2OD12NT60OlQ3KM7:TR?= MVPTRW5IWkWU
KP-4 NXnjcnd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTR4LkezOlEh|ryP NWjqUWExW0GQR2LFVi=>
NEC8 NFPUNXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTUU2hKSzVyPUS3MlE3PjFizszN M3G0eXNCVkeURWK=
G-402 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfCTWM2OD12OD63NFEzKM7:TR?= NHzTb3BUSU6JUlXS

... 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

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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