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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Cited by 23 Publications

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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 NXXCN|NbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHjTWM2OD1yLkO0O|Y{KM7:TR?= NXLMW|V1W0GQR2LFVi=>
DU-145 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTNwOUO4NVEh|ryP NFfuSIlUSU6JUlXS
GOTO MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUmwepFNUUN3ME22MlM6OTZzIN88US=> MYnTRW5IWkWU
NCI-H358 MmPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\LXHBKSzVyPUeuOVM5KM7:TR?= MnHEV2FPT1KHUh?=
IST-MES1 M1L1e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPNTWM2OD15Lkm1OlM4KM7:TR?= MkHUV2FPT1KHUh?=
KP-N-YN M3;JVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfrVlFKSzVyPUiuNlAyQSEQvF2= NXznOY1RW0GQR2LFVi=>
T-24 M3XSSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjrPFFKSzVyPUiuOFA3PzNizszN NVXs[lVXW0GQR2LFVi=>
MPP-89 M{PCT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLDTWM2OD16LkS2NlUyKM7:TR?= NWTRNnNlW0GQR2LFVi=>
NCI-SNU-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTlwME[3N|kh|ryP M{LDRXNCVkeURWK=
BFTC-905 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr4RmxKSzVyPUGwMlEzOzNizszN MWnTRW5IWkWU
MS-1 MnGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFyLkiyN|Uh|ryP NF\Se|ZUSU6JUlXS
NBsusSR NGXxTYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvuXlRKSzVyPUGwMlgzOzVizszN NFXBbXNUSU6JUlXS
BEN MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF|LkGyOlQh|ryP MVrTRW5IWkWU
HMV-II Ml[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDQWJh[UUN3ME2xOE4zOzB7IN88US=> MUjTRW5IWkWU
NCI-H1581 NVf5fpJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3jdHdFUUN3ME2xO{4xPDR5IN88US=> Ml63V2FPT1KHUh?=
ES8 MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPnTGRKSzVyPUG3MlE3PyEQvF2= NVq1Uos2W0GQR2LFVi=>
LC-2-ad NVnnUGtpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;TcGlEPTB;MUeuOFM3PiEQvF2= M{[xRXNCVkeURWK=
EW-13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPyflJzUUN3ME2xO{46PTF4IN88US=> NV\XUpZ[W0GQR2LFVi=>
AN3-CA M3vBbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIOxd3lKSzVyPUG4MlEh|ryP NXyyTGdxW0GQR2LFVi=>
DB MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjYWlcxUUN3ME2xPE44QTJ|IN88US=> MVfTRW5IWkWU
SK-MEL-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJyLkO2PFMh|ryP NWTlS3RRW0GQR2LFVi=>
CAPAN-1 M{PiU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTJ{LkG4PFQh|ryP NWHOfYRUW0GQR2LFVi=>
NCI-H2228 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJ|Lk[2Olgh|ryP MYrTRW5IWkWU
HOP-92 M1P4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofhTWM2OD1{ND6zPFM5KM7:TR?= NV;RWYZuW0GQR2LFVi=>
KYSE-270 MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJ2LkW1O|Mh|ryP NYnQO3hvW0GQR2LFVi=>
HCC1806 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljKTWM2OD1{ND63O|k6KM7:TR?= MVjTRW5IWkWU
HuO-3N1 MnjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJ3LkixPFUh|ryP NYLRfVhwW0GQR2LFVi=>
HOS M{XIemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ3LkmyPVIh|ryP MWPTRW5IWkWU
KYSE-510 M2noXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnIfZdlUUN3ME2yOk4yPjF{IN88US=> NV;hR29zW0GQR2LFVi=>
COLO-741 NUHqUW1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnQOGZIUUN3ME2yOk4{OzJ7IN88US=> M{fPTHNCVkeURWK=
H-EMC-SS NWr6NW52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\0emlEPTB;Mk[uPVI1PSEQvF2= NY\kSZRbW0GQR2LFVi=>
HCC1937 MliyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPSTWM2OD1{Nz6yNlM5KM7:TR?= NUDCfXFoW0GQR2LFVi=>
NCI-H2126 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;vWYl[UUN3ME2yO{4{QTd3IN88US=> NH7hW4JUSU6JUlXS
NCI-H1703 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPDTWM2OD1{OD6wOFE{KM7:TR?= NG\VWppUSU6JUlXS
U-2-OS M1nBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfKT4RKSzVyPUK4MlU2OTVizszN NX64RlNkW0GQR2LFVi=>
DBTRG-05MG M1;HW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVv3SHNbUUN3ME2yPE42PjVzIN88US=> NXe4dWl3W0GQR2LFVi=>
MHH-ES-1 M1zKPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnTUmc4UUN3ME2zNU46PDFizszN MUnTRW5IWkWU
HCC1419 NYLlO21sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7KdVkyUUN3ME2zNk4yOTF7IN88US=> NGjjVZVUSU6JUlXS
HOP-62 Mlv1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX3TWM2OD1|Mj6yO|AyKM7:TR?= NULvZXZlW0GQR2LFVi=>
AM-38 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTN{Lkm5N|Eh|ryP MWrTRW5IWkWU
NCI-H2009 NHfp[YhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTN|LkSwNFch|ryP MVTTRW5IWkWU
EM-2 NIPwXllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTSTWM2OD1|Mz61OVEyKM7:TR?= NVjNbnh5W0GQR2LFVi=>
SW1116 NFjBUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rMPGlEPTB;M{SuOFg{QCEQvF2= NEDJZmxUSU6JUlXS
SK-N-AS NFrEU5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TNO2lEPTB;M{WuNFcyPCEQvF2= NWi1PWt1W0GQR2LFVi=>
ChaGo-K-1 NEXaVVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37FWmlEPTB;M{WuOlA{OiEQvF2= NWq3V2J4W0GQR2LFVi=>
RT-112 MmXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfzWItlUUN3ME2zOU46QDd7IN88US=> M1O2enNCVkeURWK=
HTC-C3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTVTFVKSzVyPUO2MlI{PTVizszN MYDTRW5IWkWU
SK-NEP-1 M1vnNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33Rc2lEPTB;M{[uOlExPiEQvF2= MW\TRW5IWkWU
LB831-BLC Ml7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvZSmZKSzVyPUO3MlY2PDFizszN M2m1OnNCVkeURWK=
CTB-1 NF7iTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;1U4ROUUN3ME2zPE41PTF{IN88US=> M2HWOnNCVkeURWK=
MOLT-4 M4q2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTN6LkizPVEh|ryP NWXNdIdiW0GQR2LFVi=>
SW756 M3z3cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTRyLkmzPFUh|ryP NFf2OFVUSU6JUlXS
CAL-72 NUX4XWpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HEc2lEPTB;NEKuNFMh|ryP NXnkZVl2W0GQR2LFVi=>
KNS-62 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnq5TWM2OD12Mj62Nlk3KM7:TR?= NUn6Z2t[W0GQR2LFVi=>
KARPAS-299 MnSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXi0c5I3UUN3ME20N{4{OjN|IN88US=> NG\0eZRUSU6JUlXS
HEL M2XqVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPmOHBKSzVyPUS1MlQ3PDZizszN NXiyWGVVW0GQR2LFVi=>
KP-4 Mn7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrOWmhyUUN3ME20Ok44OzZzIN88US=> M4\Od3NCVkeURWK=
NEC8 Mmq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTR5LkG2OlEh|ryP MWLTRW5IWkWU
G-402 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTIV5VKSzVyPUS4MlcxOTJizszN M{j6XnNCVkeURWK=

... 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
NCT02214888 Terminated Arthritis Rheumatoid Boehringer Ingelheim May 2003 Phase 2
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2

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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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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID