Doramapimod (BIRB 796)

For research use only. Not for use in humans.

Catalog No.S1574

48 publications

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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Selleck's Doramapimod (BIRB 796) has been cited by 48 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 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\6TWM2OD1yLkO0O|Y{KM7:TR?= NVe5[5NnW0GQR2LFVi=>
DU-145 NUnLXmJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDuXY5GUUN3ME2zMlk{QDFzIN88US=> NWWxVJpmW0GQR2LFVi=>
GOTO NXexe4NTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTZwM{mxOlEh|ryP M1;jXXNCVkeURWK=
NCI-H358 M1nTWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[2UY56UUN3ME23MlU{QCEQvF2= MkO1V2FPT1KHUh?=
IST-MES1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTdwOUW2N|ch|ryP MVnTRW5IWkWU
KP-N-YN NYfuR45KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDPNGZ1UUN3ME24MlIxOTlizszN M1PnPXNCVkeURWK=
T-24 NVLkbYNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRThwNEC2O|Mh|ryP NVHrSFZJW0GQR2LFVi=>
MPP-89 MmPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDXR2I4UUN3ME24MlQ3OjVzIN88US=> M3fmc3NCVkeURWK=
NCI-SNU-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTlwME[3N|kh|ryP MVHTRW5IWkWU
BFTC-905 NWTFOI1CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPlZmh[UUN3ME2xNE4yOjN|IN88US=> NI\NT5FUSU6JUlXS
MS-1 NX7XfIJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nZXGlEPTB;MUCuPFI{PSEQvF2= NXy5bG82W0GQR2LFVi=>
NBsusSR MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3Kb3NKSzVyPUGwMlgzOzVizszN MYLTRW5IWkWU
BEN MlrES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXjTWM2OD1zMz6xNlY1KM7:TR?= MWfTRW5IWkWU
HMV-II NEPpUHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjROXRuUUN3ME2xOE4zOzB7IN88US=> M1rmWHNCVkeURWK=
NCI-H1581 NYjYfFZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LYOWlEPTB;MUeuNFQ1PyEQvF2= Mkf0V2FPT1KHUh?=
ES8 NE\hb|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnu2TWM2OD1zNz6xOlch|ryP NGPVTJlUSU6JUlXS
LC-2-ad NXz6VXdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrtO3RKSzVyPUG3MlQ{PjZizszN NXT1VnhlW0GQR2LFVi=>
EW-13 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fOXGlEPTB;MUeuPVUyPiEQvF2= NH23eIlUSU6JUlXS
AN3-CA MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYSyPWZbUUN3ME2xPE4yKM7:TR?= MkXFV2FPT1KHUh?=
DB NVjk[phxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF6Lke5NlMh|ryP MkfRV2FPT1KHUh?=
SK-MEL-1 NGHzOoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTJyLkO2PFMh|ryP NEHhenFUSU6JUlXS
CAPAN-1 MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlO3TWM2OD1{Mj6xPFg1KM7:TR?= NE\1c|lUSU6JUlXS
NCI-H2228 NES2e2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7kd|BKSzVyPUKzMlY3PjhizszN NInSbY1USU6JUlXS
HOP-92 Mm[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUH3[3NHUUN3ME2yOE4{QDN6IN88US=> M1fxe3NCVkeURWK=
KYSE-270 M4TJd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TWUGlEPTB;MkSuOVU4OyEQvF2= MWXTRW5IWkWU
HCC1806 NYfFcIdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTJ2Lke3PVkh|ryP NGLZUYZUSU6JUlXS
HuO-3N1 M2jEOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPiUmZXUUN3ME2yOU45OTh3IN88US=> MmPZV2FPT1KHUh?=
HOS MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\hU2lEPTB;MkWuPVI6OiEQvF2= NXjnPIFlW0GQR2LFVi=>
KYSE-510 MkKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF63S3RKSzVyPUK2MlE3OTJizszN MYLTRW5IWkWU
COLO-741 M3HOSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLSUphCUUN3ME2yOk4{OzJ7IN88US=> M2jxPHNCVkeURWK=
H-EMC-SS NEPpWWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJ4LkmyOFUh|ryP M2nCVnNCVkeURWK=
HCC1937 NF7wb|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1uyOmlEPTB;MkeuNlI{QCEQvF2= NInFV4FUSU6JUlXS
NCI-H2126 NVHjdY4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTJ5LkO5O|Uh|ryP MVjTRW5IWkWU
NCI-H1703 NU\oc2RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTJ6LkC0NVMh|ryP NGLyeHVUSU6JUlXS
U-2-OS NYPoOYl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPUTWM2OD1{OD61OVE2KM7:TR?= NYfZdJozW0GQR2LFVi=>
DBTRG-05MG M{f4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTJ6LkW2OVEh|ryP MWXTRW5IWkWU
MHH-ES-1 MoDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYP3O204UUN3ME2zNU46PDFizszN MVTTRW5IWkWU
HCC1419 M3;mN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS1cG1iUUN3ME2zNk4yOTF7IN88US=> NYX0PXQ3W0GQR2LFVi=>
HOP-62 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTN{LkK3NFEh|ryP NGq0fHlUSU6JUlXS
AM-38 NWLFS2Q2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTN{Lkm5N|Eh|ryP NXn4dZNCW0GQR2LFVi=>
NCI-H2009 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2r0Z2lEPTB;M{OuOFAxPyEQvF2= NFLnZmRUSU6JUlXS
EM-2 M2[1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7IcYV6UUN3ME2zN{42PTFzIN88US=> NVjxTFRnW0GQR2LFVi=>
SW1116 MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjoTWM2OD1|ND60PFM5KM7:TR?= M2PLcHNCVkeURWK=
SK-N-AS Mo\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHPTWM2OD1|NT6wO|E1KM7:TR?= MUPTRW5IWkWU
ChaGo-K-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWn2V4lwUUN3ME2zOU43ODN{IN88US=> MkexV2FPT1KHUh?=
RT-112 NUfU[|NzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfYTWM2OD1|NT65PFc6KM7:TR?= MXrTRW5IWkWU
HTC-C3 M3nWZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEf4OohKSzVyPUO2MlI{PTVizszN MmW2V2FPT1KHUh?=
SK-NEP-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIW3fXFKSzVyPUO2MlYyODZizszN M4LsVHNCVkeURWK=
LB831-BLC NGXkUnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzCTWM2OD1|Nz62OVQyKM7:TR?= MWfTRW5IWkWU
CTB-1 NVrRfIl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjUPYtKSzVyPUO4MlQ2OTJizszN MX7TRW5IWkWU
MOLT-4 NV60Zo1FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETOW2ZKSzVyPUO4Mlg{QTFizszN NULrSYY1W0GQR2LFVi=>
SW756 NEXFXVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGH3doxKSzVyPUSwMlk{QDVizszN M{TEZ3NCVkeURWK=
CAL-72 M3nFSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnYTWM2OD12Mj6wN{DPxE1? MUPTRW5IWkWU
KNS-62 MnzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTR{Lk[yPVYh|ryP NIr2[JNUSU6JUlXS
KARPAS-299 NIDhNXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHiW5JoUUN3ME20N{4{OjN|IN88US=> MUPTRW5IWkWU
HEL NILO[YRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHznS4lKSzVyPUS1MlQ3PDZizszN NUnucHZKW0GQR2LFVi=>
KP-4 M{P6eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTR4LkezOlEh|ryP MkOzV2FPT1KHUh?=
NEC8 NUiwW3pDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTR5LkG2OlEh|ryP NFPFNphUSU6JUlXS
G-402 NETW[|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33ad2lEPTB;NEiuO|AyOiEQvF2= MYrTRW5IWkWU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-p38 / p38 ; 

PubMed: 23349819     


The inhibitory effect of phosphorylated p38 in KB, KBV200 (B) and in MCF-7, MCF-7/ADR (C) treated with BIRB796 at various concentrations after 24 h. 

mTOR / p-S6K / S6K / p-MK2 / MK2 / p-Hsp27 / Hsp27 ; 

PubMed: 26844273     


CRC cells were treated with 4 μM LY2228820, 10 μM BIRB796 or 10 μM SB202190 for 2 h and p38 and mTORC1 signaling was analyzed by immunoblot.

p-p38 / γ-H2AX ; 

PubMed: 27082306     


The expression of p-P38 was tested via protein gel blot after the cells were treated with BIRB796.

23349819 26844273 27082306
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]

- Collapse
  • 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):
5% DMSO+40%PEG300+5%Tween80 +50%H2O
For best results, use promptly after mixing.
5mg/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
Smiles CC1=CC=C(C=C1)[N]2N=C(C=C2NC(=O)NC3=CC=C(OCCN4CCOCC4)C5=C3C=CC=C5)C(C)(C)C

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID