Doramapimod (BIRB 796)

For research use only.

Catalog No.S1574

63 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 63 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 NXTxc|VpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVH1OXlqUUN3ME2wMlM1PzZ|IN88US=> NWf2[Zh6W0GQR2LFVi=>
DU-145 MnjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTNwOUO4NVEh|ryP MkjtV2FPT1KHUh?=
GOTO NV60XlJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHUR4JKSzVyPU[uN|kyPjFizszN M3ftOXNCVkeURWK=
NCI-H358 Mn;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXjOFNKSzVyPUeuOVM5KM7:TR?= NEi4R2tUSU6JUlXS
IST-MES1 M2noXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTOV|Y5UUN3ME23Mlk2PjN5IN88US=> M3jRRXNCVkeURWK=
KP-N-YN MlrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRThwMkCxPUDPxE1? Mo\1V2FPT1KHUh?=
T-24 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rRfGlEPTB;OD60NFY4OyEQvF2= NX\KTphFW0GQR2LFVi=>
MPP-89 NGDZTJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PJcmlEPTB;OD60OlI2OSEQvF2= M3\ifHNCVkeURWK=
NCI-SNU-1 NHfHfIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTlwME[3N|kh|ryP NVi1NnREW0GQR2LFVi=>
BFTC-905 NYXrSHRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2K5c2lEPTB;MUCuNVI{OyEQvF2= NETORnNUSU6JUlXS
MS-1 NUDLUYJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTFyLkiyN|Uh|ryP M2DPVnNCVkeURWK=
NBsusSR MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzjTWM2OD1zMD64NlM2KM7:TR?= NIDzc4VUSU6JUlXS
BEN NHnObFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\pRYdKSzVyPUGzMlEzPjRizszN MUjTRW5IWkWU
HMV-II M4PVUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnj2TWM2OD1zND6yN|A6KM7:TR?= NYTWW3NUW0GQR2LFVi=>
NCI-H1581 MnHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPZTWM2OD1zNz6wOFQ4KM7:TR?= NXvP[XlwW0GQR2LFVi=>
ES8 MmnWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPlWJhKSzVyPUG3MlE3PyEQvF2= NU\oNopvW0GQR2LFVi=>
LC-2-ad MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3IXZJKSzVyPUG3MlQ{PjZizszN M1zhWHNCVkeURWK=
EW-13 NU\MVWpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TIdmlEPTB;MUeuPVUyPiEQvF2= MUnTRW5IWkWU
AN3-CA M4jq[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHOTWM2OD1zOD6xJO69VQ>? M{TMfnNCVkeURWK=
DB NHjPSIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDyTWtKSzVyPUG4Mlc6OjNizszN MlTWV2FPT1KHUh?=
SK-MEL-1 M4\ZPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvPXWFCUUN3ME2yNE4{Pjh|IN88US=> NF\GNldUSU6JUlXS
CAPAN-1 Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTHS4pKSzVyPUKyMlE5QDRizszN NXOyeYpVW0GQR2LFVi=>
NCI-H2228 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfIO4VqUUN3ME2yN{43PjZ6IN88US=> MkPaV2FPT1KHUh?=
HOP-92 NVzJfIZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTJ2LkO4N|gh|ryP MkHJV2FPT1KHUh?=
KYSE-270 M33TT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jF[2lEPTB;MkSuOVU4OyEQvF2= NVXsd25RW0GQR2LFVi=>
HCC1806 NILO[FFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\tbZlKSzVyPUK0Mlc4QTlizszN NWCyUGpiW0GQR2LFVi=>
HuO-3N1 M3jQRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTJ3LkixPFUh|ryP NHrMNnJUSU6JUlXS
HOS M{D4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJ3LkmyPVIh|ryP NGDOVpFUSU6JUlXS
KYSE-510 NFPKfmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrFSWRKSzVyPUK2MlE3OTJizszN MVjTRW5IWkWU
COLO-741 NViydmtoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXpTWM2OD1{Nj6zN|I6KM7:TR?= MlPjV2FPT1KHUh?=
H-EMC-SS NGLUfXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTJ4LkmyOFUh|ryP M37NbHNCVkeURWK=
HCC1937 M2rO[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTtTWM2OD1{Nz6yNlM5KM7:TR?= Mn;sV2FPT1KHUh?=
NCI-H2126 NGTNemlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fXNGlEPTB;MkeuN|k4PSEQvF2= M{[1bnNCVkeURWK=
NCI-H1703 M{nTZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rLNGlEPTB;MkiuNFQyOyEQvF2= M1H2dXNCVkeURWK=
U-2-OS MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnqeolKSzVyPUK4MlU2OTVizszN NHLoXmtUSU6JUlXS
DBTRG-05MG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PCNGlEPTB;MkiuOVY2OSEQvF2= MYHTRW5IWkWU
MHH-ES-1 NHOzc5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTNzLkm0NUDPxE1? NH3hRWJUSU6JUlXS
HCC1419 NXT6WYV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTPb4R{UUN3ME2zNk4yOTF7IN88US=> Mlm5V2FPT1KHUh?=
HOP-62 M4nWfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnpVo5sUUN3ME2zNk4zPzBzIN88US=> M1HUTnNCVkeURWK=
AM-38 MkLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPGbmprUUN3ME2zNk46QTNzIN88US=> NH:4c25USU6JUlXS
NCI-H2009 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17QbWlEPTB;M{OuOFAxPyEQvF2= MknNV2FPT1KHUh?=
EM-2 NVjqempDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLMTWM2OD1|Mz61OVEyKM7:TR?= MoXJV2FPT1KHUh?=
SW1116 NHnER3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnzTWM2OD1|ND60PFM5KM7:TR?= MXnTRW5IWkWU
SK-N-AS MojES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnZTWM2OD1|NT6wO|E1KM7:TR?= NGDscYxUSU6JUlXS
ChaGo-K-1 M{LKPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXy2cWdCUUN3ME2zOU43ODN{IN88US=> M1vhXXNCVkeURWK=
RT-112 NF7hToNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTN3Lkm4O|kh|ryP M4n0OnNCVkeURWK=
HTC-C3 NWPGN4htT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXQTWM2OD1|Nj6yN|U2KM7:TR?= NH;FSo5USU6JUlXS
SK-NEP-1 M3vKTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[zOHZKSzVyPUO2MlYyODZizszN MkDvV2FPT1KHUh?=
LB831-BLC MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrHVldKSzVyPUO3MlY2PDFizszN MWPTRW5IWkWU
CTB-1 MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWT6TI5QUUN3ME2zPE41PTF{IN88US=> MljBV2FPT1KHUh?=
MOLT-4 M4T4cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPzTWM2OD1|OD64N|kyKM7:TR?= M4LF[XNCVkeURWK=
SW756 NUPDfWxHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIn3c3BKSzVyPUSwMlk{QDVizszN M3rNbHNCVkeURWK=
CAL-72 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLMTWM2OD12Mj6wN{DPxE1? NF;Eb4pUSU6JUlXS
KNS-62 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzoeFZKSzVyPUSyMlYzQTZizszN NGD0UmVUSU6JUlXS
KARPAS-299 NFPHfZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTR|LkOyN|Mh|ryP NGDkcVdUSU6JUlXS
HEL NVPPXZQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\SbmlKSzVyPUS1MlQ3PDZizszN MUTTRW5IWkWU
KP-4 NEe4RpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnZZVNnUUN3ME20Ok44OzZzIN88US=> MkD5V2FPT1KHUh?=
NEC8 NWe2emlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrTTWM2OD12Nz6xOlYyKM7:TR?= NFvBflZUSU6JUlXS
G-402 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv2NVhKSzVyPUS4MlcxOTJizszN MWnTRW5IWkWU

... 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
  • 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)
Water Insoluble
Ethanol '100 mg/mL
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)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=CC=C(C4=CC=CC=C43)OCCN5CCOCC5

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID