Doramapimod (BIRB 796)

For research use only.

Catalog No.S1574

62 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 62 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 NETNO5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\ETWM2OD1yLkO0O|Y{KM7:TR?= M3fH[3NCVkeURWK=
DU-145 M{PrV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;sTWM2OD1|LkmzPFEyKM7:TR?= MoPxV2FPT1KHUh?=
GOTO M1PHV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTZwM{mxOlEh|ryP MXvTRW5IWkWU
NCI-H358 M2Lhfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4GxS2lEPTB;Nz61N|gh|ryP MWrTRW5IWkWU
IST-MES1 MmSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LOWmlEPTB;Nz65OVY{PyEQvF2= NEjYcWdUSU6JUlXS
KP-N-YN NYKzZnNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3xTWM2OD16LkKwNVkh|ryP MofNV2FPT1KHUh?=
T-24 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoiwTWM2OD16LkSwOlc{KM7:TR?= MYLTRW5IWkWU
MPP-89 NUHPN2JmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTRTWM2OD16LkS2NlUyKM7:TR?= M{TWe3NCVkeURWK=
NCI-SNU-1 NFHk[4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nJUGlEPTB;OT6wOlc{QSEQvF2= NGnONXJUSU6JUlXS
BFTC-905 NXOxNplOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLETIlKSzVyPUGwMlEzOzNizszN NUfoeYZCW0GQR2LFVi=>
MS-1 NEXXbJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;xcG9KSzVyPUGwMlgzOzVizszN MVnTRW5IWkWU
NBsusSR NGL4fWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjpZYpKSzVyPUGwMlgzOzVizszN NFrHeW5USU6JUlXS
BEN NWHKcoJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDnTWM2OD1zMz6xNlY1KM7:TR?= MWPTRW5IWkWU
HMV-II NHHsW|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTF2LkKzNFkh|ryP NYfTb4J7W0GQR2LFVi=>
NCI-H1581 MlzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF5LkC0OFch|ryP MnvOV2FPT1KHUh?=
ES8 M3\OeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:yZ3lKSzVyPUG3MlE3PyEQvF2= NUDkWJFxW0GQR2LFVi=>
LC-2-ad NUGw[lh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHCepJKSzVyPUG3MlQ{PjZizszN MlHpV2FPT1KHUh?=
EW-13 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7mW4hKSzVyPUG3Mlk2OTZizszN NIPQTYZUSU6JUlXS
AN3-CA NV:zUWxpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLwU|JKSzVyPUG4MlEh|ryP NWDCSm1RW0GQR2LFVi=>
DB MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXy[WhbUUN3ME2xPE44QTJ|IN88US=> MlTrV2FPT1KHUh?=
SK-MEL-1 NIPEb2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoD3TWM2OD1{MD6zOlg{KM7:TR?= NVT0OWdWW0GQR2LFVi=>
CAPAN-1 M4G2emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;kVYRKSzVyPUKyMlE5QDRizszN NWPqUY1lW0GQR2LFVi=>
NCI-H2228 Mn7TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzaOnpKSzVyPUKzMlY3PjhizszN MlraV2FPT1KHUh?=
HOP-92 NXe0XlI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTJ2LkO4N|gh|ryP NEPqRZlUSU6JUlXS
KYSE-270 NXXjV5RQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJ2LkW1O|Mh|ryP NWLSRYFKW0GQR2LFVi=>
HCC1806 MkLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzPd2hoUUN3ME2yOE44Pzl7IN88US=> MWHTRW5IWkWU
HuO-3N1 NWixbHkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e0WmlEPTB;MkWuPFE5PSEQvF2= NIPOfFFUSU6JUlXS
HOS MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH75NotKSzVyPUK1MlkzQTJizszN NF3TUWtUSU6JUlXS
KYSE-510 NE\ZVWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJ4LkG2NVIh|ryP NUSzR4h{W0GQR2LFVi=>
COLO-741 MmOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3WxfmlEPTB;Mk[uN|MzQSEQvF2= MmTtV2FPT1KHUh?=
H-EMC-SS NYGxfox7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPnVpdLUUN3ME2yOk46OjR3IN88US=> NEfue2hUSU6JUlXS
HCC1937 M2[5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorkTWM2OD1{Nz6yNlM5KM7:TR?= MoX2V2FPT1KHUh?=
NCI-H2126 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjWbpFMUUN3ME2yO{4{QTd3IN88US=> NUjSO|lnW0GQR2LFVi=>
NCI-H1703 M{T6Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrUTWM2OD1{OD6wOFE{KM7:TR?= NWLqbW83W0GQR2LFVi=>
U-2-OS NELrRYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HVPGlEPTB;MkiuOVUyPSEQvF2= M1m2[HNCVkeURWK=
DBTRG-05MG NXnFNZVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkSzTWM2OD1{OD61OlUyKM7:TR?= NVjqZ4ZRW0GQR2LFVi=>
MHH-ES-1 NFTkTG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTNzLkm0NUDPxE1? M3i5XHNCVkeURWK=
HCC1419 NYLudphDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1uyO2lEPTB;M{KuNVEyQSEQvF2= M4\KbXNCVkeURWK=
HOP-62 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTN{LkK3NFEh|ryP MnXUV2FPT1KHUh?=
AM-38 NHvWeZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrqWHB{UUN3ME2zNk46QTNzIN88US=> M4G5dnNCVkeURWK=
NCI-H2009 Mn:wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnLOVVKSzVyPUOzMlQxODdizszN M2ToXXNCVkeURWK=
EM-2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1T6cWlEPTB;M{OuOVUyOSEQvF2= M{fXd3NCVkeURWK=
SW1116 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3r6dWlEPTB;M{SuOFg{QCEQvF2= MX;TRW5IWkWU
SK-N-AS MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTN3LkC3NVQh|ryP MXjTRW5IWkWU
ChaGo-K-1 M3;vXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LhdmlEPTB;M{WuOlA{OiEQvF2= MnXGV2FPT1KHUh?=
RT-112 MlLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjvc|RKSzVyPUO1Mlk5PzlizszN NWXGfoQyW0GQR2LFVi=>
HTC-C3 NELEfFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkiyTWM2OD1|Nj6yN|U2KM7:TR?= Ml;GV2FPT1KHUh?=
SK-NEP-1 MnzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTN4Lk[xNFYh|ryP M{DxWnNCVkeURWK=
LB831-BLC MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWX3WpZDUUN3ME2zO{43PTRzIN88US=> MkOxV2FPT1KHUh?=
CTB-1 MmXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1mzdmlEPTB;M{iuOFUyOiEQvF2= M2GxNHNCVkeURWK=
MOLT-4 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD6UGduUUN3ME2zPE45OzlzIN88US=> NUjmOWtXW0GQR2LFVi=>
SW756 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX6zWJZnUUN3ME20NE46Ozh3IN88US=> M17YXnNCVkeURWK=
CAL-72 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHkPGdlUUN3ME20Nk4xOyEQvF2= NFLYSm9USU6JUlXS
KNS-62 MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTR{Lk[yPVYh|ryP NUXKTIpHW0GQR2LFVi=>
KARPAS-299 NEX2bJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nSfmlEPTB;NEOuN|I{OyEQvF2= NEf0eoJUSU6JUlXS
HEL NVvYW|loT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvzN29kUUN3ME20OU41PjR4IN88US=> NGPiNlRUSU6JUlXS
KP-4 M4Pz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXFcoV{UUN3ME20Ok44OzZzIN88US=> NUPqOWxOW0GQR2LFVi=>
NEC8 NVXqW4hXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\1OnRYUUN3ME20O{4yPjZzIN88US=> MlKwV2FPT1KHUh?=
G-402 MlvjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfGNnQ{UUN3ME20PE44ODF{IN88US=> MkCwV2FPT1KHUh?=

... 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)[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