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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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 NGLDW3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\pTVdKSzVyPUCuN|Q4PjNizszN M3jBNnNCVkeURWK=
DU-145 MmWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTNwOUO4NVEh|ryP MUnTRW5IWkWU
GOTO MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTLTWM2OD14LkO5NVYyKM7:TR?= M3PUWXNCVkeURWK=
NCI-H358 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rs[mlEPTB;Nz61N|gh|ryP NIGwTHNUSU6JUlXS
IST-MES1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PwcmlEPTB;Nz65OVY{PyEQvF2= MmfJV2FPT1KHUh?=
KP-N-YN MkPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXXUVZEUUN3ME24MlIxOTlizszN MW\TRW5IWkWU
T-24 NFrmWIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRThwNEC2O|Mh|ryP NVrFTJB7W0GQR2LFVi=>
MPP-89 NXLUc5Q1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlS2TWM2OD16LkS2NlUyKM7:TR?= M3rsdnNCVkeURWK=
NCI-SNU-1 NFTjflRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTlwME[3N|kh|ryP NIHqfmpUSU6JUlXS
BFTC-905 M{XjSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfOeGxKSzVyPUGwMlEzOzNizszN MlfIV2FPT1KHUh?=
MS-1 Mme2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHlcZNTUUN3ME2xNE45OjN3IN88US=> MUjTRW5IWkWU
NBsusSR NEXGToZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLiTWM2OD1zMD64NlM2KM7:TR?= MVrTRW5IWkWU
BEN MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fCfmlEPTB;MUOuNVI3PCEQvF2= M1;xVXNCVkeURWK=
HMV-II M3P4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTzc28{UUN3ME2xOE4zOzB7IN88US=> MUHTRW5IWkWU
NCI-H1581 M4Dtd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnQOGFKSzVyPUG3MlA1PDdizszN M{nqeXNCVkeURWK=
ES8 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4W3RWlEPTB;MUeuNVY4KM7:TR?= NIDhXoJUSU6JUlXS
LC-2-ad MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moq3TWM2OD1zNz60N|Y3KM7:TR?= NHzaOYhUSU6JUlXS
EW-13 M2\n[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\pTWM2OD1zNz65OVE3KM7:TR?= M3PNXHNCVkeURWK=
AN3-CA NF3yOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DseGlEPTB;MUiuNUDPxE1? MlL0V2FPT1KHUh?=
DB MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4KzemlEPTB;MUiuO|kzOyEQvF2= NGrPNm9USU6JUlXS
SK-MEL-1 NUHLNYVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPKTWM2OD1{MD6zOlg{KM7:TR?= MVHTRW5IWkWU
CAPAN-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\BcY57UUN3ME2yNk4yQDh2IN88US=> M2PofnNCVkeURWK=
NCI-H2228 NXvON41OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLzUm1KSzVyPUKzMlY3PjhizszN MVHTRW5IWkWU
HOP-92 M2D6dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV6wc2VFUUN3ME2yOE4{QDN6IN88US=> NFn1[5RUSU6JUlXS
KYSE-270 NHrF[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3rT5RKSzVyPUK0MlU2PzNizszN MlfrV2FPT1KHUh?=
HCC1806 NGXHN5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTJ2Lke3PVkh|ryP MkLEV2FPT1KHUh?=
HuO-3N1 M3faPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTJ3LkixPFUh|ryP M3PVfHNCVkeURWK=
HOS NHrRcGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXEcVltUUN3ME2yOU46Ojl{IN88US=> NHO4TIRUSU6JUlXS
KYSE-510 MmSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4O2dmlEPTB;Mk[uNVYyOiEQvF2= MlfQV2FPT1KHUh?=
COLO-741 NFfVRlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnr5TWM2OD1{Nj6zN|I6KM7:TR?= NITwRWxUSU6JUlXS
H-EMC-SS M4PONmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPETWM2OD1{Nj65NlQ2KM7:TR?= M4O2PXNCVkeURWK=
HCC1937 NELwVZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHyTWM2OD1{Nz6yNlM5KM7:TR?= NXH0RnJnW0GQR2LFVi=>
NCI-H2126 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDNOFJKSzVyPUK3MlM6PzVizszN NUXBSIFxW0GQR2LFVi=>
NCI-H1703 M4\RXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLQUFdKSzVyPUK4MlA1OTNizszN MUfTRW5IWkWU
U-2-OS MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfBTWM2OD1{OD61OVE2KM7:TR?= MUjTRW5IWkWU
DBTRG-05MG NVv0ZVU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2ezPWlEPTB;MkiuOVY2OSEQvF2= NGC0bXBUSU6JUlXS
MHH-ES-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfo[FdNUUN3ME2zNU46PDFizszN NIryOG1USU6JUlXS
HCC1419 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTN{LkGxNVkh|ryP NInQRXVUSU6JUlXS
HOP-62 M{izcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHFPYhKSzVyPUOyMlI4ODFizszN M3PvUnNCVkeURWK=
AM-38 MlzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzlXpFFUUN3ME2zNk46QTNzIN88US=> M{mzcnNCVkeURWK=
NCI-H2009 NFHEWFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTN|LkSwNFch|ryP MYnTRW5IWkWU
EM-2 M1r3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTN|LkW1NVEh|ryP MYjTRW5IWkWU
SW1116 M4X4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rzbGlEPTB;M{SuOFg{QCEQvF2= MmWwV2FPT1KHUh?=
SK-N-AS Mn[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LhbGlEPTB;M{WuNFcyPCEQvF2= Mn\MV2FPT1KHUh?=
ChaGo-K-1 M4DTNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\LOYJKSzVyPUO1MlYxOzJizszN M3[3NnNCVkeURWK=
RT-112 MnHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInEV41KSzVyPUO1Mlk5PzlizszN M13HT3NCVkeURWK=
HTC-C3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofYTWM2OD1|Nj6yN|U2KM7:TR?= MWnTRW5IWkWU
SK-NEP-1 NIjBSpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3GxbmlEPTB;M{[uOlExPiEQvF2= MUjTRW5IWkWU
LB831-BLC NXTMUplWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nNdmlEPTB;M{euOlU1OSEQvF2= Mnv3V2FPT1KHUh?=
CTB-1 Ml7mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;zbGlEPTB;M{iuOFUyOiEQvF2= M13hfnNCVkeURWK=
MOLT-4 NUO4VYQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:5W3Q4UUN3ME2zPE45OzlzIN88US=> MULTRW5IWkWU
SW756 M3jpdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33jXmlEPTB;NECuPVM5PSEQvF2= MWfTRW5IWkWU
CAL-72 NXvWZnJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTR{LkCzJO69VQ>? NWO3fXRPW0GQR2LFVi=>
KNS-62 MknmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTR{Lk[yPVYh|ryP MlOyV2FPT1KHUh?=
KARPAS-299 NXLLcoFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7t[5lXUUN3ME20N{4{OjN|IN88US=> MlzMV2FPT1KHUh?=
HEL NFWw[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\UTm81UUN3ME20OU41PjR4IN88US=> M3e3RnNCVkeURWK=
KP-4 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mor4TWM2OD12Nj63N|YyKM7:TR?= MX;TRW5IWkWU
NEC8 NWfMeZlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTR5LkG2OlEh|ryP NFnrVlBUSU6JUlXS
G-402 NFH6V3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3MV4VPUUN3ME20PE44ODF{IN88US=> NW\BOnFEW0GQR2LFVi=>

... 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):
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID