BIRB 796 (Doramapimod)

Catalog No.S1574

BIRB 796 (Doramapimod) Chemical Structure

Molecular Weight(MW): 527.66

BIRB 796 (Doramapimod) 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.

Size Price Stock Quantity  
In DMSO USD 294 In stock
USD 147 In stock
USD 270 In stock
USD 470 In stock

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5 Customer Reviews

  • Lympho-myeloid potential assessed by FACS analysis of human CD19 (B-lymphoid cells) and CD33/CD15 (myeloid cells) in bone marrow of NSG recipient mice, 17 weeks after transplantation. Each plot represents an animal from the experiment presented in panel.

    Blood 2012 119(26), 6255-8. BIRB 796 (Doramapimod) purchased from Selleck.

    A p38α/ERK crosstalk exists in CRC cells and tissues. Use of a structurally and functionally different p38α inhibitor (BIRB-796) confirms ERK1/2 phospho-activation. Using BIRB-796 for up to 72 h triggers MEK-ERK1/2 signaling in HT-29 cells.

    Cancer Lett 2012 324(1), 98-108. BIRB 796 (Doramapimod) purchased from Selleck.

  • Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.

    Int J Cancer 2014 134(3), 575-86. BIRB 796 (Doramapimod) purchased from Selleck.

    Inhibition of p38 MAPK activity prevents induction of autophagy by glucose. NIH 3T3 cells were incubated in KH medium without glucose in the presence of the p38 MAPK inhibitor BIRB796 (50 nM, middle panels). After 30 min, glucose (10 mM) and lysosomal inhibitors were added to the indicated samples and cells were further incubated for 2 h. Cell lysates were collected and processed for SDS/PAGE. LC3 levels were detected and actin served as a loading control. The values shown in the histograms represent means盨.D. from three independent experiments with the LC3-II levels normalized to actin and expressed as a percentage of the values of KH medium without glucose. *P<0.05. Glc, glucose; w/o, without.

    Biochem J 2014 449(2), 497-506. BIRB 796 (Doramapimod) purchased from Selleck.

  • BIRB 796 (Doramapimod) purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description BIRB 796 (Doramapimod) 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 MkP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTBwM{S3OlMh|ryP MmrqV2FPT1KHUh?=
DU-145 MmC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\3WZRJUUN3ME2zMlk{QDFzIN88US=> MmrWV2FPT1KHUh?=
GOTO MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;LTWM2OD14LkO5NVYyKM7:TR?= NWDEUm41W0GQR2LFVi=>
NCI-H358 NVvkWVM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXaTWM2OD15LkWzPEDPxE1? MVnTRW5IWkWU
IST-MES1 M3n4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYmwbYFRUUN3ME23Mlk2PjN5IN88US=> NH3YNFhUSU6JUlXS
KP-N-YN M{Djb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlixTWM2OD16LkKwNVkh|ryP NFHjXlRUSU6JUlXS
T-24 NY\FcFVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnISmVKSzVyPUiuOFA3PzNizszN MXzTRW5IWkWU
MPP-89 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVO2Ull7UUN3ME24MlQ3OjVzIN88US=> MXrTRW5IWkWU
NCI-SNU-1 NFT3PVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTYTWM2OD17LkC2O|M6KM7:TR?= NUPFXIFxW0GQR2LFVi=>
BFTC-905 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFyLkGyN|Mh|ryP NHnjRnBUSU6JUlXS
MS-1 NWTob|lpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonJTWM2OD1zMD64NlM2KM7:TR?= NEG5eVJUSU6JUlXS
NBsusSR M{fBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M124bGlEPTB;MUCuPFI{PSEQvF2= M3;6XXNCVkeURWK=
BEN MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrTe456UUN3ME2xN{4yOjZ2IN88US=> NFHFZ5RUSU6JUlXS
HMV-II NXzuUWhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7ib49uUUN3ME2xOE4zOzB7IN88US=> NGXoW5dUSU6JUlXS
NCI-H1581 M{KyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nEdmlEPTB;MUeuNFQ1PyEQvF2= NHLYN2NUSU6JUlXS
ES8 M3XFb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFriSmNKSzVyPUG3MlE3PyEQvF2= Ml\JV2FPT1KHUh?=
LC-2-ad NUX6UIc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjWd5NKSzVyPUG3MlQ{PjZizszN M3PXR3NCVkeURWK=
EW-13 M1vGb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUf1bHhiUUN3ME2xO{46PTF4IN88US=> NVezVlc3W0GQR2LFVi=>
AN3-CA MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfQXoZKSzVyPUG4MlEh|ryP NYG4UlV5W0GQR2LFVi=>
DB NU\YeoFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{noW2lEPTB;MUiuO|kzOyEQvF2= MVrTRW5IWkWU
SK-MEL-1 M{npOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFro[ZZKSzVyPUKwMlM3QDNizszN MkD4V2FPT1KHUh?=
CAPAN-1 NWTtRnYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLpfWpxUUN3ME2yNk4yQDh2IN88US=> MUPTRW5IWkWU
NCI-H2228 MlTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJ|Lk[2Olgh|ryP MoXmV2FPT1KHUh?=
HOP-92 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfW[WZKSzVyPUK0MlM5OzhizszN MnXLV2FPT1KHUh?=
KYSE-270 NH\IcnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoT1TWM2OD1{ND61OVc{KM7:TR?= Ml;iV2FPT1KHUh?=
HCC1806 Mn6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTJ2Lke3PVkh|ryP M1jBUnNCVkeURWK=
HuO-3N1 NG\XXJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXNTWM2OD1{NT64NVg2KM7:TR?= M{P2VXNCVkeURWK=
HOS NXy1dnh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHzTWM2OD1{NT65NlkzKM7:TR?= MkC0V2FPT1KHUh?=
KYSE-510 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLiV5ZKSzVyPUK2MlE3OTJizszN NWTpTVQ1W0GQR2LFVi=>
COLO-741 NXmzc3I3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTJ4LkOzNlkh|ryP Mm[xV2FPT1KHUh?=
H-EMC-SS MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L6XWlEPTB;Mk[uPVI1PSEQvF2= NFvqNVRUSU6JUlXS
HCC1937 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJ5LkKyN|gh|ryP NGXtfWtUSU6JUlXS
NCI-H2126 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnBTWM2OD1{Nz6zPVc2KM7:TR?= MXXTRW5IWkWU
NCI-H1703 NXT2bIYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3hd4RKSzVyPUK4MlA1OTNizszN MUfTRW5IWkWU
U-2-OS MljFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLFTWM2OD1{OD61OVE2KM7:TR?= NV;ob4FSW0GQR2LFVi=>
DBTRG-05MG M2qyR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzxdlZuUUN3ME2yPE42PjVzIN88US=> NFPocZNUSU6JUlXS
MHH-ES-1 NHXhcFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzJTWM2OD1|MT65OFEh|ryP MoXtV2FPT1KHUh?=
HCC1419 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTN{LkGxNVkh|ryP Mmf4V2FPT1KHUh?=
HOP-62 Mn[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTN{LkK3NFEh|ryP M1;hRnNCVkeURWK=
AM-38 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW[ye5B6UUN3ME2zNk46QTNzIN88US=> MoK0V2FPT1KHUh?=
NCI-H2009 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXywZXp{UUN3ME2zN{41ODB5IN88US=> NWjJ[|hHW0GQR2LFVi=>
EM-2 MlfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTN|LkW1NVEh|ryP NFThOXlUSU6JUlXS
SW1116 MnXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;wTWM2OD1|ND60PFM5KM7:TR?= NGLQR4ZUSU6JUlXS
SK-N-AS MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTLTWM2OD1|NT6wO|E1KM7:TR?= M1Tpd3NCVkeURWK=
ChaGo-K-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3rWlhFUUN3ME2zOU43ODN{IN88US=> M3jF[HNCVkeURWK=
RT-112 NGTGZVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3tTXFKSzVyPUO1Mlk5PzlizszN M2CwSHNCVkeURWK=
HTC-C3 M3\DVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;2TWM2OD1|Nj6yN|U2KM7:TR?= MWjTRW5IWkWU
SK-NEP-1 MlvtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1K2Z2lEPTB;M{[uOlExPiEQvF2= MkDPV2FPT1KHUh?=
LB831-BLC NIOxeGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrNTGRKSzVyPUO3MlY2PDFizszN MX3TRW5IWkWU
CTB-1 NFTM[FFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTN6LkS1NVIh|ryP NEXNWHFUSU6JUlXS
MOLT-4 NXjJNG85T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnr5TWM2OD1|OD64N|kyKM7:TR?= MWHTRW5IWkWU
SW756 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[5TWM2OD12MD65N|g2KM7:TR?= NYntcVl1W0GQR2LFVi=>
CAL-72 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TWTmlEPTB;NEKuNFMh|ryP MYLTRW5IWkWU
KNS-62 NX3mdJZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELtNmtKSzVyPUSyMlYzQTZizszN NFe1OlhUSU6JUlXS
KARPAS-299 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17nV2lEPTB;NEOuN|I{OyEQvF2= M1joNnNCVkeURWK=
HEL NHr0UGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\6TWM2OD12NT60OlQ3KM7:TR?= NHr3N4VUSU6JUlXS
KP-4 NETvRXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIThNW9KSzVyPUS2Mlc{PjFizszN MW\TRW5IWkWU
NEC8 MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHkTWM2OD12Nz6xOlYyKM7:TR?= NYLwdHd2W0GQR2LFVi=>
G-402 M{\BdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn4PItKSzVyPUS4MlcxOTJizszN NUHHNGM{W0GQR2LFVi=>

... 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 106 mg/mL (200.88 mM)
Ethanol 106 mg/mL (200.88 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2
NCT02209805 Completed Healthy Boehringer Ingelheim January 2001 Phase 1

Tech Support

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID