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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In DMSO USD 294 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. Doramapimod (BIRB 796) 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. Doramapimod (BIRB 796) 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. Doramapimod (BIRB 796) 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. Doramapimod (BIRB 796) purchased from Selleck.

  • Doramapimod (BIRB 796) purchased from Selleck.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

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 NHT4UYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnFTWM2OD1yLkO0O|Y{KM7:TR?= NXfRRo82W0GQR2LFVi=>
DU-145 M3nse2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnXbFI3UUN3ME2zMlk{QDFzIN88US=> NYP4U2NqW0GQR2LFVi=>
GOTO MmTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfJUnRKSzVyPU[uN|kyPjFizszN NWTzN25EW0GQR2LFVi=>
NCI-H358 MmTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTdwNUO4JO69VQ>? M4nKVHNCVkeURWK=
IST-MES1 NFrucYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIe4SlZKSzVyPUeuPVU3OzdizszN MV7TRW5IWkWU
KP-N-YN MoDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRThwMkCxPUDPxE1? MojwV2FPT1KHUh?=
T-24 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRThwNEC2O|Mh|ryP MmPzV2FPT1KHUh?=
MPP-89 NIrSS|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NViwR3ZpUUN3ME24MlQ3OjVzIN88US=> MoG3V2FPT1KHUh?=
NCI-SNU-1 M2\hfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLXXFl7UUN3ME25MlA3PzN7IN88US=> MoLwV2FPT1KHUh?=
BFTC-905 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;C[GtKSzVyPUGwMlEzOzNizszN MYLTRW5IWkWU
MS-1 NWXHVpBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf3Vlc1UUN3ME2xNE45OjN3IN88US=> M1PwSXNCVkeURWK=
NBsusSR M2HhNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTFyLkiyN|Uh|ryP MlvFV2FPT1KHUh?=
BEN NXnhN3JmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTF|LkGyOlQh|ryP NEThU4hUSU6JUlXS
HMV-II NXHJOJBJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPjW4U6UUN3ME2xOE4zOzB7IN88US=> MVrTRW5IWkWU
NCI-H1581 NHXwcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zzTmlEPTB;MUeuNFQ1PyEQvF2= MXfTRW5IWkWU
ES8 NH6yN5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmS0TWM2OD1zNz6xOlch|ryP M3HRd3NCVkeURWK=
LC-2-ad MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlL0TWM2OD1zNz60N|Y3KM7:TR?= MVXTRW5IWkWU
EW-13 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\3cGlEPTB;MUeuPVUyPiEQvF2= MWfTRW5IWkWU
AN3-CA NVzsNpJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTF6LkGg{txO NXO1cXZmW0GQR2LFVi=>
DB MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnmXItNUUN3ME2xPE44QTJ|IN88US=> NHS3WFFUSU6JUlXS
SK-MEL-1 M4DWVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEW4TnpKSzVyPUKwMlM3QDNizszN NV\Kd3AyW0GQR2LFVi=>
CAPAN-1 M1u5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTJ{LkG4PFQh|ryP MXHTRW5IWkWU
NCI-H2228 M4jhd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPZTWM2OD1{Mz62OlY5KM7:TR?= NXLhOWlQW0GQR2LFVi=>
HOP-92 NXHR[GplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTJ2LkO4N|gh|ryP MYnTRW5IWkWU
KYSE-270 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPDTWM2OD1{ND61OVc{KM7:TR?= MkXVV2FPT1KHUh?=
HCC1806 NUG3d5EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfqSolYUUN3ME2yOE44Pzl7IN88US=> MojBV2FPT1KHUh?=
HuO-3N1 M2\EbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnqZ2FLUUN3ME2yOU45OTh3IN88US=> MlfyV2FPT1KHUh?=
HOS MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTJ3LkmyPVIh|ryP NFiyeGtUSU6JUlXS
KYSE-510 NIDQTldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HwSWlEPTB;Mk[uNVYyOiEQvF2= MmDuV2FPT1KHUh?=
COLO-741 MkHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTJ4LkOzNlkh|ryP NG\rRmdUSU6JUlXS
H-EMC-SS MnTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILIelJKSzVyPUK2MlkzPDVizszN NWPteXRWW0GQR2LFVi=>
HCC1937 M4HvOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHyXHpKSzVyPUK3MlIzOzhizszN MmHlV2FPT1KHUh?=
NCI-H2126 M{\rZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fqUGlEPTB;MkeuN|k4PSEQvF2= MUfTRW5IWkWU
NCI-H1703 M2X3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfUUW5RUUN3ME2yPE4xPDF|IN88US=> M4qxb3NCVkeURWK=
U-2-OS M4TWbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTJ6LkW1NVUh|ryP MVPTRW5IWkWU
DBTRG-05MG NW\lPFk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTaV4hKSzVyPUK4MlU3PTFizszN M1\tSnNCVkeURWK=
MHH-ES-1 NWHVZZBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknlTWM2OD1|MT65OFEh|ryP MoDDV2FPT1KHUh?=
HCC1419 M{XXXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTN{LkGxNVkh|ryP MnjBV2FPT1KHUh?=
HOP-62 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoCwTWM2OD1|Mj6yO|AyKM7:TR?= M3nIdXNCVkeURWK=
AM-38 MmHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C0R2lEPTB;M{KuPVk{OSEQvF2= MmrKV2FPT1KHUh?=
NCI-H2009 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTN|LkSwNFch|ryP MXvTRW5IWkWU
EM-2 NH;wUJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HEV2lEPTB;M{OuOVUyOSEQvF2= M4LZV3NCVkeURWK=
SW1116 M3K0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr3PG1NUUN3ME2zOE41QDN6IN88US=> NH6zVlBUSU6JUlXS
SK-N-AS MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7zUFlxUUN3ME2zOU4xPzF2IN88US=> NVyycZNDW0GQR2LFVi=>
ChaGo-K-1 M4qxOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj2TWM2OD1|NT62NFMzKM7:TR?= M1r1d3NCVkeURWK=
RT-112 MlLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTN3Lkm4O|kh|ryP MVTTRW5IWkWU
HTC-C3 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTFVJFKSzVyPUO2MlI{PTVizszN MknhV2FPT1KHUh?=
SK-NEP-1 NEOzVINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3FeGJ3UUN3ME2zOk43OTB4IN88US=> NXLvd3BVW0GQR2LFVi=>
LB831-BLC MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHSTWM2OD1|Nz62OVQyKM7:TR?= MWDTRW5IWkWU
CTB-1 MkTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe5TZVbUUN3ME2zPE41PTF{IN88US=> MVvTRW5IWkWU
MOLT-4 NVTjT4E1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[2TWM2OD1|OD64N|kyKM7:TR?= MoP6V2FPT1KHUh?=
SW756 NW\kdXdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTRyLkmzPFUh|ryP NH;ofYZUSU6JUlXS
CAL-72 NUjCPZBNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M376eGlEPTB;NEKuNFMh|ryP NV3M[ZpqW0GQR2LFVi=>
KNS-62 NYTucmtIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTvTWM2OD12Mj62Nlk3KM7:TR?= NEGyTWJUSU6JUlXS
KARPAS-299 NV;BSVJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zUSGlEPTB;NEOuN|I{OyEQvF2= MlLKV2FPT1KHUh?=
HEL MnziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m5OWlEPTB;NEWuOFY1PiEQvF2= NUnlRpA1W0GQR2LFVi=>
KP-4 M2PDdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Czc2lEPTB;NE[uO|M3OSEQvF2= NWrtcXVqW0GQR2LFVi=>
NEC8 NFL1cINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnsd5lKSzVyPUS3MlE3PjFizszN NXq0TY1oW0GQR2LFVi=>
G-402 NVLtXGZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXzTWM2OD12OD63NFEzKM7:TR?= M4PXPXNCVkeURWK=

... 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 100 mg/mL (189.51 mM)
Ethanol 100 mg/mL (189.51 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID