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.

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

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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 M4fPOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPKW4tEUUN3ME2wMlM1PzZ|IN88US=> NXnTUGJ7W0GQR2LFVi=>
DU-145 MnK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTNwOUO4NVEh|ryP NX23PHRJW0GQR2LFVi=>
GOTO M{fDe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr6TWM2OD14LkO5NVYyKM7:TR?= NHvYeotUSU6JUlXS
NCI-H358 M{m4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYj3OlhLUUN3ME23MlU{QCEQvF2= Moj0V2FPT1KHUh?=
IST-MES1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;QOpFKSzVyPUeuPVU3OzdizszN MWrTRW5IWkWU
KP-N-YN NWTofWNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PPS2lEPTB;OD6yNFE6KM7:TR?= MX7TRW5IWkWU
T-24 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rWfWlEPTB;OD60NFY4OyEQvF2= MofSV2FPT1KHUh?=
MPP-89 M{eyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRThwNE[yOVEh|ryP NEHzW3dUSU6JUlXS
NCI-SNU-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXn2ZlNmUUN3ME25MlA3PzN7IN88US=> NYDSWop2W0GQR2LFVi=>
BFTC-905 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DyNmlEPTB;MUCuNVI{OyEQvF2= NXflbHdUW0GQR2LFVi=>
MS-1 NXzpPGNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTFyLkiyN|Uh|ryP MUTTRW5IWkWU
NBsusSR NIK4XIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO2cpBKSzVyPUGwMlgzOzVizszN M{j6UXNCVkeURWK=
BEN M3jXWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPJN2lKSzVyPUGzMlEzPjRizszN NEW5NVFUSU6JUlXS
HMV-II M4S3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DHVGlEPTB;MUSuNlMxQSEQvF2= M{f4Z3NCVkeURWK=
NCI-H1581 MkjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDidmVFUUN3ME2xO{4xPDR5IN88US=> NF:xWHRUSU6JUlXS
ES8 MkHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[xWlNxUUN3ME2xO{4yPjdizszN MmnrV2FPT1KHUh?=
LC-2-ad NHLibFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;kZ2lEPTB;MUeuOFM3PiEQvF2= MofrV2FPT1KHUh?=
EW-13 MnSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTF5Lkm1NVYh|ryP NIPOTmFUSU6JUlXS
AN3-CA MmnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nUW2lEPTB;MUiuNUDPxE1? NGnsTHVUSU6JUlXS
DB NEHOc29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFL2fJhKSzVyPUG4Mlc6OjNizszN NIPCfJdUSU6JUlXS
SK-MEL-1 MnvrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\Ic5hKSzVyPUKwMlM3QDNizszN NXTZSGU4W0GQR2LFVi=>
CAPAN-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPYdJRKSzVyPUKyMlE5QDRizszN NV3tTllPW0GQR2LFVi=>
NCI-H2228 NILWTVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnj6TWM2OD1{Mz62OlY5KM7:TR?= MVXTRW5IWkWU
HOP-92 M4fqfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX0WnVKSzVyPUK0MlM5OzhizszN NF;TW5NUSU6JUlXS
KYSE-270 NWr1UGpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTJ2LkW1O|Mh|ryP Mk\oV2FPT1KHUh?=
HCC1806 MorrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTJ2Lke3PVkh|ryP NHvETHBUSU6JUlXS
HuO-3N1 MofiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXIdlFKSzVyPUK1MlgyQDVizszN MlPSV2FPT1KHUh?=
HOS NYPjPVJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jiSGlEPTB;MkWuPVI6OiEQvF2= M{PvS3NCVkeURWK=
KYSE-510 NI\Ebm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ4LkG2NVIh|ryP NYXmToxPW0GQR2LFVi=>
COLO-741 NIrabpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDQ[HpKSzVyPUK2MlM{OjlizszN MVLTRW5IWkWU
H-EMC-SS NYL2[49pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjPWXhKSzVyPUK2MlkzPDVizszN MmTOV2FPT1KHUh?=
HCC1937 NYTSOmNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrZR4JuUUN3ME2yO{4zOjN6IN88US=> MXLTRW5IWkWU
NCI-H2126 NGf0[GxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDKUnk3UUN3ME2yO{4{QTd3IN88US=> MnHrV2FPT1KHUh?=
NCI-H1703 M3jKVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJ6LkC0NVMh|ryP M1:2S3NCVkeURWK=
U-2-OS NYTTSVdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzvXlk{UUN3ME2yPE42PTF3IN88US=> MkC3V2FPT1KHUh?=
DBTRG-05MG M1[yPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3r0O2lEPTB;MkiuOVY2OSEQvF2= NFrLU3pUSU6JUlXS
MHH-ES-1 NULBbXEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWL4PIFUUUN3ME2zNU46PDFizszN M4PTTHNCVkeURWK=
HCC1419 Mn;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWns[IxFUUN3ME2zNk4yOTF7IN88US=> MmjTV2FPT1KHUh?=
HOP-62 NIHQSoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj2bHJEUUN3ME2zNk4zPzBzIN88US=> Mlu0V2FPT1KHUh?=
AM-38 M{jLWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3O0OmlEPTB;M{KuPVk{OSEQvF2= MmjhV2FPT1KHUh?=
NCI-H2009 NEj3XnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTN|LkSwNFch|ryP M3iydnNCVkeURWK=
EM-2 Mk\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjWd4dKSzVyPUOzMlU2OTFizszN MoXTV2FPT1KHUh?=
SW1116 NH[1dnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN2LkS4N|gh|ryP NVfBTnA{W0GQR2LFVi=>
SK-N-AS MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnRdZV{UUN3ME2zOU4xPzF2IN88US=> MnznV2FPT1KHUh?=
ChaGo-K-1 M1\jeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LPdWlEPTB;M{WuOlA{OiEQvF2= NWjtSFNyW0GQR2LFVi=>
RT-112 NV\6[49NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzhW2xKSzVyPUO1Mlk5PzlizszN NGX5e4FUSU6JUlXS
HTC-C3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HKPGlEPTB;M{[uNlM2PSEQvF2= NWLVZWlPW0GQR2LFVi=>
SK-NEP-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDEN4hKSzVyPUO2MlYyODZizszN Ml3YV2FPT1KHUh?=
LB831-BLC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTyNlFKSzVyPUO3MlY2PDFizszN MlLZV2FPT1KHUh?=
CTB-1 M4PQfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DWS2lEPTB;M{iuOFUyOiEQvF2= NFOxR5BUSU6JUlXS
MOLT-4 Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHO0TJRKSzVyPUO4Mlg{QTFizszN MUHTRW5IWkWU
SW756 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmP1TWM2OD12MD65N|g2KM7:TR?= MYTTRW5IWkWU
CAL-72 M{G2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1n2ZmlEPTB;NEKuNFMh|ryP M4qzVnNCVkeURWK=
KNS-62 NWfxbJg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTR{Lk[yPVYh|ryP MnnNV2FPT1KHUh?=
KARPAS-299 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnL0TWM2OD12Mz6zNlM{KM7:TR?= MUfTRW5IWkWU
HEL NHq0TJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknpTWM2OD12NT60OlQ3KM7:TR?= M2izfnNCVkeURWK=
KP-4 NWrnVnp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnYVpYzUUN3ME20Ok44OzZzIN88US=> NX;xTmNiW0GQR2LFVi=>
NEC8 MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3DcoZKSzVyPUS3MlE3PjFizszN NG\rS2dUSU6JUlXS
G-402 NV;kSYd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTaTWM2OD12OD63NFEzKM7:TR?= MmrUV2FPT1KHUh?=

... 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

p38 MAPK Signaling Pathway Map

p38 MAPK Inhibitors with Unique Features

Related p38 MAPK Products

Tags: buy Doramapimod (BIRB 796) | Doramapimod (BIRB 796) supplier | purchase Doramapimod (BIRB 796) | Doramapimod (BIRB 796) cost | Doramapimod (BIRB 796) manufacturer | order Doramapimod (BIRB 796) | Doramapimod (BIRB 796) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID