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

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. 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

Choose Selective p38 MAPK Inhibitors

Click to view more

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 MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjvXZpKSzVyPUCuN|Q4PjNizszN NFntcIVUSU6JUlXS
DU-145 NIHC[odIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlG2TWM2OD1|LkmzPFEyKM7:TR?= NFvzNXdUSU6JUlXS
GOTO NXTPbHFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\uW2lEPTB;Nj6zPVE3OSEQvF2= NI[1cYpUSU6JUlXS
NCI-H358 M{HPR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojNTWM2OD15LkWzPEDPxE1? NFjIS|lUSU6JUlXS
IST-MES1 Mo\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLhXYJTUUN3ME23Mlk2PjN5IN88US=> NUHvc444W0GQR2LFVi=>
KP-N-YN NFfnR2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnETWM2OD16LkKwNVkh|ryP NGTqTmNUSU6JUlXS
T-24 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH64UmpKSzVyPUiuOFA3PzNizszN NH[yVHhUSU6JUlXS
MPP-89 NIn2XG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1v0WGlEPTB;OD60OlI2OSEQvF2= MXTTRW5IWkWU
NCI-SNU-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nqfGlEPTB;OT6wOlc{QSEQvF2= NYfUdo1wW0GQR2LFVi=>
BFTC-905 NIjscGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vRZmlEPTB;MUCuNVI{OyEQvF2= NVrCNFJmW0GQR2LFVi=>
MS-1 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;4RWlQUUN3ME2xNE45OjN3IN88US=> MmXZV2FPT1KHUh?=
NBsusSR MlrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHlUIhQUUN3ME2xNE45OjN3IN88US=> NHzkOHFUSU6JUlXS
BEN NVrIW2E6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzvTWM2OD1zMz6xNlY1KM7:TR?= MX3TRW5IWkWU
HMV-II NVfVWotwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:y[ZN2UUN3ME2xOE4zOzB7IN88US=> NILid4RUSU6JUlXS
NCI-H1581 NFrzb5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLIT3Z3UUN3ME2xO{4xPDR5IN88US=> NGmzSHZUSU6JUlXS
ES8 NYrEWW1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlWxTWM2OD1zNz6xOlch|ryP NHHmV3BUSU6JUlXS
LC-2-ad MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnGzTWM2OD1zNz60N|Y3KM7:TR?= Mnq1V2FPT1KHUh?=
EW-13 M{HK[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfyTWM2OD1zNz65OVE3KM7:TR?= NHO1XZVUSU6JUlXS
AN3-CA NYHKPWdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\QTGNnUUN3ME2xPE4yKM7:TR?= MYnTRW5IWkWU
DB M4nnUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2CzOGlEPTB;MUiuO|kzOyEQvF2= MlO5V2FPT1KHUh?=
SK-MEL-1 NGjJS|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfJTWM2OD1{MD6zOlg{KM7:TR?= MmXWV2FPT1KHUh?=
CAPAN-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXNcI9FUUN3ME2yNk4yQDh2IN88US=> MoLNV2FPT1KHUh?=
NCI-H2228 Mn3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTzSm9HUUN3ME2yN{43PjZ6IN88US=> NUm4U|hjW0GQR2LFVi=>
HOP-92 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTiOHdYUUN3ME2yOE4{QDN6IN88US=> M1XSZ3NCVkeURWK=
KYSE-270 NHzSN5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3KNo5KSzVyPUK0MlU2PzNizszN MlPCV2FPT1KHUh?=
HCC1806 NHzveoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1yye2lEPTB;MkSuO|c6QSEQvF2= NIC4d4dUSU6JUlXS
HuO-3N1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LUWGlEPTB;MkWuPFE5PSEQvF2= MYDTRW5IWkWU
HOS MojhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGe2UJdKSzVyPUK1MlkzQTJizszN M3XFb3NCVkeURWK=
KYSE-510 NF7xdW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIe0PGRKSzVyPUK2MlE3OTJizszN NWHJTGV7W0GQR2LFVi=>
COLO-741 NUnwdIgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzqd2JJUUN3ME2yOk4{OzJ7IN88US=> NW\sTno{W0GQR2LFVi=>
H-EMC-SS Mn[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHpTWM2OD1{Nj65NlQ2KM7:TR?= NGTITGhUSU6JUlXS
HCC1937 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjISWlKSzVyPUK3MlIzOzhizszN NYrIWY9QW0GQR2LFVi=>
NCI-H2126 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HtUGlEPTB;MkeuN|k4PSEQvF2= MkLhV2FPT1KHUh?=
NCI-H1703 MlnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPuNZNKSzVyPUK4MlA1OTNizszN NIHpb4hUSU6JUlXS
U-2-OS NYi4SI9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTJ6LkW1NVUh|ryP MmrVV2FPT1KHUh?=
DBTRG-05MG NG\vdZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJ6LkW2OVEh|ryP M4jJTnNCVkeURWK=
MHH-ES-1 MkfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXmdHh5UUN3ME2zNU46PDFizszN MUXTRW5IWkWU
HCC1419 MnqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzZTWM2OD1|Mj6xNVE6KM7:TR?= NEDNOIFUSU6JUlXS
HOP-62 MlrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHq2WFBKSzVyPUOyMlI4ODFizszN M1fRW3NCVkeURWK=
AM-38 M3zTSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T0PGlEPTB;M{KuPVk{OSEQvF2= M1XWXnNCVkeURWK=
NCI-H2009 NGDsUo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTN|LkSwNFch|ryP NFTYfJJUSU6JUlXS
EM-2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTN|LkW1NVEh|ryP M{CyXXNCVkeURWK=
SW1116 NInlfWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmr3TWM2OD1|ND60PFM5KM7:TR?= MlPUV2FPT1KHUh?=
SK-N-AS MoqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;4TWM2OD1|NT6wO|E1KM7:TR?= Mn7mV2FPT1KHUh?=
ChaGo-K-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfwTWM2OD1|NT62NFMzKM7:TR?= M3;6dHNCVkeURWK=
RT-112 NV\XPJFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2f0c2lEPTB;M{WuPVg4QSEQvF2= NXKxSZlKW0GQR2LFVi=>
HTC-C3 M4W4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\uXGlEPTB;M{[uNlM2PSEQvF2= M3vqWnNCVkeURWK=
SK-NEP-1 NGrC[ZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\kdGlEPTB;M{[uOlExPiEQvF2= M{naZnNCVkeURWK=
LB831-BLC NXXqXHF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXrc5pKSzVyPUO3MlY2PDFizszN M{\SeHNCVkeURWK=
CTB-1 MojxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NET4PFBKSzVyPUO4MlQ2OTJizszN NInKSllUSU6JUlXS
MOLT-4 M{LBRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPpSmpMUUN3ME2zPE45OzlzIN88US=> NUTvNGVOW0GQR2LFVi=>
SW756 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTRyLkmzPFUh|ryP MV\TRW5IWkWU
CAL-72 NEjkV2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q5OmlEPTB;NEKuNFMh|ryP Mo[5V2FPT1KHUh?=
KNS-62 M1XKcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr4cVdoUUN3ME20Nk43Ojl4IN88US=> NIrHRVZUSU6JUlXS
KARPAS-299 NXHi[JU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTKTWM2OD12Mz6zNlM{KM7:TR?= MW\TRW5IWkWU
HEL MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUiyTVQ6UUN3ME20OU41PjR4IN88US=> NELLU4xUSU6JUlXS
KP-4 NYXncJI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;wTWM2OD12Nj63N|YyKM7:TR?= MXTTRW5IWkWU
NEC8 Mke2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjFc4RkUUN3ME20O{4yPjZzIN88US=> NWW0T4p7W0GQR2LFVi=>
G-402 NUDuSZdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLBTWM2OD12OD63NFEzKM7:TR?= Mo\GV2FPT1KHUh?=

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