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.

Cited by 32 Publications

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 MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXre|hyUUN3ME2wMlM1PzZ|IN88US=> MmjzV2FPT1KHUh?=
DU-145 NELXPJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zLRWlEPTB;Mz65N|gyOSEQvF2= M1ToTHNCVkeURWK=
GOTO M2ix[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTZwM{mxOlEh|ryP MUDTRW5IWkWU
NCI-H358 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\nS2NEUUN3ME23MlU{QCEQvF2= NFi5VmRUSU6JUlXS
IST-MES1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTdwOUW2N|ch|ryP M3;qXXNCVkeURWK=
KP-N-YN NWnJW|VZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRThwMkCxPUDPxE1? MVnTRW5IWkWU
T-24 NWXH[IZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLUTWM2OD16LkSwOlc{KM7:TR?= Mk\XV2FPT1KHUh?=
MPP-89 M3f3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWG4c5VQUUN3ME24MlQ3OjVzIN88US=> MUnTRW5IWkWU
NCI-SNU-1 NHrBXYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTlwME[3N|kh|ryP Mn;HV2FPT1KHUh?=
BFTC-905 Moq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3lVXRzUUN3ME2xNE4yOjN|IN88US=> M4\XS3NCVkeURWK=
MS-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFyLkiyN|Uh|ryP M331SXNCVkeURWK=
NBsusSR NVTMZVZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTFyLkiyN|Uh|ryP MUDTRW5IWkWU
BEN M{XyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{CwdGlEPTB;MUOuNVI3PCEQvF2= M4L1WnNCVkeURWK=
HMV-II M4PDd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrVXnVKSzVyPUG0MlI{ODlizszN NYf6cIY3W0GQR2LFVi=>
NCI-H1581 NEXmUYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLvc4lKSzVyPUG3MlA1PDdizszN NUK5R4t5W0GQR2LFVi=>
ES8 NH[xbXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHYZWJ7UUN3ME2xO{4yPjdizszN MkDtV2FPT1KHUh?=
LC-2-ad MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF5LkSzOlYh|ryP MmjoV2FPT1KHUh?=
EW-13 Mni5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLyUJZKSzVyPUG3Mlk2OTZizszN NHfPbHZUSU6JUlXS
AN3-CA MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\nXWdtUUN3ME2xPE4yKM7:TR?= NGfXOnpUSU6JUlXS
DB Mln6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLwTWM2OD1zOD63PVI{KM7:TR?= MYPTRW5IWkWU
SK-MEL-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrVTWM2OD1{MD6zOlg{KM7:TR?= MoPhV2FPT1KHUh?=
CAPAN-1 M1LYZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XxT2lEPTB;MkKuNVg5PCEQvF2= M2XiWXNCVkeURWK=
NCI-H2228 NIfK[ZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJ|Lk[2Olgh|ryP NITz[JlUSU6JUlXS
HOP-92 M{HVPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\ZV2lEPTB;MkSuN|g{QCEQvF2= NIDyS4dUSU6JUlXS
KYSE-270 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJ2LkW1O|Mh|ryP MULTRW5IWkWU
HCC1806 NXXLSXBJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoL3TWM2OD1{ND63O|k6KM7:TR?= Mn3SV2FPT1KHUh?=
HuO-3N1 M4XlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1W0XGlEPTB;MkWuPFE5PSEQvF2= MmHyV2FPT1KHUh?=
HOS M3L5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\QcmlEPTB;MkWuPVI6OiEQvF2= Ml\NV2FPT1KHUh?=
KYSE-510 M37xZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHznZ3lKSzVyPUK2MlE3OTJizszN M4rTNHNCVkeURWK=
COLO-741 NFLi[2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJ4LkOzNlkh|ryP Mo\XV2FPT1KHUh?=
H-EMC-SS NWXYXlg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7pO2ZuUUN3ME2yOk46OjR3IN88US=> M{TYVnNCVkeURWK=
HCC1937 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPFbGFGUUN3ME2yO{4zOjN6IN88US=> MVrTRW5IWkWU
NCI-H2126 NVO4VIZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXDTWM2OD1{Nz6zPVc2KM7:TR?= MY\TRW5IWkWU
NCI-H1703 NGLRdWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluzTWM2OD1{OD6wOFE{KM7:TR?= MmmzV2FPT1KHUh?=
U-2-OS Ml\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3ZdnlKSzVyPUK4MlU2OTVizszN M1ezXHNCVkeURWK=
DBTRG-05MG NH30fVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HCSGlEPTB;MkiuOVY2OSEQvF2= M3fubnNCVkeURWK=
MHH-ES-1 MoT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDofm1KSzVyPUOxMlk1OSEQvF2= NVyye4k4W0GQR2LFVi=>
HCC1419 NWnoSYdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLS[mt{UUN3ME2zNk4yOTF7IN88US=> MlrwV2FPT1KHUh?=
HOP-62 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTN{LkK3NFEh|ryP MofYV2FPT1KHUh?=
AM-38 MkHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfXTWM2OD1|Mj65PVMyKM7:TR?= M{DMenNCVkeURWK=
NCI-H2009 NEPPb41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLubGpnUUN3ME2zN{41ODB5IN88US=> MmHCV2FPT1KHUh?=
EM-2 NU\pWHUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnydFJDUUN3ME2zN{42PTFzIN88US=> MXnTRW5IWkWU
SW1116 Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoC2TWM2OD1|ND60PFM5KM7:TR?= NYPHPW1DW0GQR2LFVi=>
SK-N-AS NV7nRWFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDUfndKSzVyPUO1MlA4OTRizszN NHPzb2lUSU6JUlXS
ChaGo-K-1 NUnhPZc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\SOGJ7UUN3ME2zOU43ODN{IN88US=> NH3IT|dUSU6JUlXS
RT-112 NXPOWVNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7Gd4VKSzVyPUO1Mlk5PzlizszN MVHTRW5IWkWU
HTC-C3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXnO4FFUUN3ME2zOk4zOzV3IN88US=> M3rvd3NCVkeURWK=
SK-NEP-1 NH6ySXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmX6TWM2OD1|Nj62NVA3KM7:TR?= M3PKcXNCVkeURWK=
LB831-BLC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzlNphYUUN3ME2zO{43PTRzIN88US=> NF;Pdo5USU6JUlXS
CTB-1 MoT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\lZmFiUUN3ME2zPE41PTF{IN88US=> M4TU[XNCVkeURWK=
MOLT-4 NFLYNWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTN6LkizPVEh|ryP MkDNV2FPT1KHUh?=
SW756 MluzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTRyLkmzPFUh|ryP MUfTRW5IWkWU
CAL-72 NWj6cZVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTR{LkCzJO69VQ>? M3;3UXNCVkeURWK=
KNS-62 NYraSG94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zndGlEPTB;NEKuOlI6PiEQvF2= Mnj6V2FPT1KHUh?=
KARPAS-299 Ml7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTR|LkOyN|Mh|ryP MnG4V2FPT1KHUh?=
HEL M3HoPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\NVW5ZUUN3ME20OU41PjR4IN88US=> NHTRZ5JUSU6JUlXS
KP-4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrJTWM2OD12Nj63N|YyKM7:TR?= NWC0T5cxW0GQR2LFVi=>
NEC8 NF3aZnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED4U|VKSzVyPUS3MlE3PjFizszN M4H6bHNCVkeURWK=
G-402 NG\rbphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{OzbGlEPTB;NEiuO|AyOiEQvF2= NXjTSYZtW0GQR2LFVi=>

... 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]

+ 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 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

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

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