2. MAPK/ERK Pathway Autophagy
  3. p38 MAPK Raf Autophagy
  4. Doramapimod

Doramapimod  (Synonyms: BIRB 796)

Cat. No.: HY-10320 Purity: 99.62%
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Doramapimod (BIRB 796) est un inhibiteur de p38 MAPK qui est oralement active et puissant, avec un IC50 pour p38α=38 nM, pour p38β=65 nM, pour p38γ=200 nM, et pour p38δ=520 nM. Doramapimod a une affinité picomolaire pour la kinase p38 (Kd=0.1 nM). Doramapimod inhibe également le B-Raf avec un IC50 de 83 nM.

Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.

For research use only. We do not sell to patients.

Doramapimod Chemical Structure

Doramapimod Chemical Structure

CAS No. : 285983-48-4

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Based on 26 publication(s) in Google Scholar

Other Forms of Doramapimod:

Doramapimod Related Antibodies

Top Publications Citing Use of Products

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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BRaf c-Raf Raf

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  • References

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Description

Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM[1][2].

IC50 & Target[1][2]

p38α

38 nM (IC50)

p38β

65 nM (IC50)

p38δ

520 nM (IC50)

p38γ

200 nM (IC50)

B-Raf

83.4 nM (IC50)

Abl

14600 nM (IC50)

p38 MAP kinase

0.1 nM (Kd)

Cellular Effect
Cell Line Type Value Description References
PBMC IC50
15 nM
Compound: BIRB-796
Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA
Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA
[PMID: 21888439]
PBMC IC50
30 nM
Compound: BIRB-796
Inhibition of LPS-stimulated TNFalpha release in human PBMC by ELISA
Inhibition of LPS-stimulated TNFalpha release in human PBMC by ELISA
[PMID: 18602262]
U-937 IC50
15 nM
Compound: 4; BIRB-796
Antiinflammatory activity in differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS-stimulation for 4 hrs by sandwich ELISA relative to vehicle-treated control
Antiinflammatory activity in differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS-stimulation for 4 hrs by sandwich ELISA relative to vehicle-treated control
[PMID: 26800309]
In Vitro

Doramapimod (BIRB 796) is usually associated with inflammation because of its role in T-cell proliferation and cytokine production[1].
Doramapimod (BIRB 796) blocks the stress-induced phosphorylation of the scaffold protein SAP97, further establishing that this is a physiological substrate of SAPK3/p38γ. The binding of Doramapimod to the p38 MAPKs or JNK1/2 is impairing their phosphorylation by the upstream kinase MKK6 or MKK4[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Doramapimod Related Antibodies
In Vivo

The mean xenograft weigh of Doramapimod (BIRB 796) is lighter than control. The inhibition rate of Doramapimod is 1.93%[4].
The Doramapimod (BIRB 796) treatment slightly reduces blood pressure (166±7 mm Hg at week 7; P<0.05), whereas SD rats are normotensive (123±3 mm Hg). Despite the reduction in blood pressure, untreated and Doramapimod-treated dTGRs have similar heart weight and cardiac hypertrophy indices (heart-to-tibia ratio), which are significantly higher compare with nontransgenic SD rats (310±6 versus 307±6 versus 206±5 mg/cm, respectively; P<0.05)[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

527.66

Formula

C31H37N5O3
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=C4C=CC=CC4=C(OCCN5CCOCC5)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (236.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 33.33 mg/mL (63.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8952 mL 9.4758 mL 18.9516 mL
5 mM 0.3790 mL 1.8952 mL 3.7903 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.98%

SDS (393 KB)

COA (255 KB) LCMS (257 KB) Elemental Analysis Report (112 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[3]

Human embryonic kidney (HEK) 293 and HeLa cells are exposed to 0.5 M sorbitol for 30 min or 100 ng/mL EGF for 10 min and then lysed in buffer A (50 mM Tris-HCl, pH 7.5, 1 mM EGTA, 1 mM EDTA, 1 mM sodium orthovanadate, 10 mM sodium fluoride, 50 mM sodium β-glycerophosphate, 5 mM pyrophosphate, 0.27 M sucrose, 0.1 mM phenylmethylsulfonyl fluoride, 1% (v/v) Triton X-100) plus 0.1% (v/v) 2-mercaptoethanol and Complete proteinase inhibitor mixture. Lysates are centrifuged at 18,000× g for 5 min at 4°C, and the supernatants are removed, quick-frozen in liquid nitrogen, and stored at -20°C until use. When required, cells are preincubated for 1 h without or with 10 μM SB 203580 or 10 μM PD 184352 or with different concentrations of Doramapimod for the times indicated in the figures[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4][5]

Mice[4]
Athymic nude mice (BALB/c-nu/nu), 6 to 8 weeks of age and weighing 18 to 24 g, are used. The mice are treated with Doramapimod (10 mg/kg p.o., every 3 days×5). The body weights of the animals and the two perpendicular tumor diameters (A and B) are recorded every 3 days, and the tumor volume (V) is estimated.
Rats[5]
Male transgenic dTGRs (RCC Ltd) and age-matched nontransgenic Sprague-Dawley (SD) rats (MDC) are use. 2 different protocols are performed. In protocol 2, untreated dTGR (n=15), dTGR+BIRB796 (30 mg/kg per day in the diet for 3 weeks; n=11), and SD (n=8 each group) rats are analyzed. Systolic blood pressure is measured weekly by tail cuff. Twenty-four-hour urine samples are collected in metabolic cages from weeks 5 to 7. Serum is collected at week 7. Serum creatinine and cystatin C are measured by clinical routine assays. Urinary rat albumin is determined by enzyme-linked immunosorbent assay. The aim of protocol 2 is to focus on electrophysiological alterations and mortality. Untreated dTGR (n=10), dTGR+BIRB796 (n=10), and SD (n=10) rats are studied up to week 8.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.8952 mL 9.4758 mL 18.9516 mL 47.3790 mL
5 mM 0.3790 mL 1.8952 mL 3.7903 mL 9.4758 mL
10 mM 0.1895 mL 0.9476 mL 1.8952 mL 4.7379 mL
15 mM 0.1263 mL 0.6317 mL 1.2634 mL 3.1586 mL
20 mM 0.0948 mL 0.4738 mL 0.9476 mL 2.3689 mL
25 mM 0.0758 mL 0.3790 mL 0.7581 mL 1.8952 mL
30 mM 0.0632 mL 0.3159 mL 0.6317 mL 1.5793 mL
40 mM 0.0474 mL 0.2369 mL 0.4738 mL 1.1845 mL
50 mM 0.0379 mL 0.1895 mL 0.3790 mL 0.9476 mL
60 mM 0.0316 mL 0.1579 mL 0.3159 mL 0.7896 mL
DMSO 80 mM 0.0237 mL 0.1184 mL 0.2369 mL 0.5922 mL
100 mM 0.0190 mL 0.0948 mL 0.1895 mL 0.4738 mL
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Doramapimod Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Doramapimod285983-48-4BIRB 796BIRB796BIRB-796p38 MAPKRafAutophagyRaf kinasesInhibitorinhibitorinhibit

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