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

Doramapimod (Synonyms: BIRB 796)

Cat. No.: HY-10320 Purity: 99.88%
Handling Instructions

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 7 publication(s) in Google Scholar

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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

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)

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].

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

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].

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.

285983-48-4

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (189.52 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.1895 mL 0.9476 mL 1.8952 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

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

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.74 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
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

Purity: 99.88%

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Keywords:

DoramapimodBIRB 796BIRB796BIRB-796p38 MAPKRafAutophagyRaf kinasesInhibitorinhibitorinhibit

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