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

Doramapimod (Synonyms: BIRB 796)

Cat. No.: HY-10320 Purity: 99.72%
Handling Instructions

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 (BIRB 796) has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod (BIRB 796) 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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Customer Review

Based on 6 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 (BIRB 796) has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod (BIRB 796) also inhibits B-Raf with an IC50 of 83 nM.

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].

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].

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
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KeyWords:

Doramapimod | BIRB 796 | BIRB796 | BIRB-796 | p38 MAPK | Raf | Autophagy | Raf kinases | Inhibitor | inhibitor | inhibit

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Doramapimod
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