Doramapimod

• 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].

• Product Name Alternative :

  BIRB 796

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Autophagy; p38 MAPK; Raf

• Type :

  Reference compound

• Related Pathways :

  Autophagy; MAPK/ERK Pathway

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Inflammation/Immunology; Cancer

• Assay Protocol :

  https://www.medchemexpress.com/Doramapimod.html

• Purity :

  99.98

• Solubility :

  DMSO : 100 mg/mL (ultrasonic) |Ethanol : 33.33 mg/mL (ultrasonic)

• Smiles :

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

• Molecular Formula :

  C31H37N5O3

• Molecular Weight :

  527.66

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Dietrich J, et al. The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors. Bioorg Med Chem. 2010 Aug 1;18 (15) :5738-48|[2]Cicenas J, et al. JNK, p38, ERK, and SGK1 Inhibitors in Cancer. Cancers (Basel) . 2017 Dec 21;10 (1) . pii: E1.|[3]Kuma Y, et al. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J Biol Chem, 2005, 280 (20), 19472-19479.|[4]He D, et al. BIRB796, the inhibitor of p38 mitogen-activated protein kinase, enhances the efficacy of chemotherapeutic agents in ABCB1 overexpression cells. PLoS One. 2013;8 (1) :e54181.|[5]Park JK, et al. p38 mitogen-activated protein kinase inhibition ameliorates angiotensin II-induced target organ damage. Hypertension. 2007 Mar;49 (3) :481-9.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  B-Raf; p38 MAPK; p38α; p38β; p38γ; p38δ

• CAS Number :

  [285983-48-4]