Doramapimod is a highly selective p38α MAPK inhibitor to TNF-α with EC50 of 18 nM. At 10 μM, doramapimod inhibits JNK2 in vitro, but at the low concentration necessary to inhibit p38α, it does not affect the phosphorylation of JNK substrates in cells.Pote
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
MAP kinase p38 alpha inhibitor
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
BIRB 796 (Doramapimod) is a highly selective p38α MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKCα/β/γ. A p38α MAPK and JNK2;p38 MAPK抑制剂
1.Pargellis C, Tong L, Churchill L, Cirillo PF, Gilmore T, Graham AG, Grob PM, Hickey ER, Moss N, Pav S et al.. (2002) Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site.. Nat Struct Biol, 9 (4):(268-72). [PMID:11896401]
2.Moffett K, Konteatis Z, Nguyen D, Shetty R, Ludington J, Fujimoto T, Lee KJ, Chai X, Namboodiri H, Karpusas M et al.. (2011) Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).. Bioorg Med Chem Lett, 21 (23):(7155-65). [PMID:22014550]
3.Ivshina MP et al.. (2022) CPEB1 regulates the inflammatory immune response, phagocytosis, and alternative polyadenylation in microglia.. Glia, 70 (10):(1850-1863). [PMID:35635122]
4.Lanfranco MF et al.. (2021) Expression and secretion of apoE isoforms in astrocytes and microglia during inflammation.. Glia, 69 (6):(1478-1493). [PMID:33556209]
Solution Calculators
Molarity Calculator
Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator
Determine the dilution needed to prepare a stock solution.