Adezmapimod
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod can inhibit p38 MAPK and lead to the inhibition of downstream HSP27 phosphorylation. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator[1][2][3].
Product Specifications
CAS Number
[152121-47-6]
Product Name Alternative
SB 203580; RWJ 64809
UNSPSC
12352005
Hazard Statement
H302, H319
Target
Autophagy; HSP; Mitophagy; Organoid; p38 MAPK
Type
Reference compound
Related Pathways
Autophagy; Cell Cycle/DNA Damage; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Stem Cell/Wnt
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology; Cancer
Assay Protocol
https://www.medchemexpress.com/SB-203580.html
Purity
99.96
Solubility
DMSO : 20 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)C
Molecular Formula
C21H16FN3OS
Molecular Weight
377.43
Precautions
H302, H319
References & Citations
[1]Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351 (Pt 1) :95-105.|[2]Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J Biol Chem. 2000 Mar 10;275 (10) :7395-402.|[3]Leelahavanichkul K, et al. A role for p38 MAPK in head and neck cancer cell growth and tumor-induced angiogenesis and lymphangiogenesis. Mol Oncol. 2014 Feb;8 (1) :105-18.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
P38 MAPK; p38β
Citation 01
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