Apilimod mesylate | B1129

Apilimod is a small molecule that inhibits IL-12 and IL-23 production - cytokines that are involved in autoimmune diseases through the prevention of nuclear translocation of c-Rel. It suppresses the Th1, but not the Th2, response, resulting in reduced inflammation in a mouse model of inflammatory bowel disease. Apilimod inhibits the production of IL-23p19 and IL-12/IL-23p40 subunits while decreasing skin inflammation in a clinical study of patients with psoriasis. Apilimod inhibits phosphatidylinositol-3-phosphate 5-kinase (PIKfyve; IC₅₀ = 14 nM), which is necessary and sufficient for suppression of IL-12/IL-23p40 expression.

Apilimod is a small molecule that inhibits IL-12 and IL-23 production - cytokines that are involved in autoimmune diseases - through the prevention of nuclear translocation of c-Rel. It suppresses the Th1, but not the Th2, response, resulting in reduced inflammation in a mouse model of inflammatory bowel disease. Apilimod inhibits the production of IL-23p19 and IL-12/IL-23p40 subunits while decreasing skin inflammation in a clinical study of patients with psoriasis. Apilimod inhibits phosphatidylinositol-3-phosphate 5-kinase (PIKfyve; IC₅₀ = 14 nM), which is necessary and sufficient for suppression of IL-12/IL-23p40 expression.

B1129 | Apilimod mesylate DataSheet

Alternate Name/Synonyms: (E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine dimethanesulfonate

Appearance: White to off-white solid

Formulation: N/A

CAS Number: 870087-36-8

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₅H₃₄N₆O₈S₂

Molecular Weight: 610.7

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO

Handling: Protect from air and moisture

Country of Origin: USA

Tag Line: IL-12/IL-23 inhibitor

MDL Number: N/A

PubChem CID: 11527330

SMILES: CC1=CC=CC(=C1)C=NNC2=NC(=NC(=C2)N3CCOCC3)OCCC4=CC=CC=N4.CS(=O)(=O)O.CS(=O)(=O)O

InChi: InChI=1S/C23H26N6O2.2CH4O3S/c1-18-5-4-6-19(15-18)17-25-28-21-16-22(29-10-13-30-14-11-29)27-23(26-21)31-12-8-20-7-2-3-9-24-20;2*1-5(2,3)4/h2-7,9,15-17H,8,10-14H2,1H3,(H,26,27,28);2*1H3,(H,2,3,4)/b25-17+;;

InChi Key: GAJWNIKZLYZYSY-OKUPSQOASA-N