Apilimod (mesylate)

• UNSPSC Description:

  Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively[1]. Apilimod is a potent and highly selective PIKfyve inhibitor.

• Target Antigen:

  Interleukin Related; PIKfyve

• Type:

  Reference compound

• Related Pathways:

  Immunology/Inflammation;PI3K/Akt/mTOR

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Inflammation/Immunology; Cancer

• Assay Protocol:

  https://www.medchemexpress.com/apilimod-mesylate.html

• Solubility:

  DMSO : 12.5 mg/mL (ultrasonic)|H2O : 100 mg/mL (ultrasonic)

• Smiles:

  CC1=CC=CC(/C=N/NC2=CC(N3CCOCC3)=NC(OCCC4=CC=CC=N4)=N2)=C1.CS(=O)(O)=O.CS(=O)(O)=O

• Molecular Weight:

  610.70

• References & Citations:

  [1]Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64.|[2]Billich A. Drug evaluation: apilimod, an oral IL-12/IL-23 inhibitor for the treatment of autoimmune diseases and common variable immunodeficiency.IDrugs. 2007 Jan;10(1):53-9.|[3]Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122.bioRxiv. 2023 Aug 12.|bioRxiv. 2024 Jan 23.|Biomaterials. 2022 Jun;285:121509.|bioRxiv. 2020 Apr 21;2020.04.21.053058. |bioRxiv. 2023 Apr 28.|bioRxiv. 2023 Aug 12.|bioRxiv. 2023 Aug 28.|bioRxiv. 2023 Oct 20:2023.10.19.563158.|bioRxiv. 2024 May 10.|biorxiv. 2024 May 27.|Biotechnol J. 2022 Dec 7;e2200147.|Br J Cancer. 2020 Aug;123(4):542-555.|Cancer Lett. 2023 Oct 6:216435.|Cell Mol Life Sci. 2016 Dec;73(24):4717-4737. |Commun Biol. 2022 Mar 24;5(1):262.|Exp Mol Med. 2024 Aug 1.|J Biol Chem. 2022 Dec 6;102775.|J Virol. 2021 Aug 18;JVI0097521.|Mol Biol Cell. 2022 Jan 12;mbcE21060309.|Nat Commun. 2020 Mar 27;11(1):1620.|PLoS Pathog. 2023 Feb 24;19(2):e1011202.|Proc Natl Acad Sci U S A. 2023 Dec 26;120(52):e2307423120.|Proc Natl Acad Sci U S A. 2024 May 21;121(21):e2403685121.|Sci Adv. 2022 Jul 22;8(29):eabn1440.|Sci Adv. 2023 Oct 13;9(41):eadh1134.|SSRN. 2024 Jan 26.|Theranostics. 2020 Mar 4;10(9):3925-3938.|Viruses. 2021 Jun 28;13(7):1255.|Viruses. 2023 Jun 12, 15(6), 1353.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 2

• CAS Number:

  870087-36-8