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Apilimod dimesylate

Cat. No. 7283 1 Citation Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective PIKfyve inhibitor
Chemical Name: 4-(6-(2-(3-Methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine dimethanesulfonate
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Apilimod dimesylate

Apilimod dimesylate is a potent and selective PIKfyve inhibitor (IC50 = 14 nM). Exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. Apilimod dimesylate reduces the number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. Also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma compared with normal cells. Inhibits production of IL-12 and IL-23. In motor neurons derived from patients with amyotrophic lateral sclerosis (ALS) Apilimod dimesylate promotes exocytosis of neurotoxic proteins and in mouse ALS models, the compound reduces pathology and prolongs survival. Anti-inflammatory. Water-soluble.

Compound Libraries for Apilimod dimesylate

Apilimod dimesylate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Apilimod dimesylate

M. Wt 610.7
Formula C23H26N6O2.2CH3SO3H
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 870087-36-8
PubChem ID 91885471
InChI Key GAJWNIKZLYZYSY-OKUPSQOASA-N
Smiles C[S](O)(=O)=O.C[S](O)(=O)=O.CC1=CC=CC(\C=N\NC2=CC(=NC(OCCC3=CC=CC=N3)=N2)N2CCOCC2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Apilimod dimesylate

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 61.07 100
DMSO 30.53 50

Preparing Stock Solutions for Apilimod dimesylate

The following data is based on the product molecular weight 610.7. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.64 mL 8.19 mL 16.37 mL
5 mM 0.33 mL 1.64 mL 3.27 mL
10 mM 0.16 mL 0.82 mL 1.64 mL
50 mM 0.03 mL 0.16 mL 0.33 mL

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Product Datasheets for Apilimod dimesylate

Certificate of Analysis / Product Datasheet
Safety Datasheet

References for Apilimod dimesylate

References are publications that support the biological activity of the product.

Wada et al (2007) Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood 109 1156 PMID: 17053051

Cai et al (2013) PIKfyve, a class III PI-kinase, is the target of the small molecular IL12/23 inhibitor apilimod and a new player in toll-like receptor signaling. Chem.Biol. 20 912 PMID: 23890009

Riva et al (2020) Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing. Nature 586 113 PMID: 32707573

Ou et al (2020) Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. Nat.Commun. 11 1620 PMID: 32221306

Gayle et al (2017) Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood 129 1768 PMID: 28104689

Hung et al (2023) PIKFYVE inhibition mitigates disease in models of diverse forms of ALS. Cell PMID: 36754049

If you know of a relevant reference for Apilimod dimesylate, please let us know.

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1 Citation for Apilimod dimesylate

Citations are publications that use Tocris products. Selected citations for Apilimod dimesylate include:

Markku et al (2023) SARS-CoV-2 Infection of Human Neurons Is TMPRSS2 Independent, Requires Endosomal Cell Entry, and Can Be Blocked by Inhibitors of Host Phosphoinositol-5 Kinase. J Virol 97 e0014423 PMID: 37039676

Do you know of a great paper that uses Apilimod dimesylate from Tocris? Please let us know.

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