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Apilimod - ≥98%, high purity , 1-phosphatidylinositol 3-phosphate 5-kinase inhibitor, CAS No.541550-19-0, 1-phosphatidylinositol 3-phosphate 5-kinase inhibitor

Item Number
A340149
Grouped product items
SKUSizeAvailabilityPrice Qty
A340149-25mg
25mg
In stock
$78.90
A340149-50mg
50mg
In stock
$129.90
A340149-100mg
100mg
In stock
$205.90
A340149-250mg
250mg
In stock
$463.90
A340149-1g
1g
In stock
$1,668.90
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a potent inhibitor of cytokines IL-12 and IL-23 production which are potential regulators of certain autoimmune and inflammatory diseases

View related series
Immunology/Inflammation Interleukin Related phosphoinositide kinase，FYVE-type zinc finger containing Inhibitor PI3K/Akt/mTOR PIKfyve

Basic Description

SynonymsGFW2K84S4L | Apilimod [INN] | HY-14644 | AKOS015909602 | N-[6-Morpholin-4-yl-2-(2-pyridin-2-yl-ethoxy)-pyrimidin-4-yl]-N'-[1-m-tolyl-meth-(E)-ylidene]-hydrazine | BA177430 | Apilimod | N-[(E)-(3-methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsApilimod (STA-5326) is a potent, orally active and selective inhibitor of the cytokines IL-12 and IL-23. Apilimod selectively suppresses synthesis of IL-12 and IL-23 by inhibition of phosphotransferase activity of TLR-4 regulator lipid kinase PIKfyve (pho
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of action1-phosphatidylinositol 3-phosphate 5-kinase inhibitor
Product Description

Apilimod is a potent inhibitor of the cytokines IL-12 and IL-23 production. IL-12 and IL-23 are potential regulators of certain autoimmune and inflammatory diseases.|The following water-soluble salt forms are also available:|Apilimod Hydrochloride |Apilimod mesylate

Product Properties

ALogP3.8

Associated Targets(Human)

PIKFYVE Tchem 1-phosphatidylinositol 3-phosphate 5-kinase (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIKFYVE Tchem 1-phosphatidylinositol 3-phosphate 5-kinase (270 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Murine hepatitis virus (113 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Marburgvirus (118 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Vero C1008 (1716 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name N-[(E)-(3-methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine
INCHI InChI=1S/C23H26N6O2/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/h2-7,9,15-17H,8,10-14H2,1H3,(H,26,27,28)/b25-17+
InChi Key HSKAZIJJKRAJAV-KOEQRZSOSA-N
Canonical SMILES CC1=CC(=CC=C1)C=NNC2=CC(=NC(=N2)OCCC3=CC=CC=N3)N4CCOCC4
Isomeric SMILES CC1=CC(=CC=C1)/C=N/NC2=CC(=NC(=N2)OCCC3=CC=CC=N3)N4CCOCC4
PubChem CID 10173277
Molecular Weight 418.49

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot NumberCertificate TypeDateItem
B2318896Certificate of AnalysisJan 16, 2023 A340149
B2318956Certificate of AnalysisJan 16, 2023 A340149
B2318957Certificate of AnalysisJan 16, 2023 A340149
B2318959Certificate of AnalysisJan 16, 2023 A340149
B2318961Certificate of AnalysisJan 16, 2023 A340149

Chemical and Physical Properties

Solubilityinsoluble in H2O； ≥17.9 mg/mL in DMSO； ≥6.86 mg/mL in EtOH with ultrasonic
Melt Point(°C)70-80° C

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H302:Harmful if swallowed

Precautionary Statements

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P301+P317:IF SWALLOWED: Get medical help.

Related Documents

 SDS

 Specification Sheet

References

1. Wada Y, Lu R, Zhou D, Chu J, Przewloka T, Zhang S, Li L, Wu Y, Qin J, Balasubramanyam V et al..  (2007)  Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor..  Blood,  109  (3): (1156-64).  [PMID:17053051] [10.1021/op500134e]
2. Wada Y, Cardinale I, Khatcherian A, Chu J, Kantor AB, Gottlieb AB, Tatsuta N, Jacobson E, Barsoum J, Krueger JG.  (2012)  Apilimod inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis..  PLoS ONE,  7  (4): (e35069).  [PMID:22493730] [10.1021/op500134e]
3. Cai X, Xu Y, Cheung AK, Tomlinson RC, Alcázar-Román A, Murphy L, Billich A, Zhang B, Feng Y, Klumpp M et al..  (2013)  PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling..  Chem Biol,  20  (7): (912-21).  [PMID:23890009] [10.1021/op500134e]
4. Gayle S, Landrette S, Beeharry N, Conrad C, Hernandez M, Beckett P, Ferguson SM, Mandelkern T, Zheng M, Xu T et al..  (2017)  Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma..  Blood,  129  (13): (1768-1778).  [PMID:28104689] [10.1021/op500134e]
5. Nelson EA, Dyall J, Hoenen T, Barnes AB, Zhou H, Liang JY, Michelotti J, Dewey WH, DeWald LE, Bennett RS et al..  (2017)  The phosphatidylinositol-3-phosphate 5-kinase inhibitor apilimod blocks filoviral entry and infection..  PLoS Negl Trop Dis,  11  (4): (e0005540).  [PMID:28403145] [10.1021/op500134e]
6. Baranov MV, Bianchi F, van den Bogaart G.  (2020)  The PIKfyve Inhibitor Apilimod: A Double-Edged Sword against COVID-19..  Cells,  10  (1): (30).  [PMID:33375410] [10.1021/op500134e]
7. Qiu S, Leung A, Bo Y, Kozak RA, Anand SP, Warkentin C, Salambanga FDR, Cui J, Kobinger G, Kobasa D et al..  (2018)  Ebola virus requires phosphatidylinositol (3,5) bisphosphate production for efficient viral entry..  Virology,  513  (13): (17-28).  [PMID:29031163] [10.1021/op500134e]
8. Logue J, Chakraborty AR, Johnson R, Goyal G, Rodas M, Taylor LJ, Baracco L, McGrath ME, Haupt R, Furlong BA et al..  (2022)  PIKfyve-specific inhibitors restrict replication of multiple coronaviruses in vitro but not in a murine model of COVID-19..  Commun Biol,  5  (1): (808).  [PMID:35962188] [10.1021/op500134e]
9. Baranov MV, Bianchi F, Schirmacher A, van Aart MAC, Maassen S, Muntjewerff EM, Dingjan I, Ter Beest M, Verdoes M, Keyser SGL et al..  (2019)  The Phosphoinositide Kinase PIKfyve Promotes Cathepsin-S-Mediated Major Histocompatibility Complex Class II Antigen Presentation..  iScience,  11  (13): (160-177).  [PMID:30612035] [10.1021/op500134e]
10. Ianevski A, Yao R, Fenstad MH, Biza S, Zusinaite E, Reisberg T, Lysvand H, Løseth K, Landsem VM, Malmring JF et al..  (2020)  Potential Antiviral Options against SARS-CoV-2 Infection..  Viruses,  12  (6): (1755-70).  [PMID:32545799] [10.1021/op500134e]

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