PIKfyve

FYVE domain-containing phosphatidylinositol 3-phosphate 5-kinase; Phosphatidylinositol 3-phosphate 5-kinase; Fab1

PIKfyve

Related Products

PIKfyve, a FYVE finger-containing phosphoinositide kinase, is an enzyme that in humans is encoded by the PIKFYVE gene. The principal enzymatic activity of PIKfyve is to phosphorylate PtdIns3P to PtdIns(3,5)P2. PIKfyve activity is responsible for the production of both PtdIns(3,5)P2 and phosphatidylinositol 5-phosphate (PtdIns5P). PIKfyve is a large protein, containing a number of functional domains and expressed in several spliced forms. By directly binding membrane PtdIns(3)P, the FYVE finger domain of PIKfyve is essential in localizing the protein to the cytosolic leaflet of endosomes. Impaired PIKfyve enzymatic activity by dominant-interfering mutants, siRNA- mediated ablation or pharmacological inhibition causes endosome enlargement and cytoplasmic vacuolation due to impaired PtdIns(3,5)P2 synthesis. Thus, via PtdIns(3,5)P2 production, PIKfyve participates in several aspects of endosome dynamics, thereby affecting a number of trafficking pathways that emanate from or traverse the endosomal system en route to the trans-Golgi network or later compartments along the endocytic pathway.

PIKfyve Related Products (14):

By Effects:	Inhibitors (12) Degrader (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-14644

Apilimod	Inhibitor	99.56%
Apilimod (STA 5326) 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. Apilimod is a potent and highly selective PIKfyve inhibitor.

HY-13228

YM-201636	Inhibitor	98.06%
YM-201636 is a potent and selective PIKfyve inhibitor with an IC₅₀ of 33 nM. YM-201636 also inhibits p110α with an IC₅₀ of 3.3 μM. YM-201636 inhibits retroviral replication.

HY-118630

Vacuolin-1	Inhibitor	98.93%
Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca²⁺-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation. Vacuolin-1 can induce vacuole formation and increase the percentage of enucleated cells.

HY-14644A

Apilimod mesylate	Inhibitor	99.83%
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. Apilimod is a potent and highly selective PIKfyve inhibitor.

HY-15982

APY0201	Inhibitor	99.93%
APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P₂ in the presence of in the presence of [³³P]ATP with an IC₅₀ of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.

HY-161619

RMC-113	Inhibitor
RMC-113 is a PIP4K2C and PIKfyve inhibitor with the K_i vaules of 46 nM and 370 nM. RMC-113 reverses SARS-CoV-2-induced impairment of autophagic flux. RMC-113 shows antiviral activity.

HY-159625

WX8	Inhibitor
WX8 (Ro 91-4714) is an ATP-competitive PIKFYVE inhibitor, with K_d values of 0.9 nM and 340 nM for PIKFYVE and PIP4K2C, respectively. WX8 (Ro 91-4714) inhibits lysosomal fission without effecting homotypic lysosomal fusion. WX8 (Ro 91-4714) is used in the research of autophagy-dependent cancer.

HY-119624

MOMIPP	Inhibitor	99.37%
MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB).

HY-155994

PIK5-12d	Degrader	99.90%
PIK5-12d is a PROTAC PIKfyve degrader (DC₅₀: 1.48 nM). PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d has anti-tumor activity.

HY-151473

PIKfyve-IN-1	Inhibitor	99.64%
PIKfyve-IN-1 is a highly potent and cell-active chemical probe that inhibits phosphatidylinositol-3phosphate 5-kinase (PIKfyve) with IC₅₀ value of 6.9 nM. PIKfyve-IN-1 can be used for the research of PIKfyve in virology. PIKfyve-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-160477

DC-SX029	Inhibitor	98.07%
DC-SX029 is a potent SNX10 protein-protein interaction (PPI) inhibitor with an estimated K_D constant of ~0.935 μM by surface plasmon resonance (SPR). DC-SX029 blocks the SNX10-PIKfyve interaction, thereby decreased the TBK1/c-Rel signaling activation. DC-SX029 does not affect the protein level of SNX10. DC-SX029 has the potential for inflammatory bowel disease (IBD) research.

HY-163133

PIKfyve-IN-3		99.55%
PIKfyve-IN-3 (compound L22) has a remarkable interaction with PIKfyve kinase with a K_d value of 0.47 nM. PIKfyve-IN-3 has oral activity. PIKfyve-IN-3 inhibits tumor growth in a HeLa xenograft model.

HY-154956

PIKfyve-IN-2	Inhibitor
PIKfyve-IN-2 is a potent PIKfyve kinase inhibitor and can be used for cancers, autoimmune disorders research.

HY-163943

UNI418	Inhibitor
UNI418 is a dual inhibitor of PIKfyve and PIP5K1C with antiviral activity against SARS-CoV-2 (EC₅₀=1.4 μM). UNI418 blocks ACE2-mediated SARS-CoV-2 viral endocytosis by inhibiting PIP5K1C (IC₅₀=60.1 nM; K_d=61 nM). In addition, UNI418 inhibits the proteolytic activation of proteases regulated by PIKfyve (K_d=0.78 nM) to prevent SARS-CoV-2 from entering host cells.

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