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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
25 Results for "
PIKfyve
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "PIKfyve" in MCE Product Catalog:
44
44 Publications Verification
Synonyms: STA 5326; LAM-002A free base; AIT-101
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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.
44
44 Publications Verification
Synonyms: STA 5326 mesylate; LAM-002A; AIT-101 mesylate
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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.
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16 Cited Publications
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.
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12 Cited Publications
Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca 2+-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 .
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6 Cited Publications
Cat. No.: HY-15982
CAS No.: 1232221-74-7
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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.
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1 Cited Publications
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 significantly suppresses tumor proliferation in mice bearing LTL-331R human prostate cancer PDX tumors. PIK5-12d can be used for the study of prostate cancer .
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WX8 (Ro 91-4714) is an ATP-competitive PIKFYVE inhibitor, with Kd 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 .
Cat. No.: HY-161619
CAS No.: 2258606-34-5
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RMC-113 is a PIP4K2C and PIKfyve inhibitor with the Ki vaules of 46 nM and 370 nM. RMC-113 reverses SARS-CoV-2-induced impairment of autophagic flux. RMC-113 shows antiviral activity .
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.
Cat. No.: HY-163133
CAS No.: 3033209-92-3
PIKfyve-IN-3 (compound L22) has a remarkable interaction with PIKfyve kinase with a Kd value of 0.47 nM. PIKfyve-IN-3 has oral activity. PIKfyve-IN-3 inhibits tumor growth in a HeLa xenograft model .
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PIKfyve-IN-2 is a potent PIKfyve kinase inhibitor and can be used for cancers, autoimmune disorders research .
Cat. No.: HY-160477
CAS No.: 300713-88-6
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DC-SX029 is a potent SNX10 protein-protein interaction (PPI) inhibitor with oral activity with an estimated KD 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 .
Synonyms: Methuosis inducer 1
HZX-02-059 is an allosteric inhibitor of PIKFYVE, and a methuosis inducer. HZX-02-059 disrupts the PIKfyve/TFEB axis, suppresses tubulin polymerization, reduces phosphorylated mTOR levels, downregulates p53, PI3K/AKT, c-Myc, and NF-κB pathways. HZX-02-059 induces G2/M cell cycle arrest, apoptosis, and inhibits cancer cell proliferation. HZX-02-059 can be used for the research of lymphoma, double-hit lymphoma, and B-cell acute lymphoblastic leukemia .
Cat. No.: HY-170909
CAS No.: 3097803-72-7
PIKfyve-IN-4 (Compound 40) is an orally active and selective inhibitor of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve), with an IC50 of 0.60 nM. PIKfyve-IN-4 exhibits good systemic tolerance .
Cat. No.: HY-163943
CAS No.: 1802068-51-4
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; Kd=61 nM). In addition, UNI418 inhibits the proteolytic activation of proteases regulated by PIKfyve (Kd=0.78 nM) to prevent SARS-CoV-2 from entering host cells .
Cat. No.: HY-123876
CAS No.: 2171502-44-4
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AS2677131 is a potent and orally active PIKfyve inhibitor. AS2677131 inhibits f IL-12p40, IL-6 and IL-1β through a PIKfyve-c-Rel pathway. AS2677131 selectively inhibits DNA-binding activity of c-Rel to IL-12p40 and IL-1β promoter. AS2677131 inhibits MHC class II expression on B cells. AS2677131 can be used for the researches of inflammation and immunology, such as arthritis .
Cat. No.: HY-177091
CAS No.: 2171506-45-7
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AS2795440 is a PIKfyve inhibitor. AS2795440 selectively inhibits proinflammatory cytokine such as IL-12p40 and IL-6 production and B cell activation without affecting Ca 2+ signaling. AS2795440 significantly reduces joint inflammation and bone loss in adjuvant-induced arthritis (AIA) mice model. AS2795440 can be used for inflammatory and autoimmune diseases like rheumatoid arthritis, psoriasis and inflammatory bowel disease research .
Cat. No.: HY-14644B
CAS No.: 870087-37-9
Synonyms: STA 5326 hydrochloride; LAM-002A free base hydrochloride; AIT-101 hydrochloride
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Apilimod (STA 5326) hydrochloride is a PIKFYVE kinase inhibitor that promotes NLRP3 inflammatory vesicle activation and IL-1β secretion. Apilimod hydrochloride has been shown to inhibit host cell proteases, which may prevent viral invasion but also block antiviral immune responses, potentially exacerbating immunosuppression in COVID-19.
Cat. No.: HY-RS10542
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PIKFYVE Human Pre-designed siRNA Set A contains three designed siRNAs for PIKFYVE gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
