PIK001 (PIK-001)

Chemical Structure : PIK001

Catalog No.: PC-25657Not For Human Use, Lab Use Only.

PIK001 (PIK-001) is a potent, specific small molecule PIKfyve inhibitor with IC50 of 10 nM.

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Biological Activity

PIK001 (PIK-001) is a potent, specific small molecule PIKfyve inhibitor with IC50 of 10 nM.
PIK001 demonstrates potent and specific anti MM activity, with IC50s of 40, 20, and 40 nM in KMS26, JJN3, and KMS11, respectively.
PIK001 shows <10% inhibition in 89% of kinases included in a broad 377 kinase panel, with only four kinases (CK1G2, RIPK2, VRK1, BMPR1B) being inhibited >20%, at 1 uM.
PIK001 disrupts lysosomal function and autophagy, promoting cellular vacuolation.
PIK001 (50 nM, 72 h) increased cell surface expression of MHC class I in the parental sensitive KMS26 and KMS11 HMCLs.
PIK001 showed anti-MM activity in the nanomolar range with minimal cytotoxic activity on normal human PBMCs.

Physicochemical Properties

M.Wt	414.47
Formula	C22H22N8O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-4-(5-(2-(3-methylbenzylidene)hydrazineyl)-2-(pyridin-4-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)morpholine

References

1. Bonolo De Campos C, et al. Blood. 2025 Nov 5:blood.2025030061.

PIK001 (PIK-001)

Biological Activity

Physicochemical Properties

References

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