SGC-PIKFYVE-1 | PIKfyve inhibitor | Probechem Biochemicals

Chemical Structure : SGC-PIKFYVE-1

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SGC-PIKFYVE-1 (PIKfyve inhibitor 17)

货号: PC-49344Not For Human Use, Lab Use Only.

SGC-PIKFYVE-1 is a potent, selective and cell-active chemical probe inhibitor of PIKfyve with IC50 of 4.0 nM in NanoBRET assays.

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50 mg		Get quote
100 mg		Get quote

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生物&药学活性

SGC-PIKFYVE-1 is a potent, selective and cell-active chemical probe inhibitor of PIKfyve with IC50 of 4.0 nM in NanoBRET assays.

SGC-PIKFYVE-1 inhibits viral replication in the MHV-nLuc assay with IC50 of 23.5 nM, also is a potent inhibitor of SARS-CoV-2 replication, outperformed remdesivir (IC50=86.4 nM).

SGC-PIKFYVE-1 demonstrates good kinome-wide selectivity, binding with PoC < 10 to nine or fewer WT human kinases at 1 μM.

SGC-PIKFYVE-1 reduces uptake of His6-SARS-CoV-2 spike protein by HEK293T-ACE2 cells, impacts lysosomal homeostasis.

SGC-PIKFYVE-1 disrupts multiple phases of the lifecycle of β-coronaviruses: viral replication and viral entry.

SGC-PIKFYVE-1 (10 µM) also inhibits voltage-gated sodium currents through the inhibition of Nav1.7 and Nav1.8 channels, without affecting voltage-gated calcium or potassium currents in sensory neurons.

SGC-PIKFYVE-1 (30 mg/kg) alleviated mechanical and cold sensitivity induced by neuropathic or inflammatory pain in both male and female mice, without causing motor impairments.

物理化学性质&存储条件

分子量	331.423
分子式	C20H21N5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	11-(3-(Dimethylamino)prop-1-yn-1-yl)-5,6,7,8-tetrahydropyrimido[4',5':3,4]cyclohepta[1,2-b]indol-2-amine

参考文献

1. Drewry DH, et al. J Med Chem. 2022 Oct 13;65(19):12860-12882.
2. Rodríguez-Palma EJ, et al. Neurobiol Pain. 2024 Nov 29;17:100174.

SGC-PIKFYVE-1 (PIKfyve inhibitor 17)

生物&药学活性

物理化学性质&存储条件

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SGC-PIKFYVE-1 (PIKfyve inhibitor 17)

生物&药学活性

物理化学性质&存储条件

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