3029584-84-4
Chemical Structure
BSc5367
- CAS No.: 3029584-84-4
- Formula:C20H15N3O2
- Molecular Weight:329.35
IUPAC Name: 1,1-difluoro-2-iodoethane
InChIKey: GZHRICWZECSYJT-UHFFFAOYSA-N
SMILES: COC(C1=CC(C2=CN=C3NC=C(C3=C2)C4=CN=CC=C4)=CC=C1)=O
Biological Activity: BSc5367 is a NEK1 kinase inhibitor with an IC50 of 11.5 nM. BSc5367 modulates the cell cycle, DNA repair, and microtubule dynamics, reduces YAP1 phosphorylation, induces DNA damage, and upregulates γH2A.X. BSc5367 drives TDP-43 nucleocytoplasmic translocation, inhibits NEK1-mediated ETS1 phosphorylation, increases ETS1 acetylation, sensitizes ccRCC cells to Sunitinib (HY-10255A), and mimics the phenotype of NEK1-mutant motor neurons. BSc5367 inhibits NEK1 in zebrafish models and causes expansion of renal tubule volume, affecting pronephros development. BSc5367 can be used in research related to polycystic kidney disease, renal cancer, and amyotrophic lateral sclerosis[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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BSc5367 | 98.21% | BSc5367 is a NEK1 kinase inhibitor with an IC50 of 11.5 nM. BSc5367 modulates the cell cycle, DNA repair, and microtubule dynamics, reduces YAP1 phosphorylation, induces DNA damage, and upregulates γH2A.X. BSc5367 drives TDP-43 nucleocytoplasmic translocation, inhibits NEK1-mediated ETS1 phosphorylation, increases ETS1 acetylation, sensitizes ccRCC cells to Sunitinib (HY-10255A), and mimics the phenotype of NEK1-mutant motor neurons. BSc5367 inhibits NEK1 in zebrafish models and causes expansion of renal tubule volume, affecting pronephros development. BSc5367 can be used in research related to polycystic kidney disease, renal cancer, and amyotrophic lateral sclerosis. | ||||||||||||||||||||
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References
- [1]. Pilakowski J, et al. Design, synthesis and biological evaluation of novel aminopyrazole- and 7-azaindole-based Nek1 inhibitors and their effects on zebrafish kidney development. Bioorganic & medicinal chemistry letters. 2021 Dec 01;53:128418. [Content Brief]
- [2]. Qian K, et al. HDAC8 Enhances the Function of HIF-2α by Deacetylating ETS1 to Decrease the Sensitivity of TKIs in ccRCC. Advanced science (Weinheim, Baden-Wurttemberg, Germany). 2024 Sep;11(36):e2401142.
- [3]. Brenner D, et al. A rare missense variant impacting NEK1 kinase function is associated with ALS. Acta neuropathologica communications. 2026 Jun 25;14(1):135.
