HSP90-IN-13

Names

[ CAS No. ]:
2446055-29-2

[ Name ]:
HSP90-IN-13

Biological Activity

[Description]:

HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase
Signaling Pathways >> Metabolic Enzyme/Protease >> HSP
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Signaling Pathways >> Cell Cycle/DNA Damage >> HSP
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

[Target]

HSP90:25.07 nM (IC50)

Topoisomerase-2:25.85 nM (IC50)

EGFR:38.5 nM (IC50)

VEGFR-2:126.95 nM (IC50)


[In Vitro]

HSP90-IN-13 (compound 5k) arrests the cell cycle on MCF-7 at a G2/M phase by 35.06% and induced apoptosis by 19.82%[1]. HSP90-IN-13 has anti-proliferative activity against HCT-116, Hela and MCF-7 cell lines with IC50s of 4.47 μM, 7.55 μM and 4.04 μM, respectively[1]. HSP90-IN-13 has potent multi-target inhibitory activities against EGFR, VEGFR-2 and Topoisomerase-2 with IC50 values of 38.5 nM, 126.95 nM and 25.85 nM, respectively[1].

[References]

[1]. El-Shafey HW, et al. Synthetic approaches, anticancer potential, HSP90 inhibition, multitarget evaluation, molecular modeling and apoptosis mechanistic study of thioquinazolinone skeleton: Promising antibreast cancer agent. Bioorg Chem. 2020 Aug;101:103987.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H21N5O3S

[ Molecular Weight ]:
483.54

Related Compounds