2411429-33-7

2411429-33-7 structure

Name: NCT-58
Chemical Name: NCT-58
CAS Number: 2411429-33-7
Molecular Formula: C₂₇H₃₄N₂O₅
Molecular Weight: 466.57
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2022-02-21 09:55:32
Modify Date: 2024-01-11 11:30:49
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells[1].

Name	NCT-58

Description	NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells[1].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> HSP Signaling Pathways >> Cell Cycle/DNA Damage >> HSP
Target	HSP90 Apoptosis
In Vitro	NCT-58 treatment (0.1-20 μM; 72 hours) dose-dependently reduces cell viability in HER2-positive BT474 and SKBR3 cells[1]. NCT-58 treatment (0.1-10 μM; 72 hours) increases the number of early and late apoptotic cells in HER2-positive BT474 and SKBR3 cells[1]. NCT-58 treatment (2-10 μM; 72 hours) effectively reduced the levels of truncated p95HER2 and its phosphorylated form, as well as downregulation of Akt and phospho-Akt (Ser473) protein contents in JIMT-1 and MDA-MB-453 cells[1]. Cell Viability Assay[1] Cell Line: BT474 and SKBR3 cells Concentration: 0, 0.1, 0.5, 1, 5, 10, 15, 20 μM Incubation Time: 72 hours Result: Significantly reduced cell growth. Apoptosis Analysis[1] Cell Line: BT474 and SKBR3 cells Concentration: 0, 2, 10 μM Incubation Time: 72 hours Result: Increased the number of early and late apoptotic cells. Western Blot Analysis[1] Cell Line: Trastuzumab-resistant JIMT-1 and MDA-MB-453 cells Concentration: 0, 2, 10 μM Incubation Time: 72 hours Result: Effectively reduced the levels of truncated p95HER2 and its phosphorylated form, as well as downregulation of Akt and phospho-Akt (Ser473) protein contents in JIMT-1 and MDA-MB-453 cells.
In Vivo	NCT-58 (30 mg/kg; i.p.; every other day for 47 days) suppresses Trastuzumab-resistant tumor growth[1]. NCT-58 (30 mg/kg; i.p.; every other day for 47 days) causes a significant impediment of tumor growth and a marked decrease in tumor weight[1]. Animal Model: Trastuzumab-resistant xenograft model (female nude mice; 6 weeks; BALB/c)[1] Dosage: 30 mg/kg Administration: i.p.; every other day for 47 days Result: Significantly reduced tumor growth.
References	[1]. Park S, et al. The C-terminal HSP90 inhibitor NCT-58 kills trastuzumab-resistant breast cancer stem-like cells. Cell Death Discov. 2021;7(1):354.

Molecular Formula	C₂₇H₃₄N₂O₅
Molecular Weight	466.57
Storage condition	-20°C

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