1. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Sirtuin Reactive Oxygen Species Keap1-Nrf2
  3. SPC-180002

SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway.

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SPC-180002 Chemical Structure

SPC-180002 Chemical Structure

CAS No. : 2170274-53-8

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Description

SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway[1].

IC50 & Target

SIRT1

1.13 ± 0.3 μM (IC50)

SIRT3

5.41 ± 4.8 μM (IC50)

In Vitro

SPC-180002 (0-5 μM, 24 h) inhibits cell cycle progression via p21 accumulation, which causes subsequent cellular senescence[1].
SPC-180002 dose not induce apoptosis and autophagy[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SPC-180002 (1-5mg/kg, twice a week, i.p.) inhibits the growth of various cancer cells and impedes tumor growth in MCF7 tumor xenograft[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five weeks female athymic nude mice (BALB/c)[1]
Dosage: 1 mg/kg or 5 mg/kg
Administration: i.p., twice a week
Result: Significantly impeded tumor progression. The gain of tumor volume in SPC-180002-treated mice was significantly reduced by 48% at the low dose (1 mg/kg) and by 52% at the high dose (5 mg/kg), compared to vehicle-treated mice.
Molecular Weight

317.38

Formula

C18H23NO4

CAS No.
SMILES

O=C(C(CN(CCC1=CC=CC=C1)CC(C(OC)=O)=C)=C)OC

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SPC-180002
Cat. No.:
HY-155784
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