Cat. No.: HY-176761

NSC647889

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NSC647889 is an apoptosis and autophagy inducer. NSC647889 induces apoptosis, inhibits mTOR pathway and abrogates DNA synthesis. NSC647889 triggers LC3-positive vesicle formation, modulates AKT and 4EBP1 phosphorylation and shows heightened caspase-3 activation in multicellular spheroids. NSC647889 can be used for the research of solid cancer tumour, head-neck carcinoma, and colorectal cancer.

For research use only. We do not sell to patients.

Purity: 99.28%
CAS No.: 1033931-92-8
Formula: C₃₃H₄₈N₄OS
Molecular Weight:548.83

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

NSC647889 Chemical Structure

CAS No.: 1033931-92-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Caspase-3

All Caspase Isoforms :

All mTOR Isoforms :

In Vitro

NSC-647889 (2-20 μM; 4-10 h) potently induces apoptosis in ~80% of HCT116 colon carcinoma multicellular spheroid cells (excluding hypoxic core cells) at 10 μM, reduces spheroid cell clonogenicity to ~1% at 20 μM, and shows a ~2.5-fold lower viability reduction potency in spheroids compared to monolayer cultures^[2].
NSC-647889 (10 μM; 1 h) increases Ca²⁺/calmodulin-dependent calcineurin activity in HCT116 colon carcinoma cells^[2].
NSC-647889 (1.25-10 μM; 1 h) increases intracellular calcium levels in HCT116 colon carcinoma cells in a dose-dependent manner, with an 8-fold increase over control at 7.5 μM after 1 h incubation^[2].

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

Apoptosis Analysis^[2]

Cell Line:

HCT116 colon carcinoma multicellular spheroids (MCS) and monolayer cultures
Concentration:

2 μM; 5 μM; 10 μM; 20 μM
Incubation Time:

4 h; 6 h; 8 h; 10 h
Result:

Induced apoptosis in ~80% of HCT116 spheroid cells, with apoptosis restricted to cells 0-100 µm from the spheroid surface.
Reduced clonogenicity of cells dispersed from treated spheroids to <5% of solvent-treated controls at 10 μM, and to ~1% at 20 μM.
Showed a ~2.5-fold difference in viability reduction potency between monolayer and spheroid cultures, with spheroids showing lower sensitivity.
Increased apoptosis induction (ccK18 levels) with higher concentrations in both culture systems, with monolayer cultures showing stronger apoptosis at lower doses.

In Vivo

NSC-647889 (5 mg/kg; s.c.; single dose) induces significant tumor apoptosis in FaDu head-neck carcinoma xenografts in SCID mice^[2].

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

Animal Model:

SCID mice^[2]
Dosage:

5 mg/kg
Administration:

s.c.; single dose
Result:

Increased plasma caspase-cleaved K18 (ccK18) levels significantly compared to vehicle control.
Increased total K18 levels significantly compared to vehicle control.

Chemical Information

CAS No. 1033931-92-8
Appearance Solid
Molecular Weight 548.83
Formula C₃₃H₄₈N₄OS
Color White to off-white
SMILES

C[C@@]12[C@]3([H])[C@](CCC1C[C@H](CC2)NC(NC(C4=NC=CS4)CC5=CC=CC=C5)=O)([H])[C@@]6([H])[C@](CC3)([C@H](CC6)N(C)C)C
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 2.2 mg/mL (4.01 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8221 mL

9.1103 mL

18.2206 mL

5 mM

---

10 mM

---

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Linder S, et al. Treatment of solid tumours. France, WO2012128689 A. 2012-09-27.

[2]. Mohanty C, et al. Massive induction of apoptosis of multicellular tumor spheroids by a novel compound with a calmodulin inhibitor-like mechanism. J. Cancer Res. Ther. 2013.

[3]. Sensi F, et al. Preclinical three-dimensional colorectal cancer model: The next generation of in vitro drug efficacy evaluation. J Cell Physiol. 2018;234(1):181-191. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8221 mL	9.1103 mL	18.2206 mL	45.5514 mL

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NSC647889

Apoptosis Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All Caspase Isoforms

All mTOR Isoforms