1. Apoptosis Autophagy PI3K/Akt/mTOR
  2. Apoptosis Autophagy Caspase mTOR
  3. NSC647889

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.

NSC647889

NSC647889 Chemical Structure

CAS No. : 1033931-92-8

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Description

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[1][2][3].

IC50 & Target[1]

Caspase-3

 

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.
Molecular Weight

548.83

Formula

C33H48N4OS

CAS No.
Appearance

Solid

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
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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:
NSC647889
Cat. No.:
HY-176761
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