1. Apoptosis
  2. Apoptosis
  3. Anticancer agent 83

Anticancer agent 83 is a potent anticancer agent, inhibits LOX IMVI cells growth with a GI50 value of 0.15 mM. Anticancer agent 83 reduces mitochondrial membrane potential and induces DNA damage to induces leukemia cells apoptosis.

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Anticancer agent 83 Chemical Structure

Anticancer agent 83 Chemical Structure

CAS No. : 904815-29-8

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Description

Anticancer agent 83 is a potent anticancer agent, inhibits LOX IMVI cells growth with a GI50 value of 0.15 mM. Anticancer agent 83 reduces mitochondrial membrane potential and induces DNA damage to induces leukemia cells apoptosis[1].

Cellular Effect
Cell Line Type Value Description References
A549 GI50
> 100 μM
Compound: 4a
Antiproliferative activity against human A549 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human A549 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
BALB/3T3 GI50
> 100 μM
Compound: 4a
Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
HaCaT GI50
> 100 μM
Compound: 4a
Antiproliferative activity against human HaCaT cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human HaCaT cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
HCT-116 GI50
> 100 μM
Compound: 4a
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
HCT-116 GI50
8.4 μM
Compound: 4a
Antiproliferative activity against p53-deficient human HCT-116 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against p53-deficient human HCT-116 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
HEK293 GI50
> 100 μM
Compound: 4a
Antiproliferative activity against human HEK293 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human HEK293 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
HeLa GI50
> 100 μM
Compound: 4a
Antiproliferative activity against human HeLa cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human HeLa cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
HL-60(TB) GI50
2.8 μM
Compound: 4a
Antiproliferative activity against human HL-60(TB) cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human HL-60(TB) cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
HOP-92 GI50
2.85 μM
Compound: 4a
Antiproliferative activity against human HOP-92 cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human HOP-92 cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
Jurkat GI50
0.69 μM
Compound: 4a
Antiproliferative activity against human Jurkat cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human Jurkat cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
K562 GI50
5.4 μM
Compound: 4a
Antiproliferative activity against human K562 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human K562 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
KB 3-1 GI50
7.4 μM
Compound: 4a
Antiproliferative activity against human KB 3-1 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human KB 3-1 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
LOX IMVI GI50
0.15 μM
Compound: 4a
Antiproliferative activity against human LOX IMVI cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human LOX IMVI cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
MCF7 GI50
> 100 μM
Compound: 4a
Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
MDA-MB-231 GI50
> 100 μM
Compound: 4a
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
NCI-H460 IC50
28 nM
Compound: 4a
Antiproliferative activity against human NCI-H460 cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human NCI-H460 cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
NCI-H522 GI50
1.97 μM
Compound: 4a
Antiproliferative activity against human NCI-H522 cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human NCI-H522 cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
RXF 393 GI50
4.27 μM
Compound: 4a
Antiproliferative activity against human RXF 393 cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human RXF 393 cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
SF-295 GI50
2.71 μM
Compound: 4a
Antiproliferative activity against human SF-295 cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human SF-295 cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
SK-OV-3 GI50
10 μM
Compound: 4a
Antiproliferative activity against human SK-OV-3 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human SK-OV-3 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
SR GI50
1.77 μM
Compound: 4a
Antiproliferative activity against human SR cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human SR cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
THP-1 GI50
> 100 μM
Compound: 4a
Antiproliferative activity against human THP-1 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human THP-1 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
TK-10 GI50
3.21 μM
Compound: 4a
Antiproliferative activity against human TK-10 cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human TK-10 cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
UO-31 GI50
2.88 μM
Compound: 4a
Antiproliferative activity against human UO-31 cells incubated for 48 hrs and measured by SRB assay
Antiproliferative activity against human UO-31 cells incubated for 48 hrs and measured by SRB assay
[PMID: 35973342]
WM793 GI50
> 100 μM
Compound: 4a
Antiproliferative activity against human WM793 cells incubated for 72 hrs and measured by MTT assay
Antiproliferative activity against human WM793 cells incubated for 72 hrs and measured by MTT assay
[PMID: 35973342]
In Vitro

Anticancer agent 83 (compound 4a) (0.01-100 μM; 24 h) showing strong activity towards human colon carcinoma HCT116 p53−/− cells with deletion of P53 gene (GI50=8.4 μM), human epidermoid cervix carcinoma KB3-1 (GI50=7.4 μM), human ovarian carcinoma Skov 3 cells (GI50=10 μM), and human chronic myelogenous leukemia K562 cells (GI50=5.4 μM)[1].
Anticancer agent 83 (0.5 μM; 24 h) interrupts DNA stability and induction of apoptosis in Jurkat cells, and decreases mitochondrial membrane potential[1].

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

Cell Viability Assay[1]

Cell Line: Human colon carcinoma HCT116 p53−/− cells with deletion of P53 gene, human epidermoid cervix carcinoma KB3-1, human ovarian carcinoma Skov 3 cells, and human chronic myelogenous leukemia K562 cells
Concentration: 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 24 hours
Result: Inhibited cell viability in different cells with GI50s of 8.4 M (HCT116 p53−/−), 7.4 M (KB3-1), 10 M (Skov 3), and 5.4 M (K562), respectively.

Immunofluorescence[1]

Cell Line: Jurkat cells
Concentration: 0.5 μM
Incubation Time: 24 hours
Result: Induced morphological changes (including apoptotic bodies, membrane blebbing, chromatin condensation), and DNA fragmentation in Jurkat T-cells.
Molecular Weight

377.46

Formula

C20H19N5OS

CAS No.
SMILES

O=C(C1=C(C)N(C2=CC=C(C(C)C)C=C2)N=N1)NC3=CC=C(SC#N)C=C3

Shipping

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Storage

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

Purity & Documentation
References
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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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Anticancer agent 83
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