1. Anti-infection Apoptosis Cell Cycle/DNA Damage
  2. Antibiotic Apoptosis DNA/RNA Synthesis
  3. Antibiotic DC 81

Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct.

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Antibiotic DC 81

Antibiotic DC 81 Chemical Structure

CAS No. : 81307-24-6

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Description

Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct[1][2].

Cellular Effect
Cell Line Type Value Description References
A2780 GI50
0.14 μM
Compound: 1, DC-81
Cytotoxicity against human A2780 cells after 48 hrs by SRB assay
Cytotoxicity against human A2780 cells after 48 hrs by SRB assay
[PMID: 20444601]
A2780 GI50
0.14 μM
Compound: 1, DC-81
Cytotoxicity against human A2780 cells after 24 hrs by WST-1 assay
Cytotoxicity against human A2780 cells after 24 hrs by WST-1 assay
[PMID: 20732817]
A2780 GI50
0.14 μM
Compound: 1, DC-81
Anticancer activity against human A2780 cells by SRB method
Anticancer activity against human A2780 cells by SRB method
[PMID: 21676506]
A2780 GI50
0.14 μM
Compound: 1, DC-81
Growth inhibition of human A2780 cells
Growth inhibition of human A2780 cells
10.1039/C1MD00072A
A2780 GI50
0.14 μM
Compound: 2, DC-81
Cytotoxicity against human A2780 cells by sulforhodamine B method
Cytotoxicity against human A2780 cells by sulforhodamine B method
[PMID: 21459581]
A2780 GI50
0.14 μM
Compound: 3, DC-81
Growth inhibition of human A2780 cells after 48 hrs by SRB assay
Growth inhibition of human A2780 cells after 48 hrs by SRB assay
[PMID: 20031423]
A2780 GI50
0.14 μM
Compound: 3, DC-81
Cytotoxicity against human A2780 cells after 48 hrs by SRB assay
Cytotoxicity against human A2780 cells after 48 hrs by SRB assay
[PMID: 20673627]
A2780 GI50
0.14 μM
Compound: 3, DC-81
Anticancer activity against human A2780 cells by SRB method
Anticancer activity against human A2780 cells by SRB method
[PMID: 22104151]
A2780 GI50
0.14 μM
Compound: 4, DC-81
Anticancer activity against human A2780 cells after 48 hrs by SRB assay
Anticancer activity against human A2780 cells after 48 hrs by SRB assay
[PMID: 20557981]
A2780 GI50
0.14 μM
Compound: DC-81
Growth inhibition of human A2780 cells by SRB method
Growth inhibition of human A2780 cells by SRB method
[PMID: 18207392]
A2780 GI50
0.14 μM
Compound: DC-81
Cytotoxicity against human A2780 cells after 48 hrs by SRB assay
Cytotoxicity against human A2780 cells after 48 hrs by SRB assay
[PMID: 20554354]
A-431 IC50
1.65 μM
Compound: I, DC-81
Anticancer activity against human A431 cells after 48 hrs by MTT assay
Anticancer activity against human A431 cells after 48 hrs by MTT assay
[PMID: 22209733]
A549 GI50
0.16 μM
Compound: 1, DC-81
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
[PMID: 20444601]
A549 GI50
0.16 μM
Compound: 1, DC-81
Cytotoxicity against human A549 cells after 24 hrs by WST-1 assay
Cytotoxicity against human A549 cells after 24 hrs by WST-1 assay
[PMID: 20732817]
A549 GI50
0.16 μM
Compound: 1, DC-81
Anticancer activity against human A549 cells by SRB method
Anticancer activity against human A549 cells by SRB method
[PMID: 21676506]
A549 GI50
0.16 μM
Compound: 1, DC-81
Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
10.1039/C1MD00072A
A549 GI50
0.16 μM
Compound: 2, DC-81
Cytotoxicity against human A549 cells by sulforhodamine B method
Cytotoxicity against human A549 cells by sulforhodamine B method
[PMID: 21459581]
A549 GI50
0.16 μM
Compound: 3, DC-81
Growth inhibition of human A549 cells after 48 hrs by SRB assay
Growth inhibition of human A549 cells after 48 hrs by SRB assay
[PMID: 20031423]
A549 GI50
0.16 μM
Compound: 3, DC-81
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
[PMID: 20673627]
A549 GI50
0.16 μM
Compound: 3, DC-81
Anticancer activity against human A549 cells by SRB method
Anticancer activity against human A549 cells by SRB method
[PMID: 22104151]
A549 GI50
0.16 μM
Compound: DC-81
Growth inhibition of human A549 cells by SRB method
Growth inhibition of human A549 cells by SRB method
[PMID: 18207392]
A549 GI50
0.16 μM
Compound: DC-81
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
[PMID: 20554354]
A549 IC50
1.11 μM
Compound: I, DC-81
Anticancer activity against human A549 cells after 48 hrs by MTT assay
Anticancer activity against human A549 cells after 48 hrs by MTT assay
[PMID: 22209733]
CH1 IC50
0.1 μM
Compound: 3
In vitro cytotoxicity against ovarian carcinoma cell line CH1.
In vitro cytotoxicity against ovarian carcinoma cell line CH1.
[PMID: 10514273]
CH1 IC50
0.1 μM
Compound: 5
Tested for cytotoxicity against CH1 human ovarian cells
Tested for cytotoxicity against CH1 human ovarian cells
[PMID: 10354403]
CHO-AA8 IC50
2 μM
Compound: 31 (DC-81)
In vitro cellular toxicity against chinese hamster AA8 cell line after 4 hr of compound exposure
In vitro cellular toxicity against chinese hamster AA8 cell line after 4 hr of compound exposure
[PMID: 12747786]
CHO-AA8 IC50
2000 nM
Compound: 31 (DC-81)
In vitro cellular toxicity against chinese hamster AA8 cell line after 4 hr of compound exposure
In vitro cellular toxicity against chinese hamster AA8 cell line after 4 hr of compound exposure
[PMID: 12747786]
COLO 205 GI50
0.11 μM
Compound: 1, DC-81
Cytotoxicity against human COLO205 cells after 48 hrs by SRB assay
Cytotoxicity against human COLO205 cells after 48 hrs by SRB assay
[PMID: 20444601]
COLO 205 GI50
0.11 μM
Compound: 1, DC-81
Cytotoxicity against human COLO205 cells after 24 hrs by WST-1 assay
Cytotoxicity against human COLO205 cells after 24 hrs by WST-1 assay
[PMID: 20732817]
COLO 205 GI50
0.11 μM
Compound: 1, DC-81
Anticancer activity against human COLO205 cells by SRB method
Anticancer activity against human COLO205 cells by SRB method
[PMID: 21676506]
COLO 205 GI50
0.11 μM
Compound: 1, DC-81
Growth inhibition of human COLO205 cells
Growth inhibition of human COLO205 cells
10.1039/C1MD00072A
COLO 205 GI50
0.11 μM
Compound: 2, DC-81
Cytotoxicity against human COLO205 cells by sulforhodamine B method
Cytotoxicity against human COLO205 cells by sulforhodamine B method
[PMID: 21459581]
COLO 205 GI50
0.11 μM
Compound: 3, DC-81
Growth inhibition of human COLO205 cells after 48 hrs by SRB assay
Growth inhibition of human COLO205 cells after 48 hrs by SRB assay
[PMID: 20031423]
COLO 205 GI50
0.11 μM
Compound: 3, DC-81
Cytotoxicity against human COLO205 cells after 48 hrs by SRB assay
Cytotoxicity against human COLO205 cells after 48 hrs by SRB assay
[PMID: 20673627]
COLO 205 GI50
0.11 μM
Compound: 3, DC-81
Anticancer activity against human COLO205 cells by SRB method
Anticancer activity against human COLO205 cells by SRB method
[PMID: 22104151]
COLO 205 GI50
0.11 μM
Compound: DC-81
Growth inhibition of human Colo205 cells by SRB method
Growth inhibition of human Colo205 cells by SRB method
[PMID: 18207392]
COLO 205 GI50
0.11 μM
Compound: DC-81
Cytotoxicity against human COLO205 cells after 48 hrs by SRB assay
Cytotoxicity against human COLO205 cells after 48 hrs by SRB assay
[PMID: 20554354]
COLO 205 IC50
0.86 μM
Compound: I, DC-81
Anticancer activity against human COLO205 cells after 48 hrs by MTT assay
Anticancer activity against human COLO205 cells after 48 hrs by MTT assay
[PMID: 22209733]
EMT6 IC50
1100 nM
Compound: 31 (DC-81)
In vitro cellular toxicity against murine mammary carcinoma EMT6 cell line after 4 hr of compound exposure
In vitro cellular toxicity against murine mammary carcinoma EMT6 cell line after 4 hr of compound exposure
[PMID: 12747786]
HOP-62 GI50
0.15 μM
Compound: 1, DC-81
Cytotoxicity against human HOP62 cells after 48 hrs by SRB assay
Cytotoxicity against human HOP62 cells after 48 hrs by SRB assay
[PMID: 20444601]
HOP-62 GI50
0.15 μM
Compound: 1, DC-81
Cytotoxicity against human HOP62 cells after 24 hrs by WST-1 assay
Cytotoxicity against human HOP62 cells after 24 hrs by WST-1 assay
[PMID: 20732817]
HOP-62 GI50
0.15 μM
Compound: 1, DC-81
Anticancer activity against human HOP62 cells by SRB method
Anticancer activity against human HOP62 cells by SRB method
[PMID: 21676506]
HOP-62 GI50
0.15 μM
Compound: 1, DC-81
Growth inhibition of human HOP62 cells
Growth inhibition of human HOP62 cells
10.1039/C1MD00072A
HOP-62 GI50
0.15 μM
Compound: 2, DC-81
Cytotoxicity against human HOP62 cells by sulforhodamine B method
Cytotoxicity against human HOP62 cells by sulforhodamine B method
[PMID: 21459581]
HOP-62 GI50
0.15 μM
Compound: 3, DC-81
Growth inhibition of human HOP62 cells after 48 hrs by SRB assay
Growth inhibition of human HOP62 cells after 48 hrs by SRB assay
[PMID: 20031423]
HOP-62 GI50
0.15 μM
Compound: 3, DC-81
Cytotoxicity against human HOP62 cells after 48 hrs by SRB assay
Cytotoxicity against human HOP62 cells after 48 hrs by SRB assay
[PMID: 20673627]
HOP-62 GI50
0.15 μM
Compound: DC-81
Cytotoxicity against human HOP62 cells after 48 hrs by SRB assay
Cytotoxicity against human HOP62 cells after 48 hrs by SRB assay
[PMID: 20554354]
HT-29 IC50
30.19 μM
Compound: 16b, DC-81
Cytotoxicity against human HT29 cells by MTT assay
Cytotoxicity against human HT29 cells by MTT assay
[PMID: 18538566]
HT-29 IC50
30.19 μmol
Compound: 16b, DC-81
Cytotoxicity against human HT29 cells by MTT assay
Cytotoxicity against human HT29 cells by MTT assay
[PMID: 18538566]
Jurkat IC50
2.2 μM
Compound: 9, DC-81
Antiproliferative activity against human Jurkat cells
Antiproliferative activity against human Jurkat cells
[PMID: 17081759]
K562 IC50
1 μM
Compound: 9, DC-81
Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
[PMID: 17081759]
KB GI50
0.17 μM
Compound: 1, DC-81
Cytotoxicity against human KB cells after 48 hrs by SRB assay
Cytotoxicity against human KB cells after 48 hrs by SRB assay
[PMID: 20444601]
KB GI50
0.17 μM
Compound: 1, DC-81
Cytotoxicity against human KB cells after 24 hrs by WST-1 assay
Cytotoxicity against human KB cells after 24 hrs by WST-1 assay
[PMID: 20732817]
KB GI50
0.17 μM
Compound: 1, DC-81
Anticancer activity against human KB cells by SRB method
Anticancer activity against human KB cells by SRB method
[PMID: 21676506]
KB GI50
0.17 μM
Compound: 1, DC-81
Growth inhibition of human KB cells
Growth inhibition of human KB cells
10.1039/C1MD00072A
KB GI50
0.17 μM
Compound: 2, DC-81
Cytotoxicity against human KB cells by sulforhodamine B method
Cytotoxicity against human KB cells by sulforhodamine B method
[PMID: 21459581]
KB GI50
0.17 μM
Compound: 3, DC-81
Growth inhibition of human KB cells after 48 hrs by SRB assay
Growth inhibition of human KB cells after 48 hrs by SRB assay
[PMID: 20031423]
KB GI50
0.17 μM
Compound: 3, DC-81
Cytotoxicity against human KB cells after 48 hrs by SRB assay
Cytotoxicity against human KB cells after 48 hrs by SRB assay
[PMID: 20673627]
KB GI50
0.17 μM
Compound: 3, DC-81
Anticancer activity against human KB cells by SRB method
Anticancer activity against human KB cells by SRB method
[PMID: 22104151]
KB GI50
0.17 μM
Compound: 4, DC-81
Anticancer activity against human KB cells after 48 hrs by SRB assay
Anticancer activity against human KB cells after 48 hrs by SRB assay
[PMID: 20557981]
KB GI50
0.17 μM
Compound: DC-81
Growth inhibition of human KB cells by SRB method
Growth inhibition of human KB cells by SRB method
[PMID: 18207392]
KB GI50
0.17 μM
Compound: DC-81
Cytotoxicity against human KB cells after 48 hrs by SRB assay
Cytotoxicity against human KB cells after 48 hrs by SRB assay
[PMID: 20554354]
L1210 IC50
0.38 μM
Compound: 5
Tested for cytotoxicity against L1210 Leukemia cell
Tested for cytotoxicity against L1210 Leukemia cell
[PMID: 10354403]
L1210 IC50
0.38 μM
Compound: DC-81
In vitro cytotoxicity was evaluated in L1210 cell line
In vitro cytotoxicity was evaluated in L1210 cell line
[PMID: 14505647]
L1210 IC50
0.38 μM
Compound: DC-81
In vitro cytotoxicity against leukemia L1210 cell line
In vitro cytotoxicity against leukemia L1210 cell line
[PMID: 14698184]
L1210 IC50
0.38 μM
Compound: DC-81
Compound was tested for inhibitory activity against L1210 cell line
Compound was tested for inhibitory activity against L1210 cell line
[PMID: 15225736]
L1210 IC50
0.38 μM
Compound: DC-81
In vitro cytotoxicity against mouse leukemia L1210 cell lines
In vitro cytotoxicity against mouse leukemia L1210 cell lines
[PMID: 15341949]
L1210 IC50
0.38 μM
Compound: DC-81
Tested in vitro for inhibition after 48 hr exposure against murine leukemia cell line L1210
Tested in vitro for inhibition after 48 hr exposure against murine leukemia cell line L1210
[PMID: 7996544]
L1210 IC50
0.38 μM
Compound: DC-81, 2
Cytotoxicity against mouse L1210 cells
Cytotoxicity against mouse L1210 cells
[PMID: 18378445]
MCF7 GI50
0.17 μM
Compound: 1, DC-81
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
[PMID: 20444601]
MCF7 GI50
0.17 μM
Compound: 1, DC-81
Cytotoxicity against human MCF7 cells after 24 hrs by WST-1 assay
Cytotoxicity against human MCF7 cells after 24 hrs by WST-1 assay
[PMID: 20732817]
MCF7 GI50
0.17 μM
Compound: 1, DC-81
Anticancer activity against human MCF7 cells by SRB method
Anticancer activity against human MCF7 cells by SRB method
[PMID: 21676506]
MCF7 GI50
0.17 μM
Compound: 1, DC-81
Growth inhibition of human MCF7 cells
Growth inhibition of human MCF7 cells
10.1039/C1MD00072A
MCF7 GI50
0.17 μM
Compound: 2, DC-81
Cytotoxicity against human MCF7 cells by sulforhodamine B method
Cytotoxicity against human MCF7 cells by sulforhodamine B method
[PMID: 21459581]
MCF7 GI50
0.17 μM
Compound: 3, DC-81
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
[PMID: 20031423]
MCF7 GI50
0.17 μM
Compound: 3, DC-81
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
[PMID: 20673627]
MCF7 GI50
0.17 μM
Compound: 3, DC-81
Anticancer activity against human MCF7 cells by SRB method
Anticancer activity against human MCF7 cells by SRB method
[PMID: 22104151]
MCF7 GI50
0.17 μM
Compound: DC-81
Growth inhibition of human MCF7 cells by SRB method
Growth inhibition of human MCF7 cells by SRB method
[PMID: 18207392]
MCF7 GI50
0.17 μM
Compound: DC-81
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
[PMID: 20554354]
MCF7 IC50
5 μM
Compound: 1, DC-81
Cytotoxicity against human MCF7 cells assessed as reduction cell viability after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction cell viability after 24 hrs by MTT assay
10.1039/C2MD20219K
PC-3 GI50
0.2 μM
Compound: 1, DC-81
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
[PMID: 20444601]
PC-3 GI50
0.2 μM
Compound: 1, DC-81
Cytotoxicity against human PC3 cells after 24 hrs by WST-1 assay
Cytotoxicity against human PC3 cells after 24 hrs by WST-1 assay
[PMID: 20732817]
PC-3 GI50
0.2 μM
Compound: 1, DC-81
Anticancer activity against human PC3 cells by SRB method
Anticancer activity against human PC3 cells by SRB method
[PMID: 21676506]
PC-3 GI50
0.2 μM
Compound: 1, DC-81
Growth inhibition of human PC3 cells
Growth inhibition of human PC3 cells
10.1039/C1MD00072A
PC-3 GI50
0.2 μM
Compound: 2, DC-81
Cytotoxicity against human PC3 cells by sulforhodamine B method
Cytotoxicity against human PC3 cells by sulforhodamine B method
[PMID: 21459581]
PC-3 GI50
0.2 μM
Compound: 3, DC-81
Growth inhibition of human PC3 cells after 48 hrs by SRB assay
Growth inhibition of human PC3 cells after 48 hrs by SRB assay
[PMID: 20031423]
PC-3 GI50
0.2 μM
Compound: 3, DC-81
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
[PMID: 20673627]
PC-3 GI50
0.2 μM
Compound: DC-81
Growth inhibition of human PC3 cells by SRB method
Growth inhibition of human PC3 cells by SRB method
[PMID: 18207392]
PC-3 GI50
0.2 μM
Compound: DC-81
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
[PMID: 20554354]
PC-3 IC50
1.19 μM
Compound: I, DC-81
Anticancer activity against human PC3 cells after 48 hrs by MTT assay
Anticancer activity against human PC3 cells after 48 hrs by MTT assay
[PMID: 22209733]
PC-6 IC50
0.33 μM
Compound: DC-81
In vitro cytotoxicity was evaluated in PC6 cell line
In vitro cytotoxicity was evaluated in PC6 cell line
[PMID: 14505647]
PC-6 IC50
0.33 μM
Compound: DC-81
In vitro cytotoxicity against leukemia PC6 cell line
In vitro cytotoxicity against leukemia PC6 cell line
[PMID: 14698184]
PC-6 IC50
0.33 μM
Compound: DC-81
Compound was tested for inhibitory activity against PC6 cell line
Compound was tested for inhibitory activity against PC6 cell line
[PMID: 15225736]
PC-6 IC50
0.33 μM
Compound: DC-81
In vitro cytotoxicity against human lung cancer PC-6 cells lines
In vitro cytotoxicity against human lung cancer PC-6 cells lines
[PMID: 15341949]
PC-6 IC50
0.33 μM
Compound: DC-81, 2
Cytotoxicity against human PC6 cells
Cytotoxicity against human PC6 cells
[PMID: 18378445]
SiHa GI50
0.16 μM
Compound: 3, DC-81
Anticancer activity against human SiHa cells by SRB method
Anticancer activity against human SiHa cells by SRB method
[PMID: 22104151]
SiHa GI50
0.17 μM
Compound: 1, DC-81
Cytotoxicity against human SiHa cells after 48 hrs by SRB assay
Cytotoxicity against human SiHa cells after 48 hrs by SRB assay
[PMID: 20444601]
SiHa GI50
0.17 μM
Compound: 1, DC-81
Cytotoxicity against human SiHa cells after 24 hrs by WST-1 assay
Cytotoxicity against human SiHa cells after 24 hrs by WST-1 assay
[PMID: 20732817]
SiHa GI50
0.17 μM
Compound: 1, DC-81
Anticancer activity against human SiHa cells by SRB method
Anticancer activity against human SiHa cells by SRB method
[PMID: 21676506]
SiHa GI50
0.17 μM
Compound: 1, DC-81
Growth inhibition of human SiHa cells
Growth inhibition of human SiHa cells
10.1039/C1MD00072A
SiHa GI50
0.17 μM
Compound: 2, DC-81
Cytotoxicity against human SiHa cells by sulforhodamine B method
Cytotoxicity against human SiHa cells by sulforhodamine B method
[PMID: 21459581]
SiHa GI50
0.17 μM
Compound: 3, DC-81
Growth inhibition of human SiHa cells after 48 hrs by SRB assay
Growth inhibition of human SiHa cells after 48 hrs by SRB assay
[PMID: 20031423]
SiHa GI50
0.17 μM
Compound: 3, DC-81
Cytotoxicity against human SiHa cells after 48 hrs by SRB assay
Cytotoxicity against human SiHa cells after 48 hrs by SRB assay
[PMID: 20673627]
SiHa GI50
0.17 μM
Compound: 4, DC-81
Anticancer activity against human SiHa cells after 48 hrs by SRB assay
Anticancer activity against human SiHa cells after 48 hrs by SRB assay
[PMID: 20557981]
SiHa GI50
0.17 μM
Compound: DC-81
Growth inhibition of human SiHa cells by SRB method
Growth inhibition of human SiHa cells by SRB method
[PMID: 18207392]
SiHa GI50
0.17 μM
Compound: DC-81
Cytotoxicity against human SiHa cells after 48 hrs by SRB assay
Cytotoxicity against human SiHa cells after 48 hrs by SRB assay
[PMID: 20554354]
SK-OV-3 IC50
1900 nM
Compound: 31 (DC-81)
In vitro cellular toxicity against human ovarian carcinoma SKOV3 cell line after 4 hr of compound exposure
In vitro cellular toxicity against human ovarian carcinoma SKOV3 cell line after 4 hr of compound exposure
[PMID: 12747786]
UV4 IC50
1500 nM
Compound: 31 (DC-81)
In vitro cellular toxicity against chinese hamster UV4 cell line after 4 hr of compound exposure
In vitro cellular toxicity against chinese hamster UV4 cell line after 4 hr of compound exposure
[PMID: 12747786]
ZR-75-1 GI50
2.34 μM
Compound: 1, DC-81
Growth inhibition of human ZR-75-1 cells
Growth inhibition of human ZR-75-1 cells
10.1039/C1MD00072A
ZR-75-1 GI50
2.37 μM
Compound: 1, DC-81
Cytotoxicity against human ZR-75-1 cells after 48 hrs by SRB assay
Cytotoxicity against human ZR-75-1 cells after 48 hrs by SRB assay
[PMID: 20444601]
ZR-75-1 GI50
2.37 μM
Compound: 1, DC-81
Cytotoxicity against human ZR-75-1 cells after 24 hrs by WST-1 assay
Cytotoxicity against human ZR-75-1 cells after 24 hrs by WST-1 assay
[PMID: 20732817]
ZR-75-1 GI50
2.37 μM
Compound: 1, DC-81
Anticancer activity against human ZR-75-1 cells by SRB method
Anticancer activity against human ZR-75-1 cells by SRB method
[PMID: 21676506]
ZR-75-1 GI50
2.37 μM
Compound: 2, DC-81
Cytotoxicity against human ZR-75-1 cells by sulforhodamine B method
Cytotoxicity against human ZR-75-1 cells by sulforhodamine B method
[PMID: 21459581]
ZR-75-1 GI50
2.37 μM
Compound: 3, DC-81
Growth inhibition of human ZR-75-1 cells after 48 hrs by SRB assay
Growth inhibition of human ZR-75-1 cells after 48 hrs by SRB assay
[PMID: 20031423]
ZR-75-1 GI50
2.37 μM
Compound: 3, DC-81
Cytotoxicity against human ZR-75-1 cells after 48 hrs by SRB assay
Cytotoxicity against human ZR-75-1 cells after 48 hrs by SRB assay
[PMID: 20673627]
ZR-75-1 GI50
2.37 μM
Compound: 3, DC-81
Anticancer activity against human ZR-75-1 cells by SRB method
Anticancer activity against human ZR-75-1 cells by SRB method
[PMID: 22104151]
ZR-75-1 GI50
2.37 μM
Compound: 4, DC-81
Anticancer activity against human ZR-75-1 cells after 48 hrs by SRB assay
Anticancer activity against human ZR-75-1 cells after 48 hrs by SRB assay
[PMID: 20557981]
ZR-75-1 GI50
2.37 μM
Compound: DC-81
Growth inhibition of human Zr-75-1 cells by SRB method
Growth inhibition of human Zr-75-1 cells by SRB method
[PMID: 18207392]
ZR-75-1 GI50
2.37 μM
Compound: DC-81
Cytotoxicity against human ZR-75-1 cells after 48 hrs by SRB assay
Cytotoxicity against human ZR-75-1 cells after 48 hrs by SRB assay
[PMID: 20554354]
In Vitro

Antibiotic DC 81 shows cytotoxicity against human melanoma cell lines B16, A375, A2058, and RPMI7951, with IC50 values of 4.4 μM, 18.5 μM, 31.0 μM, and 41.5 μM, respectively[1][2].
Antibiotic DC 81 exhibits its biological activity by covalently binding to the N2 of guanine in the minor groove of DNA, via the electrophilic carbinolamine functionality at N10-C11[1].
Antibiotic DC 81 (4 μM, 24 h) induces mitochondria dependent apoptosis[2].

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

Apoptosis Analysis[2]

Cell Line: B16 melanoma cells
Concentration: 4 μM
Incubation Time: 24 h
Result: Induced mitochondria dependent apoptosis.
In Vivo

Antibiotic DC 81 (0-10 mg/kg, i.p., at day 4, 7, 10, 13 after tumor cell injection) decreases the tumor burden in tumor-bearing mice, but the Antibiotic DC 81 at 10 mg/kg impairs cardiac muscle enzyme and liver function significantly[2].

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

Animal Model: Female C57BL/6 mice (8-12 weeks old, B16 cells were injected into the tail veins of mice)[2]
Dosage: 0.1, 1, 10 mg/kg
Administration: i.p., at day 4, 7, 10, 13 after tumor cell injection
Result: Substantially decreased the tumor burden by 20% at 1 mg/kg. DC-81 at 10 mg/kg induced an 8-10-fold increase of GPT and a 6-8-fold increase in CPK, which indicated severe impaired liver function and muscle damage. Did not impair significant renal function as demonstrated by serum creatinine.
Molecular Weight

246.26

Formula

C13H14N2O3

CAS No.
SMILES

O=C1C2=CC(OC)=C(O)C=C2N=C[C@@]3([H])N1CCC3

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