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 Chemical Structure

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].

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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    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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Antibiotic DC 81
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HY-107767
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