733035-26-2
Chemical Structure
Diazepinomicin
Synonym(s): ECO-4601; TLN-4601; BU 4664L
- CAS No.: 733035-26-2
- Formula:C28H34N2O4
- Molecular Weight:462.58
IUPAC Name: 4,6,8-trihydroxy-10-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one
InChIKey: SALVHVNECODMJP-GNUCVDFRSA-N
SMILES: O=C1C2=CC=CC(O)=C2NC3=C(O)C=C(O)C=C3N1C/C=C(C)/CC/C=C(C)/CC/C=C(C)\C
Biological Activity: Diazepinomicin (ECO-4601) is a reagent with both anticancer and antibacterial activities.. Diazepinomicin decreases Bcl2 and BAX expression, induces dose-dependent cell death and apoptotic bodies, and inhibits Ras-MAPK signaling and tumor growth/proliferation. Diazepinomicin induces apoptosis through caspase 3 activation, PARP cleavage, cytochrome C release, loss of membrane potential, and DNA fragmentation, independent of PBR expression. Diazepinomicin binds PBR/TSPO and displaces PK11195 through its farnesyl side chain rather than the dibenzodiazepinone core. Diazepinomicin can be used in research on hepatocellular carcinoma, Gram-positive bacterial infections, and glioma[1][2][3].
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Diazepinomicin | Diazepinomicin (ECO-4601) is a reagent with both anticancer and antibacterial activities.. Diazepinomicin decreases Bcl2 and BAX expression, induces dose-dependent cell death and apoptotic bodies, and inhibits Ras-MAPK signaling and tumor growth/proliferation. Diazepinomicin induces apoptosis through caspase 3 activation, PARP cleavage, cytochrome C release, loss of membrane potential, and DNA fragmentation, independent of PBR expression. Diazepinomicin binds PBR/TSPO and displaces PK11195 through its farnesyl side chain rather than the dibenzodiazepinone core. Diazepinomicin can be used in research on hepatocellular carcinoma, Gram-positive bacterial infections, and glioma. | |||||||||||||||||||||
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References
- [1]. Rambabu V, et al. In vitro cytotoxicity perspective of diazepinomicin (ECO-4601) on human hepatoma cell line (HEPG2)[J]. Biomedicine & Aging Pathology, 2014, 4(1): 65-70.
- [2]. Charan RD, et al. Diazepinomicin, a new antimicrobial alkaloid from a marine Micromonospora sp. J Nat Prod. 2004;67(8):1431-1433. [Content Brief]
- [3]. Bertomeu T, et al. TLN-4601 peripheral benzodiazepine receptor (PBR/TSPO) binding properties do not mediate apoptosis but confer tumor-specific accumulation. Biochemical pharmacology. 2010 Nov 15;80(10):1572-9. [Content Brief]
