Abcam, ab144247, Echinomycin, HIF-1alpha inhibitor

Size: 1mg / 5mg
MW 1101.3 Da, Purity >98%. Potent, reversible cell-permeable HIF-1α inhibitor (EC 50 = 1.2 nM, hypoxia-induced HIF-1 transcription activity in U215 cells). Specifically intercalates into DNA. Antibacterial, antiviral, antiangiogenic and antitumor effects in vivo. .
Key facts
CAS number:512-64-1,
Purity:>98%,
Form:SolidSee storage information,
Source:Streptomyces echinatus,
Molecular weight:1101.3 Da,
Molecular formula:C51H64N12O12S2,
PubChem:3197,
Nature:Native,
Solubility:Soluble in DMSO to 5 mM,
Biochemical name:Echinomycin,
Biological description:Potent, reversible cell-permeable HIF-1α inhibitor (EC50 = 1.2 nM, hypoxia-induced HIF-1 transcription activity in U215 cells). Specifically intercalates into DNA. Antibacterial, antiviral, antiangiogenic and antitumor effects in vivo.,
Canonical smiles:CC1C(=O)N(C2CSC(C(C(=O)N(C(C(=O)OCC(C(=O)N1)NC(=O)C3=NC4=CC=CC=C4N=C3)C(C)C)C)N(C(=O)C(NC(=O)C(COC(=O)C(N(C2=O)C)C(C)C)NC(=O)C5=NC6=CC=CC=C6N=C5)C)C)SC)C,
InChi:InChI=1S/C51H64N12O12S2/c1-25(2)38-49(72)74-22-36(59-42(65)34-21-53-30-17-13-15-19-32(30)57-34)44(67)55-28(6)46(69)63(10)40-48(71)62(9)39(26(3)4)50(73)75-23-35(58-41(64)33-20-52-29-16-12-14-18-31(29)56-33)43(66)54-27(5)45(68)60(7)37(47(70)61(38)8)24-77-51(40)76-11/h12-21,25-28,35-40,51H,22-24H2,1-11H3,(H,54,66)(H,55,67)(H,58,64)(H,59,65),
InChiKey:AUJXLBOHYWTPFV-UHFFFAOYSA-N,
IUPAC Name:N-[2,4,12,15,17,25-hexamethyl-27-methylsulfanyl-3,6,10,13,16,19,23,26-octaoxo-11,24-di(propan-2-yl)-20-(quinoxaline-2-carbonylamino)-9,22-dioxa-28-thia-2,5,12,15,18,25-hexazabicyclo[12.12.3]nonacosan-7-yl]quinoxaline-2-carboxamide

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
Werner's syndrome helicase (WRN) also known as Bloom's syndrome protein (Blm) plays a critical role in the maintenance of genome stability. It is an ATP-dependent DNA helicase with a mass of approximately 143 kDa that unwinds DNA during replication and repair processes. WRN is expressed in various tissues particularly in those with high proliferative capacity like the thymus pancreas and testis. Besides WRN other related proteins such as DNA polymerase iota FEN1 DNA polymerase kappa/POLK and DNA polymerase eta also contribute to DNA replication and repair functions.
Biological function summary
These proteins participate in complex interactions required for accurate DNA repair. WRN and Blm specifically are involved in processing stalled replication forks and resolving unusual DNA structures. These helicases function in conjunction with the DNA polymerases and FEN1 ensuring the fidelity of DNA synthesis and repair. These activities precisely control homologous recombination and the repair of double-strand breaks which are essential for preventing genomic instability.
Pathways
These proteins mainly interact within the DNA damage response and repair pathways. WRN and Blm participate in the homologous recombination and base excision repair pathways. Proteins like Nrf2 are linked to these pathways by regulation of the oxidative stress response which affects DNA repair processes. The interaction between FEN1 and the polymerases kappa and eta further facilitates the excision and synthesis steps necessary for gap-filling during the repair mechanism.
Mutations or dysfunctions in these proteins contribute to syndromes such as Werner's syndrome and Bloom syndrome. These disorders are characterized by premature aging and heightened cancer susceptibility respectively. The DNA repair defects related to these proteins also connect them to other conditions like Fanconi anemia. In this context aberrations in WRN and Blm alongside their interactions with FEN1 and DNA polymerases can exacerbate disease phenotypes stressing the relevance of effective DNA repair in maintaining cellular integrity.