AdipoGen Life Sciences

GE23077 A1/B1

CHF 110.00

In stock

AG-CN2-0305-M0011 mgCHF 110.00

AG-CN2-0305-M0055 mgCHF 380.00

AG-CN2-0305-M02525 mgCHF 1'140.00

More Information
Product Details
Synonyms	Antibiotic GE23077A1/Antibiotic GE23077B1 Mixture
Product Type	Chemical
Properties
Formula	C₃₁H₅₁N₉O₁₆[A1] C₃₁H₄₉N₉O₁₆[B1]
MW	805.8 [A1] 803.8 [B1]
CAS	752989-46-1 [Mixture A1/B1] 752989-45-0 [A1] 752989-44-9 [B1]
Source/Host Chemicals	Isolated from Actinomadura sp.
Purity Chemicals	≥70% (HPLC, for A1/B1)
Appearance	White to off-white powder.
Solubility	Soluble in DMSO or water.
Identity	Determined by ¹H-NMR and MS.
Declaration	Manufactured by Naicons Srl.
Other Product Data	Purity Note:The purity is referred exclusively to the main congener(s), the sample also contains minor related congeners. See: Antibiotics GE23077, novel inhibitors of bacterial RNA polymerase. I. Taxonomy, isolation and characterization: I. Ciciliato, et al.; J. Antibiot. 57, 210 (2004)
InChi Key	LHEVPJVFNYHCLJ-USIKRYRBSA-N
Smiles	O=C1NC(CNC(/C(C)=C/C)=O)C(NC(CO)C(NC(C(C)C)C(NC(C(NC(C(C)O)C(NCC(O)C(NC1C(O)=O)=O)=O)=O)C(C(C(N)=O)O)O)=O)=O)=O.O=C2NC(CNC(C(C)CC)=O)C(NC(CO)C(NC(C(C)C)C(NC(C(NC(C(C)O)C(NCC(O)C(NC2C(O)=O)=O)=O)=O)C(C(C(N)=O)O)O)=O)=O)=O
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Keep cool and dry. Protect from light. Protect from light when in solution.
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Description

Cyclic heptapeptide antibiotic.
Potent and selective inhibitor of bacterial RNA polymerase (RNAP). Inhibits Gram-positive (Bacillus subtilis) and Gram-negative (Escherichia coli) RNAPs with IC₅₀ ~20nM, whereas it is not active on E. coli DNA polymerase or on eukaryotic (wheat germ) RNAP II (IC₅₀ values >100µM).
Even though of its potent activity in vitro on purified bacterial RNAPs, it shows a narrow spectrum of antimicrobial activity in vivo on Gram-positive and Gram-negative bacteria, due to lack of membrane permeability.
Acts at the level of transcription initiation. Binds directly to the bacterial RNA polymerase (RNAP) active-center 'i' and 'i+1' nucleotide binding sites, preventing the binding of initiating nucleotides and thereby preventing transcription initiation.
Tool for mechanistic studies on bacterial RNAP and for potential anti-infective drug discovery.

Product References

Antibiotics GE23077, novel inhibitors of bacterial RNA polymerase. I. Taxonomy, isolation and characterization: I. Ciciliato, et al.; J. Antibiot. 57, 210 (2004)
Mode of action of the microbial metabolite GE23077, a novel potent and selective inhibitor of bacterial RNA polymerase: E. Sarubbi, et al.; Eur. J. Biochem. 271, 3146 (2004)
Antibiotics GE23077, novel inhibitors of bacterial RNA polymerase. II. Structure elucidation: A. Marazzi, et al.; J. Antibiot. 58, 260 (2005)
Antibiotics GE23077, novel inhibitors of bacterial RNA polymerase. Part 3: Chemical derivatization: R. Mariani, et al.; Bioorg. Med. Chem. Lett. 15, 3748 (2005)
GE23077 binds to the RNA polymerase 'i' and 'i+1' sites and prevents the binding of initiating nucleotides: Y. Zhang, et al.; Elife 3, e02450 (2014)

Call	+41 61 926 6040
Fax	+41 61 926 6049